Professor Fairlie is an NHMRC Research Investigator Fellow (Level 3) (2022-present), a Node Leader of the ARC Centre of Excellence for Innovations in Peptide Protein Science, one of four Centre Directors and former Head of the Division of Chemistry of Structural Biology at the Institute for Molecular Bioscience (since 2009), and an Affiliate Professor of the School of Chemistry and Molecular Biosciences. He was previously an NHMRC Senior Principal Research Fellow (2012-2021), a Node Leader at the ARC Centre of Excellence in Advanced Molecular Imaging (2014-2021), an ARC Federation Fellow (2006-2011), an ARC Professorial Fellow (2002-2006), and Scientific Director and Chief Scientific Officer of a startup company. He undertook postdoctoral studies at Stanford University and University of Toronto, postgraduate studies at Australian National University and University of New South Wales, and undergraduate studies at University of Adelaide.
His research group works across the disciplines of chemistry (synthesis, structure, reaction mechanisms), biochemistry (enzyme inhibitors, protein-protein interactions, GPCRs, transcription factors), immunology (innate immune cells in health and disease, mucosal T cells), and pharmacology (molecular pharmacology and human cell signalling, experimental pharmacology in rodent models of human diseases). He has published over 450 scientific journal articles in high impact chemistry journals (e.g. Chem Rev, J Am Chem Soc, Angew Chem Int Edit, Chem Sci, J Med Chem, Org Lett, J Org Chem) and biology journals (e.g. Nature, Science, Nature Immunology, Immunity, Science Immunology, Nature Communications, J Exp Med, J Clin Invest, Proc Natl Acad Sci, Diabetes, Cancer Res, Br J Pharmacol). He has been a Highly Cited Researcher (Clarivate Analytics), with over 37,000 citations and 104 publications with over 100 citations (Google Scholar), and has collaborated with many of the world’s largest pharmaceutical and biotechnology companies.
Our researchers work at interfaces of chemistry and biology to better understand the molecular mechanisms of life, ageing, disease and death.
Our chemists study organic, medicinal and biological chemistry, especially using organic synthesis, computer-aided molecular design, nuclear magnetic resonance spectroscopy to create new chemical structures that interact with or mimic protein surfaces. We discover new chemical structures, reactions and mechanisms; enzyme inhibitors, agonists and antagonists of protein function; and molecules that mimic the structures and functions of bioactive protein surfaces.
Our biologists study mechanisms of protein and cell activation, signalling pathways, biological processes, disease development and drug action. We use novel experimental compounds discovered in our group as molecular tools to interrogate the functions of human proteins and cells, and apply some of them to the treatment of animal models of human diseases.
Our interdisciplinary expertise can be combined across multiple subdisciplines of chemistry and biology to gain insights into biochemical processes, human physiology, disease pathology, and we develop skills in biochemistry, pharmacology, virology, immunology, oncology or neurobiology. We work, in some cases with industry partners, to discover new basic research and apply some of our discoveries to develop experimental treatments for viral or parasitic infections, such as HIV, dengue fever and malaria; inflammatory diseases, such as arthritis, asthma, inflammatory bowel disease and rare immunological disorders; metabolic and cardiovascular disorders linked to obesity and type 2 diabetes; neurodegenerative diseases and cancers.
Journal Article: Achiral derivatives of hydroxamate AR-42 potently inhibit class I HDAC enzymes and cancer cell proliferation
Tng, Jiahui, Lim, Junxian, Wu, Kai-Chen, Lucke, Andrew J., Xu, Weijun, Reid, Robert C. and Fairlie, David P. (2020). Achiral derivatives of hydroxamate AR-42 potently inhibit class I HDAC enzymes and cancer cell proliferation. Journal of Medicinal Chemistry, 63 (11) acs.jmedchem.0c00230, 5956-5971. doi: 10.1021/acs.jmedchem.0c00230
Journal Article: The molecular basis underpinning the potency and specificity of MAIT cell antigens
Awad, Wael, Ler, Geraldine J. M., Xu, Weijun, Keller, Andrew N., Mak, Jeffrey Y. W., Lim, Xin Yi, Liu, Ligong, Eckle, Sidonia B. G., Le Nours, Jérôme, McCluskey, James, Corbett, Alexandra J., Fairlie, David P. and Rossjohn, Jamie (2020). The molecular basis underpinning the potency and specificity of MAIT cell antigens. Nature Immunology, 21 (4), 400-411. doi: 10.1038/s41590-020-0616-6
Journal Article: A novel long-range n to π* interaction secures the smallest known α-helix in water
Hoang, Huy N., Wu, Chongyang, Hill, Timothy A., Dantas de Araujo, Aline, Bernhardt, Paul V., Liu, Ligong and Fairlie, David P. (2019). A novel long-range n to π* interaction secures the smallest known α-helix in water. Angewandte Chemie International Edition, 58 (52) ange.201911277, 18873-18877. doi: 10.1002/anie.201911277
Journal Article: Alpha-synuclein structure and Parkinson's disease - Lessons and emerging principles
Meade, Richard M., Fairlie, David P. and Mason, Jody M. (2019). Alpha-synuclein structure and Parkinson's disease - Lessons and emerging principles. Molecular Neurodegeneration, 14 (1) 29, 29. doi: 10.1186/s13024-019-0329-1
Journal Article: Inhibitors of class I histone deacetylases attenuate thioacetamide-induced liver fibrosis in mice by suppressing hepatic Type 2 inflammation
Loh, Zhixuan, Fitzsimmons, Rebecca L., Reid, Robert C., Ramnath, Divya, Clouston, Andrew, Gupta, Praveer K., Irvine, Katharine M., Powell, Elizabeth E., Schroder, Kate, Stow, Jennifer L., Sweet, Matthew J., Fairlie, David P. and Iyer, Abishek (2019). Inhibitors of class I histone deacetylases attenuate thioacetamide-induced liver fibrosis in mice by suppressing hepatic Type 2 inflammation. British Journal of Pharmacology, 176 (19) bph.14768, 3775-3790. doi: 10.1111/bph.14768
Journal Article: Twists or turns: stabilising alpha vs. beta turns in tetrapeptides
Hoang, Huy N., Hill, Timothy A., Ruiz-Gómez, Gloria, Diness, Frederik, Mason, Jody M., Wu, Chongyang, Abbenante, Giovanni, Shepherd, Nicholas E. and Fairlie, David P. (2019). Twists or turns: stabilising alpha vs. beta turns in tetrapeptides. Chemical Science, 10 (45), 10595-10600. doi: 10.1039/c9sc04153b
Journal Article: Glucuronic acid as a helix-inducing linker in short peptides
Wu, Chongyang, Hoang, Huy N, Liu, Ligong and Fairlie, David P (2018). Glucuronic acid as a helix-inducing linker in short peptides. Chemical Communications, 54 (17), 2162-2165. doi: 10.1039/c7cc09785a
Journal Article: Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a
Lohman, Rink-Jan, Hamidon, Johan K., Reid, Robert C., Rowley, Jessica A., Yau, Mei-Kwan, Halili, Maria A., Nielsen, Daniel S., Lim, Junxian, Wu, Kai-Chen, Loh, Zhixuan, Do, Anh, Suen, Jacky Y., Iyer, Abishek and Fairlie, David P. (2017). Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a. Nature Communications, 8 (1) 351, 351. doi: 10.1038/s41467-017-00414-w
Journal Article: Stabilizing short-lived Schiff base derivatives of 5-aminouracils that activate mucosal-associated invariant T cells
Mak, Jeffrey Y. W., Xu, Weijun, Reid, Robert C., Corbett, Alexandra J., Meehan, Bronwyn S., Wang, Huimeng, Chen, Zhenjun, Rossjohn, Jamie, McCluskey, James, Liu, Ligong and Fairlie, David P. (2017). Stabilizing short-lived Schiff base derivatives of 5-aminouracils that activate mucosal-associated invariant T cells. Nature Communications, 8 (1) 14599, 14599. doi: 10.1038/ncomms14599
Journal Article: Electrophilic helical peptides that bond covalently, irreversibly, and selectively in a protein-protein interaction site
Dantas De Araujo, Aline, Lim, Junxian, Good, Andrew C., Skerlj, Renato T. and Fairlie, David P. (2017). Electrophilic helical peptides that bond covalently, irreversibly, and selectively in a protein-protein interaction site. ACS Medicinal Chemistry Letters, 8 (1), 22-26. doi: 10.1021/acsmedchemlett.6b00395
Journal Article: Membrane-anchored serine protease matriptase is a trigger of pulmonary fibrogenesis
Bardou, Oliver, Menou, Awen, Francois, Charlene, Duitman, Jan Willem, von der Thusen, Jan H., Borie, Raphael, Sales, Katiuchia Uzzun, Mutze, Kathrin, Castier, Yves, Sage, Edouard, Liu, Ligong, Bugge, Thomas H., Fairlie, David P., Konigshoff, Melanie, Crestani, Bruno and Borensztain, Keren S. (2015). Membrane-anchored serine protease matriptase is a trigger of pulmonary fibrogenesis. American Journal of Respiratory and Critical Care Medicine, 193 (8), 847-860. doi: 10.1164/rccm.201502-0299OC
Journal Article: Improving on nature: making a cyclic heptapeptide orally bioavailable
Nielsen, Daniel S., Hoang, Huy N., Lohman, Rink-Jan, Hill, Timothy A., Lucke, Andrew J., Craik, David J., Edmonds, David J., Griffith, David A., Rotter, Charles J., Ruggeri, Roger B., Price, David A., Liras, Spiros and Fairlie, David P. (2014). Improving on nature: making a cyclic heptapeptide orally bioavailable. Angewandte Chemie - International Edition, 53 (45), 12059-12063. doi: 10.1002/anie.201405364
Journal Article: Constraining cyclic peptides to mimic protein structure motifs
Hill, Timothy A., Shepherd, Nicholas E., Diness, Frederik and Fairlie, David P. (2014). Constraining cyclic peptides to mimic protein structure motifs. Angewandte Chemie (International Edition), 53 (48), 13020-13041. doi: 10.1002/anie.201401058
Journal Article: Pathway-selective antagonism of proteinase activated receptor 2
Suen, J. Y., Cotterell, A., Lohman, R. J., Lim, J., Han, A., Yau, M. K., Liu, L., Cooper, M. A., Vesey, D. A. and Fairlie, D. P. (2014). Pathway-selective antagonism of proteinase activated receptor 2. British Journal of Pharmacology, 171 (17), 4112-4124. doi: 10.1111/bph.12757
Journal Article: Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides
Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Lim, Junxian and Fairlie, David P. (2014). Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides. Journal of the American Chemical Society, 136 (34), 11914-11917. doi: 10.1021/ja506518t
Journal Article: Complement c5a receptor facilitates cancer metastasis by altering t-cell responses in the metastatic niche
Vadrevu, Saurya Kumari, Chintala, Navin K., Sharma, Sharad K., Sharma, Priya, Cleveland, Clayton, Riediger, Linley, Manne, Sasikanth, Fairlie, David P., Gorczyca, Wojciech, Almanza, Othon, Karbowniczek, Magdalena and Markiewski, Maciej M. (2014). Complement c5a receptor facilitates cancer metastasis by altering t-cell responses in the metastatic niche. Cancer Research, 74 (13), 3454-3465. doi: 10.1158/0008-5472.CAN-14-0157
Journal Article: T-cell activation by transitory neo-antigens derived from distinct microbial pathways
Corbett, Alexandra J., Eckle, Sidonia B. G., Birkinshaw, Richard W., Liu, Ligong, Patel, Onisha, Mahony, Jennifer, Chen, Zhenjun, Reantragoon, Rangsima, Meehan, Bronwyn, Cao, Hanwei, Williamson, Nicholas A., Strugnell, Richard A., Van Sinderen, Douwe, Mak, Jeffrey Y. W., Fairlie, David P., Kjer-Nielsen, Lars, Rossjohn, Jamie and McClusky, James (2014). T-cell activation by transitory neo-antigens derived from distinct microbial pathways. Nature, 509 (7500), 361-365. doi: 10.1038/nature13160
Journal Article: Downsizing a human inflammatory protein to a small molecule with equal potency and functionality
Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Hamidon, Johan K., Reed, Anthony N., Chu, Peifei, Suen, Jacky Y., Stoermer, Martin J., Blakeney, Jade S., Lim, Junxian, Faber, Jonathan M. and David P. Fairlie, (2013). Downsizing a human inflammatory protein to a small molecule with equal potency and functionality. Nature Communications, 4 (2802) 2802, 1-9. doi: 10.1038/ncomms3802
Developing a new type of drug for inflammatory lung disease
(2023–2025) NHMRC Development Grant
Modulating protein-protein interactions in disease
(2022–2026) NHMRC Investigator Grants
Targeting CEP55 in triple-negative breast cancer
(2022–2025) United States Congressionally Directed Medical Research Programs - Breast Cancer Research Program
Peptide modulators for drug discovery
Doctor Philosophy
Novel chemical approaches to drugs that selectively target immune cells
Doctor Philosophy
New strategies in heterocyclic chemistry for drug discovery
Doctor Philosophy
Targeting strategies for drug design
Selective binding of small molecules with proteins underpins most drug discovery. However, while a compound can be devised to interact with a single protein, this cannot drive the molecule into a specific location where functional modulation of the target protein only at that location is desired for therapy. Instead, designed compounds usually bind to the protein wherever it is expressed in the body and this can be deterimental to normal healthy physiology. This project will investigate a number of promising new approaches to directing protein-binding compounds to specific compartments of cells and organisms. It will require a combination of organic synthesis, medicinal chemistry, molecular modelling and chemical biology. The new approaches will be tested and optimised with the goal of inhibiting or activating desired proteins in specific compartments in order to modulate disease-causing protein functions without altering normal healthy physiology. Achieving these aims will require enthusiasm, a high degree of self-motivation, lateral thinking, strong chemical knowledge and hands-on skills in organic synthesis (solution and solid phase), NMR characterisation (including 2D NMR structure analysis), HPLC purification, mass spectrometry, and computer modelling. Some knowledge of enzyme assays and cell biology would be an advantage. The long term goal is to design new compounds and profile them for selective effects on target genes/proteins/cells/rodent models of inflammatory diseases and cancer. Outcomes will include new knowledge of protein function in disease; greater understanding of medicinal and organic chemistry in drug design, drug targeting, mechanisms and effectiveness of drug action; patentable methods and bioactive compounds; and new experimental leads to new medicines for development towards the clinic.
Tng, Jiahui, Lim, Junxian, Wu, Kai-Chen, Lucke, Andrew J., Xu, Weijun, Reid, Robert C. and Fairlie, David P. (2020). Achiral derivatives of hydroxamate AR-42 potently inhibit class I HDAC enzymes and cancer cell proliferation. Journal of Medicinal Chemistry, 63 (11) acs.jmedchem.0c00230, 5956-5971. doi: 10.1021/acs.jmedchem.0c00230
The molecular basis underpinning the potency and specificity of MAIT cell antigens
Awad, Wael, Ler, Geraldine J. M., Xu, Weijun, Keller, Andrew N., Mak, Jeffrey Y. W., Lim, Xin Yi, Liu, Ligong, Eckle, Sidonia B. G., Le Nours, Jérôme, McCluskey, James, Corbett, Alexandra J., Fairlie, David P. and Rossjohn, Jamie (2020). The molecular basis underpinning the potency and specificity of MAIT cell antigens. Nature Immunology, 21 (4), 400-411. doi: 10.1038/s41590-020-0616-6
A novel long-range n to π* interaction secures the smallest known α-helix in water
Hoang, Huy N., Wu, Chongyang, Hill, Timothy A., Dantas de Araujo, Aline, Bernhardt, Paul V., Liu, Ligong and Fairlie, David P. (2019). A novel long-range n to π* interaction secures the smallest known α-helix in water. Angewandte Chemie International Edition, 58 (52) ange.201911277, 18873-18877. doi: 10.1002/anie.201911277
Alpha-synuclein structure and Parkinson's disease - Lessons and emerging principles
Meade, Richard M., Fairlie, David P. and Mason, Jody M. (2019). Alpha-synuclein structure and Parkinson's disease - Lessons and emerging principles. Molecular Neurodegeneration, 14 (1) 29, 29. doi: 10.1186/s13024-019-0329-1
Loh, Zhixuan, Fitzsimmons, Rebecca L., Reid, Robert C., Ramnath, Divya, Clouston, Andrew, Gupta, Praveer K., Irvine, Katharine M., Powell, Elizabeth E., Schroder, Kate, Stow, Jennifer L., Sweet, Matthew J., Fairlie, David P. and Iyer, Abishek (2019). Inhibitors of class I histone deacetylases attenuate thioacetamide-induced liver fibrosis in mice by suppressing hepatic Type 2 inflammation. British Journal of Pharmacology, 176 (19) bph.14768, 3775-3790. doi: 10.1111/bph.14768
Twists or turns: stabilising alpha vs. beta turns in tetrapeptides
Hoang, Huy N., Hill, Timothy A., Ruiz-Gómez, Gloria, Diness, Frederik, Mason, Jody M., Wu, Chongyang, Abbenante, Giovanni, Shepherd, Nicholas E. and Fairlie, David P. (2019). Twists or turns: stabilising alpha vs. beta turns in tetrapeptides. Chemical Science, 10 (45), 10595-10600. doi: 10.1039/c9sc04153b
Glucuronic acid as a helix-inducing linker in short peptides
Wu, Chongyang, Hoang, Huy N, Liu, Ligong and Fairlie, David P (2018). Glucuronic acid as a helix-inducing linker in short peptides. Chemical Communications, 54 (17), 2162-2165. doi: 10.1039/c7cc09785a
Lohman, Rink-Jan, Hamidon, Johan K., Reid, Robert C., Rowley, Jessica A., Yau, Mei-Kwan, Halili, Maria A., Nielsen, Daniel S., Lim, Junxian, Wu, Kai-Chen, Loh, Zhixuan, Do, Anh, Suen, Jacky Y., Iyer, Abishek and Fairlie, David P. (2017). Exploiting a novel conformational switch to control innate immunity mediated by complement protein C3a. Nature Communications, 8 (1) 351, 351. doi: 10.1038/s41467-017-00414-w
Mak, Jeffrey Y. W., Xu, Weijun, Reid, Robert C., Corbett, Alexandra J., Meehan, Bronwyn S., Wang, Huimeng, Chen, Zhenjun, Rossjohn, Jamie, McCluskey, James, Liu, Ligong and Fairlie, David P. (2017). Stabilizing short-lived Schiff base derivatives of 5-aminouracils that activate mucosal-associated invariant T cells. Nature Communications, 8 (1) 14599, 14599. doi: 10.1038/ncomms14599
Dantas De Araujo, Aline, Lim, Junxian, Good, Andrew C., Skerlj, Renato T. and Fairlie, David P. (2017). Electrophilic helical peptides that bond covalently, irreversibly, and selectively in a protein-protein interaction site. ACS Medicinal Chemistry Letters, 8 (1), 22-26. doi: 10.1021/acsmedchemlett.6b00395
Membrane-anchored serine protease matriptase is a trigger of pulmonary fibrogenesis
Bardou, Oliver, Menou, Awen, Francois, Charlene, Duitman, Jan Willem, von der Thusen, Jan H., Borie, Raphael, Sales, Katiuchia Uzzun, Mutze, Kathrin, Castier, Yves, Sage, Edouard, Liu, Ligong, Bugge, Thomas H., Fairlie, David P., Konigshoff, Melanie, Crestani, Bruno and Borensztain, Keren S. (2015). Membrane-anchored serine protease matriptase is a trigger of pulmonary fibrogenesis. American Journal of Respiratory and Critical Care Medicine, 193 (8), 847-860. doi: 10.1164/rccm.201502-0299OC
Improving on nature: making a cyclic heptapeptide orally bioavailable
Nielsen, Daniel S., Hoang, Huy N., Lohman, Rink-Jan, Hill, Timothy A., Lucke, Andrew J., Craik, David J., Edmonds, David J., Griffith, David A., Rotter, Charles J., Ruggeri, Roger B., Price, David A., Liras, Spiros and Fairlie, David P. (2014). Improving on nature: making a cyclic heptapeptide orally bioavailable. Angewandte Chemie - International Edition, 53 (45), 12059-12063. doi: 10.1002/anie.201405364
Constraining cyclic peptides to mimic protein structure motifs
Hill, Timothy A., Shepherd, Nicholas E., Diness, Frederik and Fairlie, David P. (2014). Constraining cyclic peptides to mimic protein structure motifs. Angewandte Chemie (International Edition), 53 (48), 13020-13041. doi: 10.1002/anie.201401058
Pathway-selective antagonism of proteinase activated receptor 2
Suen, J. Y., Cotterell, A., Lohman, R. J., Lim, J., Han, A., Yau, M. K., Liu, L., Cooper, M. A., Vesey, D. A. and Fairlie, D. P. (2014). Pathway-selective antagonism of proteinase activated receptor 2. British Journal of Pharmacology, 171 (17), 4112-4124. doi: 10.1111/bph.12757
Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Lim, Junxian and Fairlie, David P. (2014). Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides. Journal of the American Chemical Society, 136 (34), 11914-11917. doi: 10.1021/ja506518t
Vadrevu, Saurya Kumari, Chintala, Navin K., Sharma, Sharad K., Sharma, Priya, Cleveland, Clayton, Riediger, Linley, Manne, Sasikanth, Fairlie, David P., Gorczyca, Wojciech, Almanza, Othon, Karbowniczek, Magdalena and Markiewski, Maciej M. (2014). Complement c5a receptor facilitates cancer metastasis by altering t-cell responses in the metastatic niche. Cancer Research, 74 (13), 3454-3465. doi: 10.1158/0008-5472.CAN-14-0157
T-cell activation by transitory neo-antigens derived from distinct microbial pathways
Corbett, Alexandra J., Eckle, Sidonia B. G., Birkinshaw, Richard W., Liu, Ligong, Patel, Onisha, Mahony, Jennifer, Chen, Zhenjun, Reantragoon, Rangsima, Meehan, Bronwyn, Cao, Hanwei, Williamson, Nicholas A., Strugnell, Richard A., Van Sinderen, Douwe, Mak, Jeffrey Y. W., Fairlie, David P., Kjer-Nielsen, Lars, Rossjohn, Jamie and McClusky, James (2014). T-cell activation by transitory neo-antigens derived from distinct microbial pathways. Nature, 509 (7500), 361-365. doi: 10.1038/nature13160
Downsizing a human inflammatory protein to a small molecule with equal potency and functionality
Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Hamidon, Johan K., Reed, Anthony N., Chu, Peifei, Suen, Jacky Y., Stoermer, Martin J., Blakeney, Jade S., Lim, Junxian, Faber, Jonathan M. and David P. Fairlie, (2013). Downsizing a human inflammatory protein to a small molecule with equal potency and functionality. Nature Communications, 4 (2802) 2802, 1-9. doi: 10.1038/ncomms3802
Thiazoles in peptides and peptidomimetics
Mak, Jeffrey Y. W., Xu, Weijun and Fairlie, David P. (2017). Thiazoles in peptides and peptidomimetics. Peptidomimetics I. (pp. 235-266) edited by William D. Lubell. Cham, Switzerland: Springer. doi: 10.1007/7081_2015_176
Helix-constrained nociceptin peptides are potent agonists and antagonists of ORL-1 and nociception
Lohman, Rink-Jan, Harrison, Rosemary S., Ruiz-Gomez, Gloria, Hoang, Huy Ngoc, Shepherd, Nicholas E., Chow, Shiao, Hill, Timothy A., Madala, Praveen K. and Fairlie, David P. (2015). Helix-constrained nociceptin peptides are potent agonists and antagonists of ORL-1 and nociception. Nociceptin opioid. (pp. 1-55) edited by Gerald Litwack. Maryland Heights, MO, United States: Academic Press. doi: 10.1016/bs.vh.2014.10.001
Recent advances in β-Strand mimetics
Loughlin, Wendy A. and Fairlie, David P. (2011). Recent advances in β-Strand mimetics. Amino acids, peptides and proteins in organic chemistry: protection reactions, medicinal chemistry, combinatorial synthesis. (pp. 129-147) edited by Andrew B. Hughes. Somerset, NJ, United States: Wiley-VCH. doi: 10.1002/9783527631827.ch3
Tumor-associated antigenic peptides as vaccine candidates
Hans, Dhiraj, Young, Paul R. and Fairlie, David P. (2009). Tumor-associated antigenic peptides as vaccine candidates. Tumor-associated antigens. (pp. 303-316) edited by Olivier Gires and Barbara Seliger. Weinheim, Germany: Wiley - VCH Verlag. doi: 10.1002/9783527625970.ch17
Reid, Robert, C. and Fairlie, David P. (2008). Parallel synthesis af anticancer, antiinflammatory and antiviral agents derived from L- and D- amino acids. High-throughput lead optimisation in drug discovery. (pp. 177-194) edited by Tushar Kshirsagar. Boca Raton, USA: CRC Press.
Amyloid peptides and proteins in review
Harrison, R. S., Sharpe, P. C., Singh, Y. and Fairlie, D. P. (2007). Amyloid peptides and proteins in review. Reviews of physiology, biochemistry and pharmacology. (pp. 1-77) edited by S. G. Amara, B. Bamberg, T. Fleischmann, S. C. Gudermann, S. C. Hebert, R. Jahn, W. J. Lederer, R. Lill, A. Miyajima, S. Offermanns and R. Zechner. Berlin, Germany: Springer. doi: 10.1007/112_2007_0701
Discovery of Potent Cyclic Antagonists of Human C5a Receptors
Taylor, S. M. and Fairlie, D. (2005). Discovery of Potent Cyclic Antagonists of Human C5a Receptors. Structural Biology of the Complement System. (pp. 341-362) edited by I. Morikis and J Lambris. New York: CRC Press, Taylor and Francis.
Current approaches to peptidomimetics
Kelso, M. J. and Fairlie, D. (2003). Current approaches to peptidomimetics. Molecular Pathomechanisms and New Trends in Drug Research. (pp. 579-598) edited by I. Toth and G. Keri. London and New York: Taylor and Francis.
Fairlie, D. P. and Reid, R. C. (1997). Mimicking extended conformations of protease substrates: Designing cyclic peptidomimetics to inhibit HIV-1 protease. Advances in amino acid mimetics and peptidomimetics. (pp. 77-107) London: JAI Press Inc.
Protease-activated receptor 2 attenuates doxorubicin-induced apoptosis in colon cancer cells
Shah, Himani, Hill, Timothy A., Lim, Junxian and Fairlie, David P. (2023). Protease-activated receptor 2 attenuates doxorubicin-induced apoptosis in colon cancer cells. Journal of Cell Communication and Signaling, 1-15. doi: 10.1007/s12079-023-00791-6
Gerokonstantis, Dimitrios Triantafyllos, Mantzourani, Christiana, Gkikas, Dimitrios, Wu, Kai-Chen, Hoang, Huy N., Triandafillidi, Ierasia, Barbayianni, Ilianna, Kanellopoulou, Paraskevi, Kokotos, Alexandros C., Moutevelis-Minakakis, Panagiota, Aidinis, Vassilis, Politis, Panagiotis K., Fairlie, David P. and Kokotos, George (2023). N-(2-Aminophenyl)-benzamide Inhibitors of Class I HDAC Enzymes with Antiproliferative and Antifibrotic Activity. Journal of Medicinal Chemistry, 66 (20), 1-20. doi: 10.1021/acs.jmedchem.3c01422
Salim, Angela A., Hussein, Waleed M., Dewapriya, Pradeep, Hoang, Huy N., Zhou, Yahao, Samarasekera, Kaumadi, Khalil, Zeinab G., Fairlie, David P. and Capon, Robert J. (2023). Talarolides Revisited: Cyclic Heptapeptides from an Australian Marine Tunicate-Associated Fungus, Talaromyces sp. CMB-TU011. Marine Drugs, 21 (9) 487, 487. doi: 10.3390/md21090487
Nelson, Adam G., Wang, Huimeng, Dewar, Phoebe M., Eddy, Eleanor M., Li, Songyi, Lim, Xin Yi, Patton, Timothy, Zhou, Yuchen, Pediongco, Troi J., Meehan, Lucy J., Meehan, Bronwyn S., Mak, Jeffrey Y. W., Fairlie, David P., Stent, Andrew W., Kjer-Nielsen, Lars, McCluskey, James, Eckle, Sidonia B. G., Corbett, Alexandra J., Souter, Michael N. T. and Chen, Zhenjun (2023). Synthetic 5-amino-6-D-ribitylaminouracil paired with inflammatory stimuli facilitates MAIT cell expansion in vivo. Frontiers in Immunology, 14 1109759. doi: 10.3389/fimmu.2023.1109759
Molecular insights into metabolite antigen recognition by mucosal-associated invariant T cells
Awad, Wael, Ciacchi, Lisa, McCluskey, James, Fairlie, David P and Rossjohn, Jamie (2023). Molecular insights into metabolite antigen recognition by mucosal-associated invariant T cells. Current Opinion in Immunology, 83 102351, 102351. doi: 10.1016/j.coi.2023.102351
Goudarzi, Mohaddeseh H., Eagles, David A., Lim, Junxian, Biggs, Kimberley A., Kotze, Andrew C., Ruffell, Angela P., Fairlie, David P., King, Glenn F. and Walker, Andrew A. (2023). Venom composition and bioactive RF-amide peptide toxins of the saddleback caterpillar, Acharia stimulea (Lepidoptera: Limacodidae). Biochemical Pharmacology, 213 115598, 1-11. doi: 10.1016/j.bcp.2023.115598
Rollo, Rachel F., Mori, Giorgia, Hill, Timothy A., Hillemann, Doris, Niemann, Stefan, Homolka, Susanne, Fairlie, David P. and Blumenthal, Antje (2023). Wollamide Cyclic Hexapeptides Synergize with Established and New Tuberculosis Antibiotics in Targeting Mycobacterium tuberculosis. Microbiology Spectrum, 11 (4). doi: 10.1128/spectrum.00465-23
Francis, Nidhish, Sanaei, Reza, Ayodele, Babatunde A., O'Brien‐Simpson, Neil M., Fairlie, David P., Wijeyewickrema, Lakshmi C., Pike, Robert N., Mackie, Eleanor Jean and Pagel, Charles Neil (2023). Effect of a protease‐activated receptor‐2 antagonist (GB88) on inflammation‐related loss of alveolar bone in periodontal disease. Journal of Periodontal Research, 58 (3), 544-552. doi: 10.1111/jre.13120
Wang, Yizhuo, Abrol, Rishika, Mak, Jeffrey Y. W., Das Gupta, Kaustav, Ramnath, Divya, Karunakaran, Denuja, Fairlie, David P. and Sweet, Matthew J. (2023). Histone deacetylase 7: a signalling hub controlling development, inflammation, metabolism and disease. The FEBS Journal, 290 (11), 2805-2832. doi: 10.1111/febs.16437
Suppression of MR1 by human cytomegalovirus inhibits MAIT cell activation
Ashley, Caroline L., McSharry, Brian P., McWilliam, Hamish E. G., Stanton, Richard J., Fielding, Ceri A., Mathias, Rommel A., Fairlie, David P., McCluskey, James, Villadangos, Jose A., Rossjohn, Jamie, Abendroth, Allison and Slobedman, Barry (2023). Suppression of MR1 by human cytomegalovirus inhibits MAIT cell activation. Frontiers in Immunology, 14 1107497, 1-13. doi: 10.3389/fimmu.2023.1107497
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Wu, Kai-Chen, Condon, Nicholas D., Hill, Timothy A., Reid, Robert C., Fairlie, David and Lim, Junxian (2023). Ras related protein Rab5a regulates complement C5a receptor trafficking, chemotaxis and chemokine secretion in human macrophages. Journal of Innate Immunity, 15 (1), 468-484. doi: 10.1159/000530012
Wang, Carl J.H., Awad, Wael, Liu, Ligong, Mak, Jeffrey Y.W., Veerapen, Natacha, Illing, Patricia T., Purcell, Anthony W., Eckle, Sidonia B.G., McCluskey, James, Besra, Gurdyal S., Fairlie, David P., Rossjohn, Jamie and Le Nours, Jérôme (2022). Quantitative affinity measurement of small molecule ligand binding to Major Histocompatibility Complex class-I related protein 1 MR1. Journal of Biological Chemistry, 298 (12) 102714, 1-12. doi: 10.1016/j.jbc.2022.102714
Helical structure in cyclic peptides: effect of N-methyl amides versus esters
Wu, Chongyang, Hoang, Huy N., Hill, Timothy A., Lim, Junxian, Kok, W. Mei, Akondi, Kalyani, Liu, Ligong and Fairlie, David P. (2022). Helical structure in cyclic peptides: effect of N-methyl amides versus esters. Chemical Communications, 58 (89), 12475-12478. doi: 10.1039/d2cc05092g
A specialized tyrosine-based endocytosis signal in MR1 controls antigen presentation to MAIT cells
Lim, Hui Jing, Wubben, Jacinta M., Garcia, Cristian Pinero, Cruz-Gomez, Sebastian, Deng, Jieru, Mak, Jeffrey Y.W., Hachani, Abderrahman, Anderson, Regan J., Painter, Gavin F., Goyette, Jesse, Amarasinghe, Shanika L., Ritchie, Matthew E., Roquilly, Antoine, Fairlie, David P., Gaus, Katharina, Rossjohn, Jamie, Villadangos, Jose A. and McWilliam, Hamish E.G. (2022). A specialized tyrosine-based endocytosis signal in MR1 controls antigen presentation to MAIT cells. Journal of Cell Biology, 221 (12) e202110125. doi: 10.1083/jcb.202110125
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Wang, Peiqi, Hill, Timothy A., Mitchell, Justin, Fitzsimmons, Rebecca L., Xu, Weijun, Loh, Zhixuan, Suen, Jacky Y., Lim, Junxian, Iyer, Abishek and Fairlie, David P. (2022). Modifying a hydroxyl patch in glucagon-like peptide 1 produces biased agonists with unique signaling profiles. Journal of Medicinal Chemistry, 65 (17), 11759-11775. doi: 10.1021/acs.jmedchem.2c00653
de Araujo, Aline Dantes, Hoang, Huy N., Lim, Junxian, Mak, Jeffrey and Fairlie, David P. (2022). Tuning electrostatic and hydrophobic surfaces of aromatic rings to enhance membrane association and cell uptake of peptides. Angewandte Chemie International Edition, 61 (29) e202203995, e202203995. doi: 10.1002/anie.202203995
de Araujo, Aline D., Lim, Junxian, Wu, Kai-Chen, Hoang, Huy N., Nguyen, Huy T. and Fairlie, David P. (2022). Landscaping macrocyclic peptides: stapling hDM2-binding peptides for helicity, protein affinity, proteolytic stability and cell uptake. RSC Chemical Biology, 3 (7), 895-904. doi: 10.1039/d1cb00231g
de Araujo, Aline D., Hoang, Huy N., Lim, Junxian, Mak, Jeffrey Y. W. and Fairlie, David P. (2022). Tuning Electrostatic and Hydrophobic Surfaces of Aromatic Rings to Enhance Membrane Association and Cell Uptake of Peptides. Angewandte Chemie, 134 (29). doi: 10.1002/ange.202203995
Sinniah, Enakshi, Wu, Zhixuan, Shen, Sophie, Naval-Sanchez, Marina, Chen, Xiaoli, Lim, Junxian, Helfer, Abbigail, Iyer, Abishek, Tng, Jiahui, Lucke, Andrew J., Reid, Robert C., Redd, Meredith A., Nefzger, Christian M., Fairlie, David P. and Palpant, Nathan J. (2022). Temporal perturbation of histone deacetylase activity reveals a requirement for HDAC1–3 in mesendoderm cell differentiation. Cell Reports, 39 (7) 110818, 1-21. doi: 10.1016/j.celrep.2022.110818
Wang, Huimeng, Nelson, Adam G., Wang, Bingjie, Zhao, Zhe, Lim, Xin Yi, Shi, Mai, Meehan, Lucy J., Jia, Xiaoxiao, Kedzierska, Katherine, Meehan, Bronwyn S., Eckle, Sidonia B. G., Souter, Michael N. T., Pediongco, Troi J., Mak, Jeffrey Y. W., Fairlie, David P., McCluskey, James, Wang, Zhongfang, Corbett, Alexandra J. and Chen, Zhenjun (2022). The balance of IL ‐12 and IL ‐23 determines the bias of MAIT1 versus MAIT17 responses during bacterial infection. Immunology & Cell Biology, 100 (7), 547-561. doi: 10.1111/imcb.12556
Differential location of NKT and MAIT cells within lymphoid tissue
Johnson, Darryl N., Ruan, Zheng, Petley, Emma V., Devi, Sapna, Holz, Lauren E., Uldrich, Adam P., Mak, Jeffrey Y. W., Hor, Jyh Liang, Mueller, Scott N., McCluskey, James, Fairlie, David P., Darcy, Phillip K., Beavis, Paul A., Heath, William R. and Godfrey, Dale I. (2022). Differential location of NKT and MAIT cells within lymphoid tissue. Scientific Reports, 12 (1) 4034, 4034. doi: 10.1038/s41598-022-07704-4
Ramnath, Divya, Das Gupta, Kaustav, Wang, Yizhuo, Abrol, Rishika, Curson, James E. B., Lim, Junxian, Reid, Robert C., Mansell, Ashley, Blumenthal, Antje, Karunakaran, Denuja, Fairlie, David P. and Sweet, Matthew J. (2022). The histone deacetylase Hdac7 supports LPS‐inducible glycolysis and Il‐1β production in murine macrophages via distinct mechanisms. Journal of Leukocyte Biology, 111 (2), 327-336. doi: 10.1002/jlb.2mr1021-260r
Tran, Thao Thanh, Mathmann, Carmen D., Gatica-Andrades, Marcela, Rollo, Rachel F., Oelker, Melanie, Ljungberg, Johanna K., Nguyen, Tam T. K., Zamoshnikova, Alina, Kummari, Lalith K., Wyer, Orry J. K., Irvine, Katharine M., Melo-Bolívar, Javier, Gross, Annette, Brown, Darren, Mak, Jeffrey Y. W., Fairlie, David P., Hansford, Karl A., Cooper, Matthew A., Giri, Rabina, Schreiber, Veronika, Joseph, Shannon R., Simpson, Fiona, Barnett, Timothy C., Johansson, Jörgen, Dankers, Wendy, Harris, James, Wells, Timothy J., Kapetanovic, Ronan, Sweet, Matthew J. ... Blumenthal, Antje (2022). Inhibition of the master regulator of Listeria monocytogenes virulence enables bacterial clearance from spacious replication vacuoles in infected macrophages. PLoS Pathogens, 18 (1) e1010166, e1010166. doi: 10.1371/journal.ppat.1010166
Hesping, Eva, Chua, Ming Jang, Pflieger, Marc, Qian, Yunan, Dong, Lilong, Bachu, Prabhakar, Liu, Ligong, Kurz, Thomas, Fisher, Gillian M., Skinner-Adams, Tina S., Reid, Robert C., Fairlie, David P., Andrews, Katherine T. and Gorse, Alain-Dominique J.P. (2022). QSAR classification models for prediction of hydroxamate histone deacetylase inhibitor activity against malaria parasites. ACS Infectious Diseases, 8 (1), 106-117. doi: 10.1021/acsinfecdis.1c00355
Human MAIT cells respond to and suppress HIV-1
Phetsouphanh, Chansavath, Phalora, Prabhjeet, Hackstein, Carl-Philipp, Thornhill, John, Munier, Mee Ling, Meyerowitz, Jodi, Murray, Lyle, VanVuuren, Cloete, Goedhals, Dominique, Drexhage, Linnea, Moore, Rebecca, Sattentau, Quentin J, Mak, Jeffrey YW, Fairlie, David P, Fidler, Sarah, Kelleher, Anthony, Frater, John and Klenerman, Paul (2021). Human MAIT cells respond to and suppress HIV-1. eLife, 10 e50324. doi: 10.7554/elife.50324
Chen, Kai-En, Guo, Qian, Hill, Timothy A., Cui, Yi, Kendall, Amy K., Yang, Zhe, Hall, Ryan J., Healy, Michael D., Sacharz, Joanna, Norwood, Suzanne J., Fonseka, Sachini, Xie, Boyang, Reid, Robert C., Leneva, Natalya, Parton, Robert G., Ghai, Rajesh, Stroud, David A., Fairlie, David P, Suga, Hiroaki, Jackson, Lauren P., Teasdale, Rohan D., Passioura, Toby and Collins, Brett M. (2021). De novo macrocyclic peptides for inhibiting, stabilizing, and probing the function of the retromer endosomal trafficking complex. Science Advances, 7 (49) eabg4007, eabg4007. doi: 10.1126/sciadv.abg4007
Synthesis of benzoxazole-based vorinostat analogs and their antiproliferative activity
Mantzourani, Christiana, Gkikas, Dimitrios, Kokotos, Alexandros, Nummela, Pirjo, Theodoropoulou, Maria A., Wu, Kai-Chen, Fairlie, David P., Politis, Panagiotis K., Ristimäki, Ari and Kokotos, George (2021). Synthesis of benzoxazole-based vorinostat analogs and their antiproliferative activity. Bioorganic Chemistry, 114 105132, 1-9. doi: 10.1016/j.bioorg.2021.105132
Chemical modulators of mucosal associated Invariant T cells
Mak, Jeffrey Y.W., Liu, Ligong and Fairlie, David P. (2021). Chemical modulators of mucosal associated Invariant T cells. Accounts of Chemical Research, 54 (17) acs.accounts.1c00359, 3462-3475. doi: 10.1021/acs.accounts.1c00359
MAIT cells regulate NK cell-mediated tumor immunity
Petley, Emma V., Koay, Hui-Fern, Henderson, Melissa A., Sek, Kevin, Todd, Kirsten L., Keam, Simon P., Lai, Junyun, House, Imran G., Li, Jasmine, Zethoven, Magnus, Chen, Amanda X. Y., Oliver, Amanda J., Michie, Jessica, Freeman, Andrew J., Giuffrida, Lauren, Chan, Jack D., Pizzolla, Angela, Mak, Jeffrey Y. W., McCulloch, Timothy R., Souza-Fonseca-Guimaraes, Fernando, Kearney, Conor J., Millen, Rosemary, Ramsay, Robert G., Huntington, Nicholas D., McCluskey, James, Oliaro, Jane, Fairlie, David P., Neeson, Paul J., Godfrey, Dale I. ... Darcy, Phillip K. (2021). MAIT cells regulate NK cell-mediated tumor immunity. Nature Communications, 12 (1) 4746, 1-15. doi: 10.1038/s41467-021-25009-4
Chua, Ming Jang, Tng, Jiahui, Hesping, Eva, Fisher, Gillian M., Goodman, Christopher D., Skinner-Adams, Tina, Do, Darren, Lucke, Andrew J., Reid, Robert C., Fairlie, David P. and Andrews, Katherine T. (2021). Histone deacetylase inhibitor AR-42 and achiral analogues kill malaria parasites in vitro and in mice. International Journal for Parasitology: Drugs and Drug Resistance, 17, 118-127. doi: 10.1016/j.ijpddr.2021.08.006
Zhao, Zhe, Wang, Huimeng, Shi, Mai, Zhu, Tianyuan, Pediongco, Troi, Lim, Xin Yi, Meehan, Bronwyn S., Nelson, Adam G., Fairlie, David P., Mak, Jeffrey Y. W., Eckle, Sidonia B. G., de Lima Moreira, Marcela, Tumpach, Carolin, Bramhall, Michael, Williams, Cameron G., Lee, Hyun Jae, Haque, Ashraful, Evrard, Maximilien, Rossjohn, Jamie, McCluskey, James, Corbett, Alexandra J. and Chen, Zhenjun (2021). Francisella tularensis induces Th1 like MAIT cells conferring protection against systemic and local infection. Nature Communications, 12 (1) 4355, 1-15. doi: 10.1038/s41467-021-24570-2
Humphries, Tyrone L. R., Shen, Kunyu, Iyer, Abishek, Johnson, David W., Gobe, Glenda C., Nikolic-Paterson, David, Fairlie, David P. and Vesey, David A. (2021). PAR2-induced tissue factor synthesis by primary cultures of human kidney tubular epithelial cells is modified by glucose availability. International Journal of Molecular Sciences, 22 (14) 7532, 1-12. doi: 10.3390/ijms22147532
Targeting Class IIa HDACs: insights from henotypes and inhibitors
Liu, Ligong, Dong, Lilong, Bourguet, Erika and Fairlie, David P. (2021). Targeting Class IIa HDACs: insights from henotypes and inhibitors. Current Medicinal Chemistry, 28 (42), 8628-8672. doi: 10.2174/0929867328666210629160647
Araujo, Aline D., Nguyen, Huy T. and Fairlie, David P. (2021). Front Cover: Late‐Stage Hydrocarbon Conjugation and Cyclisation in Synthetic Peptides and Proteins (ChemBioChem 10/2021). ChemBioChem, 22 (10), 1686-1686. doi: 10.1002/cbic.202100189
Late‐stage hydrocarbon conjugation and cyclisation in synthetic peptides and proteins
Araujo, Aline D., Nguyen, Huy T. and Fairlie, David P. (2021). Late‐stage hydrocarbon conjugation and cyclisation in synthetic peptides and proteins. ChemBioChem, 22 (10), 1784-1789. doi: 10.1002/cbic.202000796
Morais, Christudas, Rajandram, Retnagowri, Blakeney, Jade S., Iyer, Abishek, Suen, Jacky Y., Johnson, David W., Gobe, Glenda C., Fairlie, David P. and Vesey, David A. (2021). Expression of protease activated receptor-2 is reduced in renal cell carcinoma biopsies and cell lines. PLoS One, 16 (3) e0248983, e0248983. doi: 10.1371/journal.pone.0248983
Identification and phenotype of MAIT cells in cattle and their response to bacterial infections
Edmans, Matthew D., Connelley, Timothy K., Jayaraman, Siddharth, Vrettou, Christina, Vordermeier, Martin, Mak, Jeffrey Y. W., Liu, Ligong, Fairlie, David P., Maze, Emmanuel Atangana, Chrun, Tiphany, Klenerman, Paul, Eckle, Sidonia B. G., Tchilian, Elma and Benedictus, Lindert (2021). Identification and phenotype of MAIT cells in cattle and their response to bacterial infections. Frontiers in Immunology, 12 627173, 627173. doi: 10.3389/fimmu.2021.627173
Iyer, Abishek, Humphries, Tyrone L. R., Owens, Evan P., Zhao, Kong-Nan, Masci, Paul P., Johnson, David W., Nikolic-Paterson, David, Gobe, Glenda C., Fairlie, David P. and Vesey, David A. (2021). PAR2 activation on human kidney tubular epithelial cells induces tissue factor synthesis, that enhances blood clotting. Frontiers in Physiology, 12 615428, 615428. doi: 10.3389/fphys.2021.615428
Connecting hydrophobic surfaces in cyclic peptides increases membrane permeability
Hoang, Huy N., Hill, Timothy A. and Fairlie, David P. (2021). Connecting hydrophobic surfaces in cyclic peptides increases membrane permeability. Angewandte Chemie International Edition, 60 (15), 8385-8390. doi: 10.1002/anie.202012643
Howson, Lauren J., Li, Jasmine, von Borstel, Anouk, Barugahare, Adele, Mak, Jeffrey Y. W., Fairlie, David P., McCluskey, James, Turner, Stephen J., Davey, Martin S. and Rossjohn, Jamie (2021). Mucosal-associated invariant t cell effector function is an intrinsic cell property that can be augmented by the metabolic cofactor α-ketoglutarate. The Journal of Immunology, 206 (7) ji2001048, 1425-1435. doi: 10.4049/jimmunol.2001048
HDAC7 inhibition by phenacetyl and phenylbenzoyl hydroxamates
Mak, Jeffrey Y. W., Wu, Kai-Chen, Gupta, Praveer K., Barbero, Sheila, McLaughlin, Maddison G., Lucke, Andrew J., Tng, Jiahui, Lim, Junxian, Loh, Zhixuan, Sweet, Matthew J, Reid, Robert C., Liu, Ligong and Fairlie, David P. (2021). HDAC7 inhibition by phenacetyl and phenylbenzoyl hydroxamates. Journal of Medicinal Chemistry, 64 (4), 2186-2204. doi: 10.1021/acs.jmedchem.0c01967
Maruyama-Fumoto, Kana, McGuire, John J., Fairlie, David P., Shinozuka, Kazumasa and Kagota, Satomi (2021). Activation of protease-activated receptor 2 is associated with blood pressure regulation and proteinuria reduction in metabolic syndrome. Clinical and Experimental Pharmacology and Physiology, 48 (2), 211-220. doi: 10.1111/1440-1681.13431
Duszyc, Kinga, Gomez, Guillermo A., Lagendijk, Anne K., Yau, Mei-Kwan, Nanavati, Bageshri Naimish, Gliddon, Briony L., Hall, Thomas E., Verma, Suzie, Hogan, Benjamin M., Pitson, Stuart M., Fairlie, David P., Parton, Robert G. and Yap, Alpha S. (2021). Mechanotransduction activates RhoA in the neighbors of apoptotic epithelial cells to engage apical extrusion. Current Biology, 31 (6), 1326-1336.e5. doi: 10.1016/j.cub.2021.01.003
PAR2 induces ovarian cancer cell motility by merging three signalling pathways to transactivate EGFR
Jiang, Yuhong, Lim, Junxian, Wu, Kai‐Chen, Xu, Weijun, Suen, Jacky Y. and Fairlie, David P. (2021). PAR2 induces ovarian cancer cell motility by merging three signalling pathways to transactivate EGFR. British Journal of Pharmacology, 178 (4) bph.15332, 913-932. doi: 10.1111/bph.15332
Taking the Myc out of cancer: toward therapeutic strategies to directly inhibit c-Myc
Madden, Sarah K., de Araujo, Aline Dantas, Gerhardt, Mara, Fairlie, David P. and Mason, Jody M. (2021). Taking the Myc out of cancer: toward therapeutic strategies to directly inhibit c-Myc. Molecular Cancer, 20 (1) 3, 3. doi: 10.1186/s12943-020-01291-6
Sheng, Yong Hua, Giri, Rabina, Davies, Julie, Schreiber, Veronika, Alabbas, Saleh, Movva, Ramya, He, Yaowu, Wu, Andy, Hooper, John, McWhinney, Brett, Oancea, Iulia, Kijanka, Gregor, Hasnain, Sumaira, Lucke, Andrew J., Fairlie, David P., McGuckin, Michael A., Florin, Timothy H. and Begun, Jakob (2021). A nucleotide analog prevents colitis associated cancer via Β-catenin independently of inflammation and autophagy. Cellular and Molecular Gastroenterology and Hepatology, 11 (1), 33-53. doi: 10.1016/j.jcmgh.2020.05.012
Fortified coiled coils: enhancing eechanical stability with lactam or metal staples
López-García, Patricia, de Araujo, Aline D., Bergues-Pupo, Ana E., Tunn, Isabell, Fairlie, David P. and Blank, Kerstin G. (2021). Fortified coiled coils: enhancing eechanical stability with lactam or metal staples. Angewandte Chemie - International Edition, 60 (1) anie.202006971, 232-236. doi: 10.1002/anie.202006971
Leeansyah, Edwin, Hey, Ying Ying, Sia, Wan Rong, Ng, Justin Han Jia, Gulam, Muhammad Yaaseen, Boulouis, Caroline, Zhu, Feng, Ahn, Matae, Mak, Jeffrey Y.W., Fairlie, David P., Kwa, Andrea Lay Hoon, Sandberg, Johan K. and Wang, Lin-Fa (2020). MR1-restricted T cells with MAIT-like characteristics are functionally conserved in the Pteropid Bat Pteropus alecto. iScience, 23 (12) 101876, 101876. doi: 10.1016/j.isci.2020.101876
Kennedy, Amanda J., Sundström, Linda, Geschwindner, Stefan, Poon, Eunice K. Y., Jiang, Yuhong, Chen, Rongfeng, Cooke, Rob, Johnstone, Shawn, Madin, Andrew, Lim, Junxian, Liu, Qingqi, Lohman, Rink-Jan, Nordqvist, Anneli, Fridén-Saxin, Maria, Yang, Wenzhen, Brown, Dean G., Fairlie, David P. and Dekker, Niek (2020). Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition. Communications Biology, 3 (1) 782, 782. doi: 10.1038/s42003-020-01504-0
Yu, Huifeng, Yang, Amy, Derrick, Steven, Mak, Jeffrey Y. W., Liu, Ligong, Fairlie, David P. and Cowley, Siobhan (2020). Artificially induced MAIT cells inhibit M. bovis BCG but not M. tuberculosis during in vivo pulmonary infection. Scientific Reports, 10 (1) 13579, 13579. doi: 10.1038/s41598-020-70615-9
Mechanische Verstärkung von Coiled Coils mit Lactam und Histidin‐Metall‐Klammern
López‐García, Patricia, Araujo, Aline D., Bergues‐Pupo, Ana E., Tunn, Isabell, Fairlie, David P. and Blank, Kerstin G. (2020). Mechanische Verstärkung von Coiled Coils mit Lactam und Histidin‐Metall‐Klammern. Angewandte Chemie, 133 (1), 234-239. doi: 10.1002/ange.202006971
Atypical TRAV1-2-T cell receptor recognition of the antigen-presenting molecule MR1
Awad, Wael, Meermeier, Erin W., Sandoval-Romero, Maria L., Le Nours, Jérôme, Worley, Aneta H., Null, Megan D., Liu, Ligong, McCluskey, James, Fairlie, David P., Lewinsohn, David M. and Rossjohn, Jamie (2020). Atypical TRAV1-2-T cell receptor recognition of the antigen-presenting molecule MR1. Journal of Biological Chemistry, 295 (42), 14445-14457. doi: 10.1074/jbc.RA120.015292
McWilliam, Hamish E. G., Mak, Jeffrey Y. W., Awad, Wael, Zorkau, Matthew, Cruz-Gomez, Sebastian, Lim, Hui Jing, Yan, Yuting, Wormald, Sam, Dagley, Laura F., Eckle, Sidonia B. G., Corbett, Alexandra J., Liu, Haiyin, Li, Shihan, Reddiex, Scott J. J., Mintern, Justine D., Liu, Ligong, McCluskey, James, Rossjohn, Jamie, Fairlie, David P. and Villadangos, Jose A. (2020). Endoplasmic reticulum chaperones stabilize ligand-receptive MR1 molecules for efficient presentation of metabolite antigens. Proceedings of the National Academy of Sciences, 117 (40), 1-12. doi: 10.1073/pnas.2011260117
Yu, Huifeng, Yang, Amy, Liu, Ligong, Mak, Jeffrey Y. W., Fairlie, David P. and Cowley, Siobhan (2020). CXCL16 stimulates antigen-induced MAIT cell accumulation but trafficking during lung infection is CXCR6-independent. Frontiers in Immunology, 11 1773, 1773. doi: 10.3389/fimmu.2020.01773
Kapetanovic, Ronan, Afroz, Syeda Farhana, Ramnath, Divya, Lawrence, Grace M.E.P., Okada, Takashi, Curson, James E.B., Bruin, Jost, Fairlie, David P., Schroder, Kate, St John, Justin C., Blumenthal, Antje and Sweet, Matthew J. (2020). Lipopolysaccharide promotes Drp1‐dependent mitochondrial fission and associated inflammatory responses in macrophages. Immunology and Cell Biology, 98 (7) imcb.12363, 528-539. doi: 10.1111/imcb.12363
Absence of mucosal-associated invariant T cells in a person with a homozygous point mutation in MR1
Howson, Lauren J., Awad, Wael, von Borstel, Anouk, Lim, Hui Jing, McWilliam, Hamish E. G., Sandoval-Romero, Maria L., Majumdar, Shamik, Hamzeh, Abdul Rezzak, Andrews, Thomas D., McDermott, David H., Murphy, Philip M., Le Nours, Jérôme, Mak, Jeffrey Y. W., Liu, Ligong, Fairlie, David P., McCluskey, James, Villadangos, Jose A., Cook, Matthew C., Turner, Stephen J., Davey, Martin S., Ojaimi, Samar and Rossjohn, Jamie (2020). Absence of mucosal-associated invariant T cells in a person with a homozygous point mutation in MR1. Science Immunology, 5 (49) 9492, eabc9492. doi: 10.1126/sciimmunol.abc9492
Boulouis, Caroline, Sia, Wan Rong, Gulam, Muhammad Yaaseen, Teo, Jocelyn Qi Min, Png, Yi Tian, Phan, Thanh Kha, Mak, Jeffrey Y. W., Fairlie, David P., Poon, Ivan K. H., Koh, Tse Hsien, Bergman, Peter, Lim, Chwee Ming, Wang, Lin-Fa, Kwa, Andrea Lay Hoon, Sandberg, Johan K. and Leeansyah, Edwin (2020). Human MAIT cell cytolytic effector proteins synergize to overcome carbapenem resistance in Escherichia coli. PLoS Biology, 18 (6) e3000644, e3000644. doi: 10.1371/journal.pbio.3000644
Systemic delivery of peptides by the oral route: formulation and medicinal chemistry approaches
Brayden, D. J., Hill, T. A., Fairlie, D. P., Maher, S. and Mrsny, R. J. (2020). Systemic delivery of peptides by the oral route: formulation and medicinal chemistry approaches. Advanced Drug Delivery Reviews, 157, 2-36. doi: 10.1016/j.addr.2020.05.007
Tng, Jiahui, Lim, Junxian, Wu, Kai-Chen, Lucke, Andrew J., Xu, Weijun, Reid, Robert C. and Fairlie, David P. (2020). Achiral derivatives of hydroxamate AR-42 potently inhibit class I HDAC enzymes and cancer cell proliferation. Journal of Medicinal Chemistry, 63 (11) acs.jmedchem.0c00230, 5956-5971. doi: 10.1021/acs.jmedchem.0c00230
Koay, Hui Fern, Su, Shian, Amann-Zalcenstein, Daniela, Daley, Stephen R, Comerford, Iain, Whyte, Carly E, Konstantinov, Igor E, d’Udekem, Yves, Baldwin, Tracey, Hickey, Peter F, Berzins, Stuart P, Mak, Jeffrey Y.W., Kallies, Axel, Chen, Zhenjun, Nussing, Simone, Kedzierska, Katherine, Mackay, Laura K, McColl, Shaun R, Deenick, Elissa K, Fairlie, David P, McCluskey, James, Goodnow, Christopher C, Ritchie, Matthew E, Belz, Gabrielle T, Naik, Shalin H, Pellicci, Daniel G and Godfrey, Dale I (2020). A divergent transcriptional landscape underpins the development and functional branching of MAIT cells. The Journal of Immunology, 204 (1_Supplement), 223.8-223.8. doi: 10.4049/jimmunol.204.supp.223.8
Virus-mediated suppression of the antigen presentation molecule MR1
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The molecular basis underpinning the potency and specificity of MAIT cell antigens
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Alpha-synuclein structure and Parkinson's disease - Lessons and emerging principles
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Complement C3a and C5a receptors promote GVHD by suppressing mitophagy in recipient dendritic cells
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MAIT cells protect against pulmonary Legionella longbeachae infection
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An overview on the identification of MAIT cell antigens
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Bicyclic helical peptides as dual inhibitors selective for Bcl2A1 and Mcl-1 proteins
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Lysine deacetylases and regulated glycolysis in macrophages
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Chemically Diverse Helix-Constrained Peptides Using Selenocysteine Crosslinking
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Human blood MAIT cell subsets defined using MR1 tetramers
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Glucuronic acid as a helix-inducing linker in short peptides
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Chemical approaches to modulating complement-mediated diseases
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Protease activated receptor 2 controls myelin development, resiliency and repair
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Downsizing proto-oncogene cFos to short helix-constrained peptides that bind Jun
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Quinazolinone derivatives as inhibitors of homologous recombinase RAD51
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The ribosomal protein S19 suppresses antitumor immune responses via the complement C5a receptor 1
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Drugs and drug-like molecules can modulate the function of mucosal-associated invariant T cells
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Alpha helix nucleation by a simple cyclic tetrapeptide
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Histone deacetylases (HDAC) in physiological and pathological bone remodelling
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Product release is rate-limiting for catalytic processing by the Dengue virus protease
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Downsizing the BAD BH3 peptide to small contrained alpha-helices with improved ligand efficiency
Shepherd, Nicholas E., Harrison, Rosemary S., Ruiz-Gomez, Gloria, Abbenante, Giovanni, Mason, Jody M. and Fairlie, David P. (2016). Downsizing the BAD BH3 peptide to small contrained alpha-helices with improved ligand efficiency. Organic and Biomolecular Chemistry, 46 (14), 10939-10945. doi: 10.1039/C6OB02185A
A three-stage intrathymic development pathway for the mucosal-associated invariant T cell lineage
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Review stapling peptides using cysteine crosslinking
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Helix nucleation by the smallest known α-helix in water
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Protease activated receptor 2 (PAR2) modulators: a patent review (2010–2015)
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Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity
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Differential anti-inflammatory activity of HDAC inhibitors in human macrophages and rat arthritis
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Philippe, Gregoire, Huang, Yen-Hua, Cheneval, Olivier, Lawrence, Nicole, Zhang, Zhen, Fairlie, David P., Craik, David J., Dantas De Araujo, Aline and Troeira Henriques, Sonia (2016). Development of cell-penetrating peptide-based drug leads to inhibit MDMX:p53 and MDM2:p53 interactions. Biopolymers - Peptide Science, 106 (6), 853-863. doi: 10.1002/bip.22893
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Potent small agonists of protease activated receptor 2
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Recognition of Vitamin B precursors and byproducts by Mucosal Associated Invariant T cells
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Histone deacetylase enzymes as drug targets for the control of the sheep blowfly, Lucilia cuprina
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Singh, Ranee, Reed, Anthony N., Chu, Peifei, Scully, Conor C. G., Yau, Mei-Kwan, Suen, Jacky Y., Durek, Thomas, Reid, Robert C. and Fairlie, David P. (2015). Potent complement C3a receptor agonists derived from oxazole amino acids: structure-activity relationships. Bioorganic and Medicinal Chemistry Letters, 25 (23), 5604-5608. doi: 10.1016/j.bmcl.2015.10.038
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Membrane-anchored serine protease matriptase is a trigger of pulmonary fibrogenesis
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Flexibility versus rigidity for orally bioavailable cyclic hexapeptides
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Repurposing Registered Drugs as Antagonists for Protease-Activated Receptor 2
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Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists
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Nutrient and immune sensing are obligate pathways in metabolism, immunity and disease
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Three homology models for PAR2 derived from different templates: Application to antagonist discovery
Perry, Samuel R., Xu, Weijun, Wirija, Anna, Lim, Junxian, Yau, Mei-Kwan, Stoermer, Martin J., Lucke, Andrew J. and Fairlie, David P. (2015). Three homology models for PAR2 derived from different templates: Application to antagonist discovery. Journal of Chemical Information And Modeling, 55 (6), 1181-1191. doi: 10.1021/acs.jcim.5b00087
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Inhibiting histone deacetylase 1 suppresses both inflammation and bone loss in arthritis
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Facile synthesis of mono- and bis-methylated Fmoc-Dap, -Dab and -Orn amino acids
Lindahl, Fredrik, Hoang, Huy N., Fairlie, David P. and Cooper, Matthew A. (2015). Facile synthesis of mono- and bis-methylated Fmoc-Dap, -Dab and -Orn amino acids. Chemical Communications, 51 (21), 4496-4498. doi: 10.1039/c4cc09780g
Small molecule inhibitors of disulfide bond formation by the bacterial DsbA-DsbB dual enzyme system
Halili, Maria A., Bachu, Prabhakar, Lindahl, Fredrik, Bechara, Cherine, Mohanty, Biswaranjan, Reid, Robert C., Scanlon, Martin, Robinson, Carol V., Fairlie, David P. and Martin, Jennifer L. (2015). Small molecule inhibitors of disulfide bond formation by the bacterial DsbA-DsbB dual enzyme system. ACS Chemical Biology, 10 (4), 957-964. doi: 10.1021/cb500988r
Toward peptide-based inhibitors as therapies for Parkinson's disease
Mason, Jody M. and Fairlie, David P. (2015). Toward peptide-based inhibitors as therapies for Parkinson's disease. Future Medicinal Chemistry, 7 (16), 2103-2105. doi: 10.4155/fmc.15.139
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Improving on nature: making a cyclic heptapeptide orally bioavailable
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Potent heterocyclic ligands for human complement C3a receptor
Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Hamidon, Johan K., Lim, Junxian, Stoermer, Martin J. and Fairlie, David P. (2014). Potent heterocyclic ligands for human complement C3a receptor. Journal of Medicinal Chemistry, 57 (20), 8459-8470. doi: 10.1021/jm500956p
Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding
Harrison, Rosemary S., Shepherd, Nicholas E., Hoang, Huy N., Beyer, Renee L., Ruiz-Gomez, Gloria, Kelso, Michael J., Mei Kok, W., Hill, Timothy A., Abbenante, Giovanni and Fairlie, David P. (2014). Helical cyclic pentapeptides constrain HIV-1 Rev peptide for enhanced RNA binding. Tetrahedron, 70 (42), 7645-7650. doi: 10.1016/j.tet.2014.07.096
Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbed
Hill, Timothy A., Lohman, Rink-Jan, Hoang, Huy N., Nielsen, Daniel S., Scully, Conor C. G., Kok, W. Mei, Liu, Ligong, Lucke, Andrew J., Stoermer, Martin J., Schroeder, Christina I., Chaousis, Stephanie, Colless, Barbara, Bernhardt, Paul V., Edmonds, David J., Griffith, David A., Rotter, Charles J., Ruggeri, Roger B., Price, David A., Liras, Spiros, Craik, David J. and Fairlie, David P. (2014). Cyclic penta- and hexaleucine peptides without N-methylation are orally absorbed. ACS Medicinal Chemistry Letters, 5 (10), 1148-1151. doi: 10.1021/ml5002823
Constraining cyclic peptides to mimic protein structure motifs
Hill, Timothy A., Shepherd, Nicholas E., Diness, Frederik and Fairlie, David P. (2014). Constraining cyclic peptides to mimic protein structure motifs. Angewandte Chemie (International Edition), 53 (48), 13020-13041. doi: 10.1002/anie.201401058
Fixierung cyclischer Peptide: Mimetika von Proteinstrukturmotiven
Hill, Timothy A., Shepherd, Nicholas E., Diness, Frederik and Fairlie, David P. (2014). Fixierung cyclischer Peptide: Mimetika von Proteinstrukturmotiven. Angewandte Chemie, 126 (48), 13234-13257. doi: 10.1002/ange.201401058
Pathway-selective antagonism of proteinase activated receptor 2
Suen, J. Y., Cotterell, A., Lohman, R. J., Lim, J., Han, A., Yau, M. K., Liu, L., Cooper, M. A., Vesey, D. A. and Fairlie, D. P. (2014). Pathway-selective antagonism of proteinase activated receptor 2. British Journal of Pharmacology, 171 (17), 4112-4124. doi: 10.1111/bph.12757
Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Lim, Junxian and Fairlie, David P. (2014). Stereoelectronic effects dictate molecular conformation and biological function of heterocyclic amides. Journal of the American Chemical Society, 136 (34), 11914-11917. doi: 10.1021/ja506518t
Eckle, Sidonia B.G., Birkinshaw, Richard W., Kostenko, Lyudmila, Corbett, Alexandra J., McWilliam, Hamish E. G., Reantragoon, Rangsima, Chen, Zhenjun, Gherardin, Nicholas A., Beddoe, Travis, Liu, Ligong, Patel, Onisha, Meehan, Bronwyn, Fairlie, David P., Villadangos, Jose A., Godfrey, Dale I., Kjer-Nielsen, Lars, McCluskey, James and Rossjohn, Jamie (2014). A molecular basis underpinning the T cell receptor heterogeneity of mucosal-associated invariant T cells. Journal of Experimental Medicine, 211 (8), 1585-1600. doi: 10.1084/jem.20140484
Vadrevu, Saurya Kumari, Chintala, Navin K., Sharma, Sharad K., Sharma, Priya, Cleveland, Clayton, Riediger, Linley, Manne, Sasikanth, Fairlie, David P., Gorczyca, Wojciech, Almanza, Othon, Karbowniczek, Magdalena and Markiewski, Maciej M. (2014). Complement c5a receptor facilitates cancer metastasis by altering t-cell responses in the metastatic niche. Cancer Research, 74 (13), 3454-3465. doi: 10.1158/0008-5472.CAN-14-0157
Kurth, Fabian, Duprez, Wilko, Premkumar, Lakshmanane, Schembri, Mark A., Fairlie, David P. and Martin, Jennifer L. (2014). Crystal Structure of the Dithiol Oxidase DsbA Enzyme from Proteus Mirabilis Bound Non-covalently to an Active Site Peptide Ligand.. Journal of Biological Chemistry, 289 (28), 19810-19822. doi: 10.1074/jbc.M114.552380
Comparative α-Helicity of Cyclic Pentapeptides in Water
de Araujo, Aline D., Hoang, Huy N., Kok, W. Mei, Diness, Frederik, Gupta, Praveer, Hill, Timothy A., Driver, Russell W., Price, David A., Liras, Spiros and Fairlie, David P. (2014). Comparative α-Helicity of Cyclic Pentapeptides in Water. Angewandte Chemie International Edition, 53 (27), 6965-6969. doi: 10.1002/anie.201310245/abstract
T-cell activation by transitory neo-antigens derived from distinct microbial pathways
Corbett, Alexandra J., Eckle, Sidonia B. G., Birkinshaw, Richard W., Liu, Ligong, Patel, Onisha, Mahony, Jennifer, Chen, Zhenjun, Reantragoon, Rangsima, Meehan, Bronwyn, Cao, Hanwei, Williamson, Nicholas A., Strugnell, Richard A., Van Sinderen, Douwe, Mak, Jeffrey Y. W., Fairlie, David P., Kjer-Nielsen, Lars, Rossjohn, Jamie and McClusky, James (2014). T-cell activation by transitory neo-antigens derived from distinct microbial pathways. Nature, 509 (7500), 361-365. doi: 10.1038/nature13160
C5aR and C5L2 act in concert to balance immunometabolism in adipose tissue
Poursharifi, Pegah, Lapointe, Marc, Fisette, Alexandre, Lu, Huiling, Roy, Christian, Munkonda, Mercedes Nancy, Fairlie, David P. and Cianflone, Katherine (2014). C5aR and C5L2 act in concert to balance immunometabolism in adipose tissue. Molecular and Cellular Endocrinology, 382 (1), 325-333. doi: 10.1016/j.mce.2013.10.019
Biased signalling and proteinase-activated receptors (PARs): Targeting inflammatory disease
Hollenberg, M. D., Mihara, K., Polley, D., Suen, J. Y., Han, A., Fairlie, D. P. and Ramachandran, R. (2014). Biased signalling and proteinase-activated receptors (PARs): Targeting inflammatory disease. British Journal of Pharmacology, 171 (5), 1180-1194. doi: 10.1111/bph.12544
Lysine acetylation in sexual stage malaria parasites is a target for antimalarial small molecules
Trenholme, Katharine, Marek, Linda, Duffy, Sandra, Pradel, Gabriele, Fisher, Gillian, Hansen, Finn K., Skinner-Adams, Tina S., Butterworth, Alice, Ngwa, Che Julius, Moecking, Jonas, Goodman, Christopher D., McFadden, Geoffrey I., Sumanadasa, Subathdrage D. M., Fairlie, David P., Avery, Vicky M., Kurz, Thomas and Andrews, Katherine T. (2014). Lysine acetylation in sexual stage malaria parasites is a target for antimalarial small molecules. Antimicrobial Agents and Chemotherapy, 58 (7), 3666-3678. doi: 10.1128/AAC.02721-13
Walden, Patricia, Halili, Maria, Julia Archbold, Fredrik Lindahl, Fairlie, David P., Inaba, Kenji and Martin, Jennifer L. (2013). The alpha-proteobacteria Wolbachia pipientis protein disulfide machinery has a regulatory mechanism absent in gamma-proteobacteria. PloS One, 8 (11) e81440, e81440.1-e81440.9. doi: 10.1371/journal.pone.0081440
Downsizing a human inflammatory protein to a small molecule with equal potency and functionality
Reid, Robert C., Yau, Mei-Kwan, Singh, Ranee, Hamidon, Johan K., Reed, Anthony N., Chu, Peifei, Suen, Jacky Y., Stoermer, Martin J., Blakeney, Jade S., Lim, Junxian, Faber, Jonathan M. and David P. Fairlie, (2013). Downsizing a human inflammatory protein to a small molecule with equal potency and functionality. Nature Communications, 4 (2802) 2802, 1-9. doi: 10.1038/ncomms3802
Kurth, Fabian, Rimmer, Kieran, Premkumar, Lakshmanane, Mohanty, Biswaranjan, Duprez, Wilko, Halili, Maria A., Shouldice, Stephen R., Heras, Begoña, Fairlie, David P., Scanlon, Martin J. and Martin, Jennifer L. (2013). Comparative sequence, structure and redox analyses of Klebsiella pneumoniae DsbA show that anti-virulence target DsbA enzymes fall into distinct classes. PloS One, 8 (11) e80210, e80210.1-e80210.15. doi: 10.1371/journal.pone.0080210
Hohenhaus, Daniel M., Schaale, Kolja, Le Cao, Kim-Anh, Seow, Vernon, Iyer, Abishek, Fairlie, David P. and Sweet, Matthew J. (2013). An mRNA atlas of G protein-coupled receptor expression during primary human monocyte/macrophage differentiation and lipopolysaccharide-mediated activation identifies targetable candidate regulators of inflammation. Immunobiology, 218 (11), 1345-1353. doi: 10.1016/j.imbio.2013.07.001
Toward drugs for protease-activated receptor 2 (PAR2)
Yau, Mei-Kwan, Liu, L.igong and Fairlie, David P. (2013). Toward drugs for protease-activated receptor 2 (PAR2). Journal of Medicinal Chemistry, 56 (19), 7477-7497. doi: 10.1021/jm400638v
Reantragoon, Rangsima, Corbett, Alexandra J., Sakala, Isaac G., Gherardin, Nicholas A., Furness, John B., Chen, Zhenjun, Eckle, Sidonia B. G., Uldrich, Adam P., Birkinshaw, Richard W., Patel, Onisha, Kostenko, Lyudmila, Meehan, Bronwyn, Kedzierska, Katherine, Liu, Ligong, Fairlie, David P., Hansen, Ted H., Godfrey, Dale I., Rossjohn, Jamie, McCluskey, James and Kjer-Nielsen, Lars (2013). Antigen-loaded MR1 tetramers define T cell receptor heterogeneity in mucosal-associated invariant T cells. Journal of Experimental Medicine, 210 (11), 2305-2320. doi: 10.1084/jem.20130958
Seow, Vernon, Lim, Junxian, Iyer, Abishek, Suen, Jacky Y., Ariffin, Juliana K., Hohenhaus, Daniel M., Sweet, Matthew J. and Fairlie, David P. (2013). Inflammatory Responses Induced by Lipopolysaccharide Are Amplified in Primary Human Monocytes but Suppressed in Macrophages by Complement Protein C5a. Journal of Immunology, 191 (8), 4308-4316. doi: 10.4049/jimmunol.1301355
Premkumar, Lakshmanane, Heras, Begoña, Duprez, Wilko, Walden, Patricia, Halili, Maria, Kurth, Fabian, Fairlie, David P. and Martin, Jennifer L. (2013). Rv2969c, essential for optimal growth in Mycobacterium tuberculosis, is a DsbA-like enzyme that interacts with VKOR-derived peptides and has atypical features of DsbA-like disulfide oxidases. Acta Crystallographica Section D: Biological Crystallography, 69 (10), 1981-1994. doi: 10.1107/S0907444913017800
Croker, Daniel E., Halai, Reena, Fairlie, David P. and Cooper, Matthew A. (2013). C5a, but not C5a-des Arg, induces upregulation of heteromer formation between complement C5a receptors C5aR and C5L2. Immunology and Cell Biology, 91 (10), 625-633. doi: 10.1038/icb.2013.48
Tan, Cindy S. E., Hobson-Peters, Jody M., Stoermer, Martin J., Fairlie, David P., Khromykh, Alexander A. and Hall, Roy A. (2013). An interaction between the methyltransferase and RNA dependent RNA polymerase domains of the West Nile virus NS5 protein. Journal of General Virology, 94 (Pt. 9), 1961-1971. doi: 10.1099/vir.0.054395-0
Lim, Junxian, Iyer, Abishek, Liu, Ligong, Suen, Jacky Y., Lohman, Rink-Jan, Seow, Vernon, Yau, Mei-Kwan, Brown, Lindsay and Fairlie, David P. (2013). Diet-induced obesity, adipose inflammation, and metabolic dysfunction correlating with PAR2 expression are attenuated by PAR2 antagonism. The FASEB Journal, 27 (12), 4757-4767. doi: 10.1096/fj.13-232702
Recognition of vitamin B metabolites by mucosal-associated invariant T cells
Patel, Onisha, Kjer-Nielsen, Lars, Le Nours, Jerome, Eckle, Sidonia B. G., Birkinshaw, Richard, Beddoe, Travis, Corbett, Alexandra J., Liu, Ligong, Miles, John J., Meehan, Bronwyn, Reantragoon, Rangsima, Sandoval-Romero, Maria L., Sullivan, Lucy C., Brooks, Andrew G., Chen, Zhenjun, Fairlie, David P., McCluskey, James and Rossjohn, Jamie (2013). Recognition of vitamin B metabolites by mucosal-associated invariant T cells. Nature Communications, 4 (1) 2142, 2142.1-2142.8. doi: 10.1038/ncomms3142
Shakespear, Melanie R., Hohenhaus, Daniel M., Kelly, Greg M., Kamal, Nabilah A., Gupta, Praveer, Labzin, Larisa I., Schroder, Kate, Garceau, Valerie, Barbero, Sheila, Iyer, Abishek, Hume, David A., Reid, Robert C., Irvine, Katharine M., Fairlie, David P. and Sweet, Matthew J. (2013). Histone deacetylase 7 promotes Toll-like Receptor 4-dependent pro-inflammatory gene expression in macrophages. Journal of Biological Chemistry, 288 (35), 25362-25374. doi: 10.1074/jbc.M113.496281
Identification and characterization of bi-thiazole-2,2'-diamines as kinase inhibitory scaffolds
Ngoei, Kevin R. W., Ng, Dominic C. H., Gooley, Paul R., Fairlie, David P., Stoermer, Martin J. and Bogoyevitch, Marie A. (2013). Identification and characterization of bi-thiazole-2,2'-diamines as kinase inhibitory scaffolds. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, 1834 (6), 1077-1088. doi: 10.1016/j.bbapap.2013.02.001
PAR2-induced inflammatory responses in human kidney tubular epithelial cells
Vesey, David A., Suen, Jacky Y., Seow, Vernon, Lohman, Rink-Jan, Liu, Ligong, Gobe, Glenda C., Johnson, David W. and Fairlie, David P. (2013). PAR2-induced inflammatory responses in human kidney tubular epithelial cells. American Journal of Physiology - Renal Physiology, 304 (6), F737-F750. doi: 10.1152/ajprenal.00540.2012
Rao, Tara, Ruiz-Gomez, Gloria, Hill, Timothy A., Hoang, Huy N., Fairlie, David P. and Mason, Jody M. (2013). Truncated and Helix-Constrained Peptides with High Affinity and Specificity for the cFos Coiled-Coil of AP-1. PLoS One, 8 (3) e59415, e59415.1-e59415.12. doi: 10.1371/journal.pone.0059415
Liu, Junxian, Iyer, Abishek, Suen, Jacky Y., Seow, Vernon, Reid, Robert C., Brown, Lindsay and Fairlie, David P. (2013). C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling. The FASEB Journal, 27 (2), 822-831. doi: 10.1096/fj.12-220582
Efficient chemical synthesis of human complement protein C3a
Ghassemian, Artin, Wang, Ching-I Anderson, Yau, Mei-Kwan, Reid, Robert C., Lewis, Richard J., Fairlie, David P., Alewood, Paul F. and Durek, Thomas (2013). Efficient chemical synthesis of human complement protein C3a. Chemical Communications, 49 (23), 2356-2358. doi: 10.1039/c3cc40537k
The Future of Peptide-based Drugs
Craik, David J., Fairlie, David P., Liras, Spiros and Price, David (2013). The Future of Peptide-based Drugs. Chemical Biology and Drug Design, 81 (1), 136-147. doi: 10.1111/cbdd.12055
Total synthesis, structure, and oral absorption of a thiazole cyclic peptide, sanguinamide A
Nielsen, Daniel S., Hoang, Huy N., Lohman, Rink-Jan, Diness, Frederik and Fairlie, David P. (2013). Total synthesis, structure, and oral absorption of a thiazole cyclic peptide, sanguinamide A. Organic Letters, 14 (22), 5720-5723. doi: 10.1021/ol3027347
MR1 presents microbial vitamin B metabolites to MAIT cells
Kjer-Nielsen, Lars, Patel, Onisha, Corbett, Alexandra J., Le Nours, Jerome, Meehan, Bronwyn, Liu, Ligong, Bhati, Mugdha, Chen, Zhenjun, Kostenko, Lyudmila, Reantragoon, Rangsima, Williamson, Nicholas A., Purcell, Anthony W., Dudek, Nadine L., McConville, Malcolm J., O'Hair, Richard A. J., Khairallah, George N., Godfrey, Dale I., Fairlie, David P., Rossjohn, Jamie and McCluskey, James (2012). MR1 presents microbial vitamin B metabolites to MAIT cells. Nature, 491 (7426), 717-725. doi: 10.1038/nature11605
Targeting quorum sensing and competence stimulation for antimicrobial chemotherapy
Shepherd, Nicholas E., Harrison, Rosemary S. and Fairlie, David P. (2012). Targeting quorum sensing and competence stimulation for antimicrobial chemotherapy. Current Drug Targets, 13 (11), 1348-1359. doi: 10.2174/138945012803530233
Iyer, Abishek, Lim, Junxian, Poudyal, Hemant, Reid, Robert C., Suen, Jacky Y., Webster, Julie, Prins, Johannes B., Whitehead, Jonathan P., Fairlie, David P. and Brown, Lindsay (2012). An inhibitor of phospholipase A2 group IIA modulates adipocyte signaling and protects against diet-induced metabolic syndrome in rats. Diabetes, 61 (9), 2320-2329. doi: 10.2337/db11-1179
Catalyst-free N-arylation using unactivated fluorobenzenes
Diness, Frederik and Fairlie, David (2012). Catalyst-free N-arylation using unactivated fluorobenzenes. Angewandte Chemie International Edition, 51 (32), 8012-8016. doi: 10.1002/anie.201202149
Towards histone deacetylase inhibitors as new antimalarial drugs
Andrews, Katherine T., Tran, Tran N. and Fairlie, David P. (2012). Towards histone deacetylase inhibitors as new antimalarial drugs. Current Pharmaceutical Design, 18 (24), 3467-3479. doi: 10.2174/138161212801327257
Halai, Reena, Croker, Daniel E., Suen, Jacky Y., Fairlie, David P. and Cooper, Matthew A. (2012). A comparative study of impedance versus optical label-free systems relative to labelled assays in a predominantly Gi coupled GPCR (C5aR) signalling. Biosensors, 2 (3), 273-290. doi: 10.3390/bios2030273
Lohman, Rink-Jan, Cotterell, Adam J., Barry, Grant D., Liu, Ligong, Suen, Jacky Y., Vesey, David A. and Fairlie, David P. (2012). An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats. The FASEB Journal, 26 (7), 2877-2887. doi: 10.1096/fj.11-201004
Antimalarial activity of the anticancer histone deacetylase inhibitor SB939
Sumanadasa, Subathdrage D. M., Goodman, Christopher D., Lucke, Andrew J., Skinner-Adams, Tina, Sahama, Ishani, Haque, Ashraful, Do, Tram Anh, McFadden, Geoffrey I., Fairlie, David P. and Andrews, Katherine T. (2012). Antimalarial activity of the anticancer histone deacetylase inhibitor SB939. Antimicrobial Agents and Chemotherapy, 56 (7), 3849-3856. doi: 10.1128/AAC.00030-12
Fairlie, David (2012). Chemical biology down under. Current Topics in Medicinal Chemistry, 12 (14), 1469-1470. doi: 10.2174/156802612802652475
Towards isozyme-selective HDA inhibitors for interrogating disease
Gupta, Praveer, Reid, Robert C., Iyer, Abishek, Sweet, Matthew J. and Fairlie, David (2012). Towards isozyme-selective HDA inhibitors for interrogating disease. Current Topics in Medicinal Chemistry, 12 (14), 1479-1499. doi: 10.2174/156802612802652420
Folding pentapeptides into left and right handed alpha helices
Hoang, Huy N., Abbenante, Giovanni, Hill, Timothy A., Ruiz-Gomez, Gloria and Fairlie, David P. (2012). Folding pentapeptides into left and right handed alpha helices. Tetrahedron, 68 (23), 4513-4516. doi: 10.1016/j.tet.2011.10.108
Histone deacetylase inhibitors as suppressors of bone destruction in inflammatory diseases
Cantley, Melissa D., Bartold, Peter M., Fairlie, David P., Rainsford, K. D. and Haynes, David R. (2012). Histone deacetylase inhibitors as suppressors of bone destruction in inflammatory diseases. Journal of Pharmacy and Pharmacology, 64 (6), 763-774. doi: 10.1111/j.2042-7158.2011.01421.x
Matching cavities in G protein-coupled receptors to infer ligand-binding sites
Madala, Praveen K., Fairlie, David P. and Bodén, Mikael (2012). Matching cavities in G protein-coupled receptors to infer ligand-binding sites. Journal of Chemical Information and Modeling, 52 (5), 1401-1410. doi: 10.1021/ci2005498
Thundyil, John, Pavlovski, Dale, Hsieh, Yu-Hsuan, Gelderblom, Mathias, Magnus, Tim, Fairlie, David P. and Arumugam, Thiruma V. (2012). C5a receptor (CD88) and TLR2 inhibition improves hypothermia-induced neuroprotection in an in vitro ischemic model. NeuroMolecular Medicine, 14 (1), 30-39. doi: 10.1007/s12017-012-8167-0
Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110)
Suen, J. Y., Barry, G. D., Lohman, R. J., Halili, M. A., Cotterell, A. J., Le, G. T. and Fairlie, D. P. (2012). Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). British Journal of Pharmacology, 165 (5), 1413-1423. doi: 10.1111/j.1476-5381.2011.01610.x
Antagonism of protease-activated receptor 2 protects against experimental colitis.
Lohman, Rink-Jan, Cotterell, Adam J., Suen, Jacky, Liu, Ligong, Do, Anh T., Vesey, David A. and Fairlie, David P. (2012). Antagonism of protease-activated receptor 2 protects against experimental colitis.. Journal of Pharmacology and Experimental Therapeutics, 340 (2), 256-265. doi: 10.1124/jpet.111.187062
Andrews, Katherine T., Gupta, Archna P., Tran, Thanh N., Fairlie, David P., Gobert, Geoffrey N. and Bozdech, Zbynek (2012). Comparative gene expression profiling of P. falciparum malaria parasites exposed to three different histone deacetylase inhibitors. Plos One, 7 (2) e31847, e31847-1-e31847-9. doi: 10.1371/journal.pone.0031847
HDAC inhibitors: Modulating leukocyte differentiation, survival, proliferation and inflammation
Sweet, Matthew J., Shakespear, Melanie R., Kamal, Nabilah A. and Fairlie, David P. (2012). HDAC inhibitors: Modulating leukocyte differentiation, survival, proliferation and inflammation. Immunology and Cell Biology, 90 (1), 14-22. doi: 10.1038/icb.2011.88
HDACs and their inhibitors in immunology: teaching anticancer drugs new tricks
Fairlie, David P. and Sweet, Matthew J. (2012). HDACs and their inhibitors in immunology: teaching anticancer drugs new tricks. Immunology and Cell Biology, 90 (1), 3-5. doi: 10.1038/icb.2011.105
Lysine acetylation in obesity, diabetes and metabolic disease
Iyer, Abishek, Fairlie, David P. and Brown, Lindsay (2012). Lysine acetylation in obesity, diabetes and metabolic disease. Immunology and Cell Biology, 90 (1), 39-46. doi: 10.1038/icb.2011.99
Structures of peptide agonists for human protease activated receptor 2
Stoermer, Martin J., Flanagan, Bernadine, Beyer, Renée L., Madala, Praveen K. and Fairlie, David P. (2012). Structures of peptide agonists for human protease activated receptor 2. Bioorganic and Medicinal Chemistry Letters, 22 (2), 916-919. doi: 10.1016/j.bmcl.2011.12.029
Histone deacetylase inhibitors and periodontal bone loss
Cantley, M. D., Bartold, P. M., Marino, V., Fairlie, D. P., Le, G. T., Lucke, A. J. and Haynes, D. R. (2011). Histone deacetylase inhibitors and periodontal bone loss. Journal of Periodontal Research, 46 (6), 697-703. doi: 10.1111/j.1600-0765.2011.01392.x
Inhibitors of histone deacetylases in class I and class II suppress human osteoclasts in vitro
Cantley, M. D., Fairlie, D. P., Bartold, P. M., Rainsford, K. D., Le, G. T., Lucke, A. J., Holding, C. A. and Haynes, D. R. (2011). Inhibitors of histone deacetylases in class I and class II suppress human osteoclasts in vitro. Journal of Cellular Physiology, 226 (12), 3233-3241. doi: 10.1002/jcp.22684
Synthesis of the Thiazole-Thiazoline Fragment of Largazole Analogues
Diness, Frederik, Nielsen, Daniel S. and Fairlie, David P. (2011). Synthesis of the Thiazole-Thiazoline Fragment of Largazole Analogues. Journal of Organic Chemistry, 76 (23), 9845-9851. doi: 10.1021/jo201675r
Protein a-turns recreated in structurally stable small molecules
Hoang, Huy N., Driver, Russell W., Beyer, Renée L., Malde, Alpeshkumar K., Le, Giang T., Abbenante, Giovanni, Mark, Alan E. and Fairlie, David P. (2011). Protein a-turns recreated in structurally stable small molecules. Angewandte Chemie International Edition, 123 (47), 11303-11307. doi: 10.1002/ange.201105119
Iyer, Abishek, Woodruff, Trent M., Wu, Mike C. L., Stylianou, Con, Reid, Robert C., Fairlie, David P., Taylor, Stephen M. and Brown, Lindsay (2011). Inhibition of inflammation and fibrosis by a complement C5a receptor antagonist in DOCA-salt hypertensive rats. Journal of Cardiovascular Pharmacology, 58 (5), 479-486. doi: 10.1097/FJC.0b013e31822a7a09
Histone deacetylases as regulators of inflammation and immunity
Shakespear, Melanie R., Halili, Maria A., Irvine, Katharine M., Fairlie, David P. and Sweet, Matthew J. (2011). Histone deacetylases as regulators of inflammation and immunity. Trends in Immunology, 32 (7), 335-343. doi: 10.1016/j.it.2011.04.001
Structure, function and pathophysiology of protease activated receptors
Adams, Mark N., Ramachandran, Rithwik, Yau, Mei-Kwan, Suen, Jacky Y., Fairlie, David P., Hollenberg, Morley D. and Hooper, John D. (2011). Structure, function and pathophysiology of protease activated receptors. Pharmacology and Therapeutics, 120 (3), 248-282. doi: 10.1016/j.pharmthera.2011.01.003
Marfurt, Jutta, Chalfein, Ferryanto, Prayoga, Pak, Wabiser, Frans, Kenangalem, Enny, Piera, Kim A., Fairlie, David P., Tjitra, Emiliana, Anstey, Nicholas M., Andrews, Kathy T. and Price, Rick N. (2011). Ex Vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax. Antimicrobial agents and chemotherapy, 55 (3), 961-966. doi: 10.1128/AAC.01220-10
Amyloid formation from an α-helical peptide bundle is seeded by 310-helix aggregates
Singh, Yogendra, Sharpe, Philip C., Hoang, Huy N., Lucke, Andrew J., McDowall, Alasdair W., Bottomley, Stephen P. and Fairlie, David P. (2011). Amyloid formation from an α-helical peptide bundle is seeded by 310-helix aggregates. Chemistry: A European Journal, 17 (1), 151-160. doi: 10.1002/chem.201002500
Antimalarial histone deacetylase inhibitors containing cinnamate or NSAID components
Wheatley, Nicole C., Andrews, Katherine T., Tran, Truc L., Lucke, Andrew J., Reid, Robert C. and Fairlie, David P. (2010). Antimalarial histone deacetylase inhibitors containing cinnamate or NSAID components. Bioorganic & Medicinal Chemistry Letters, 20 (23), 7080-7084. doi: 10.1016/j.bmcl.2010.09.096
Inhibitors selective for HDAC6 in enzymes and cells
Gupta, Praveer K., Reid, Robert C., Liu, Ligong, Lucke, Andrew J., Broomfield, Steve A., Andrews, Melanie R., Sweet, Matthew J. and Fairlie, David P. (2010). Inhibitors selective for HDAC6 in enzymes and cells. Bioorganic & Medicinal Chemistry Letters, 20 (23), 7067-7070. doi: 10.1016/j.bmcl.2010.09.100
Harrison, Rosemary S., Ruiz-Gomez, Gloria, Hill, Timothy A., Chow, Shiao Y., Shepherd, Nicholas E., Lohman, Rink-Jan, Abbenante, Giovanni, Hoang, Huy N. and Fairlie, David P. (2010). Novel helix-constrained nociceptin derivatives are potent agonists and antagonists of ERK phosphorylation and thermal analgesia in mice. Journal of Medicinal Chemistry, 53 (23), 8400-8408. doi: 10.1021/jm101139f
Suen, JY, Gardiner, B, Grimmond, S and Fairlie, DP (2010). Profiling gene expression induced by protease-activated receptor 2 (PAR2) activation in human kidney cells. PLoS One, 5 (11) e13809, e13809-1-e13809-14. doi: 10.1371/journal.pone.0013809
Scully, Conor C. G., Blakeney, Jade S., Singh, Ranee, Hoang, Huy N., Abbenante, Giovanni, Reid, Robert C. and Fairlie, David P. (2010). Selective Hexapeptide Agonists and Antagonists for Human Complement C3a Receptor (Journal of Medicinal Chemistry (2010) 53 (4938). Journal of Medicinal Chemistry, 53 (22), 8208-8208. doi: 10.1021/jm1013314
Novel agonists and antagonists for human protease activated receptor 2
Barry, Grant D., Suen, Jacky Y., Le, Giang T., Cotterell, Adam, Reid, Robert C. and Fairlie, David P. (2010). Novel agonists and antagonists for human protease activated receptor 2. Journal of Medicinal Chemistry, 53 (20), 7428-7440. doi: 10.1021/jm100984y
Selective hexapeptide agonists and antagonists for human complement C3a receptor
Scully, Conor C. G., Blakeney, Jade S., Singh, Ranee, Hoang, Huy N., Abbenante, Giovanni, Reid, Robert C. and Fairlie, David P. (2010). Selective hexapeptide agonists and antagonists for human complement C3a receptor. Journal of Medicinal Chemistry, 53 (13), 4938-4948. doi: 10.1021/jm1003705
Update 1 of: Beta-strand mimetics
Loughlin, Wendy A., Tyndall, Joel D. A., Glenn, Matthew P., Hill, Timothy A. and Fairlie, David P. (2010). Update 1 of: Beta-strand mimetics. Chemical Reviews, 110 (6), 1-38. doi: 10.1021/cr900395y
Update 1 of: Proteases universally recognize beta strands in their active sites
Madala, Praveen K., Tyndall, Joel D. A., Nall, Tessa and Fairlie, David P. (2010). Update 1 of: Proteases universally recognize beta strands in their active sites. Chemical Reviews, 110 (4), 1-33. doi: 10.1021/cr900368a
Update 1 of: beta-strand mimetics
Loughlin, Wendy A., Tyndall, Joel D. A., Glenn, Matthew P., Hill, Timothy A. and Fairlie, David P. (2010). Update 1 of: beta-strand mimetics. Chemical Reviews, 110 (6), PR32-PR69. doi: 10.1021/cr040648k
Halili, Maria A., Andrews, Melanie R., Labzin, Larisa I., Schroder, Kate, Matthias, Gabriele, Cao, Chun, Lovelace, Erica, Reid, Robert C., Le, Giang T., Hume, David A., Irvine, Katharine M., Matthias, Patrick, Fairlie, David P. and Sweet, Matthew J. (2010). Differential effects of selective HDAC inhibitors on macrophage inflammatory responses to the Toll-like receptor 4 agonist LPS. Journal of Leukocyte Biology, 87 (6), 1103-1114. doi: 10.1189/jlb.0509363
Harrison, Rosemary S., Shepherd, Nicholas E., Hoang, Huy N., Ruiz-Goméz, Gloria, Hill, Timothy A., Driver, Russell W., Desai, Vishal S., Young, Paul R., Abbenante, Giovanni and Fairlie, David P. (2010). Downsizing human, bacterial, and viral proteins to short water-stable alpha helices that maintain biological potency. Proceedings of the National Academy of Sciences of the United States of America, 107 (26), 11686-11691. doi: 10.1073/pnas.1002498107
Ruiz-Gomez, Gloria, Tyndall, Joel D. A., Pfeiffer, Bernhard, Abbenante, Giovanni and Fairlie, David (2010). Update 1 of: Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure. Chemical Reviews, 110 (6), 1-41. doi: 10.1021/cr900344w
Antifibrotic activity of an inhibitor of histone deacetylases in DOCA-salt hypertensive rats
Iyer, Abishek, Fenning, Andrew, Lim, Junxian, Le, Giang T, Reid, Robert C, Halili, Maria A, Fairlie, David P and Brown, Lindsay (2010). Antifibrotic activity of an inhibitor of histone deacetylases in DOCA-salt hypertensive rats. British Journal of Pharmacology, 159 (7), 1408-1417. doi: 10.1111/j.1476-5381.2010.00637.x
Ruiz-Gomez, Gloria, Tyndall, Joel D. A., Pfeiffer, Bernhard, Abbenante, Giovanni and Fairlie, David P. (2010). Update 1 of: Over One Hundred Petide-Activated G Protein-Coupled Receptors Recognized Ligands with Turn Structure. Chemical Reviews, 110 (4), PR1-PR41.
Noncovalent tripeptidyl benzyl- And cyclohexyl-amine inhibitors of the cysteine protease caspase-1
Loser, Reik, Abbenante, Giovanni, Madala, Praveen K., Halili, Maria, Le, Giang T. and Fairlie, David P. (2010). Noncovalent tripeptidyl benzyl- And cyclohexyl-amine inhibitors of the cysteine protease caspase-1. Journal of Medicinal Chemistry, 53 (6), 2651-2655. doi: 10.1021/jm901790w
Inflammatory lipid mediators in adipocyte function and obesity
Iyer, Abishek, Fairlie, David P., Prins, Johannes B., Hammock, Bruce D. and Brown, Lindsay (2010). Inflammatory lipid mediators in adipocyte function and obesity. Nature Reviews Endocrinology, 6 (2), 71-82. doi: 10.1038/nrendo.2009.264
Kampmann, T., Yennamalli, R., Campbell, P., Stoermer, M. J., Fairlie, D. P., Kobe, B. and Young, P. R. (2009). In silico screening of small molecule libraries using the dengue virus envelope E protein has identified compounds with antiviral activity against multiple flaviviruses. Antiviral Research, 84 (3), 234-241. doi: 10.1016/j.antiviral.2009.09.007
Left- and right-handed alpha-helical turns in homo- and hetero-chiral helical scaffolds
Shepherd, N. E., Hoang, H. N., Abbenante, G and Fairlie, D. P. (2009). Left- and right-handed alpha-helical turns in homo- and hetero-chiral helical scaffolds. Journal of the American Chemical Society, 131 (43), 15877-15886. doi: 10.1021/ja9065283
Structure-activity relationships for substrate-based inhibitors of human complement factor B
Ruiz-Gomez, G, Lim, J, Halili, M. A., Le, G. T., Madala, P. K., Abbenante, G and Fairlie, D. P. (2009). Structure-activity relationships for substrate-based inhibitors of human complement factor B. JOURNAL OF MEDICINAL CHEMISTRY, 52 (19), 6042-6052. doi: 10.1021/jm900781m
Base-sensitivity of arginine alpha-ketoamide inhibitors of serine proteases
Stoermer, Martin J., Leung, Donmienne, Young, Paul R. and Fairlie, David P. (2009). Base-sensitivity of arginine alpha-ketoamide inhibitors of serine proteases. Australian Journal of Chemistry, 62 (9), 988-992. doi: 10.1071/CH09150
A cyclic beta-strand tripeptide with an alpha-helix like CD spectrum
Driver, Russell W., Hoang, Huy N., Abbenante, Giovanni and Fairlie, David P. (2009). A cyclic beta-strand tripeptide with an alpha-helix like CD spectrum. Organic Letters, 11 (14), 3092-3095. doi: 10.1021/ol901181b
Metal clips that induce unstructured pentapeptides to be alpha-Helical in water
Ma, Michelle T., Hoang, Huy N., Scully, Conor C. G., Appleton, Trevor G. and Fairlie, David P. (2009). Metal clips that induce unstructured pentapeptides to be alpha-Helical in water. Journal of the American Chemical Society, 131 (12), 4505-4512. doi: 10.1021/ja900047w
Cantley, M. D., Bartold, P. M., Marino, V, Reid, R. C., Fairlie, D. P., Wyszynski, R. N., Zilm, P. S. and Haynes, D. R. (2009). The use of live-animal micro-computed tomography to determine the effect of a novel phospholipase A(2) inhibitor on alveolar bone loss in an in vivo mouse model of periodontitis. Journal of Periodontal Research, 44 (3), 317-322. doi: 10.1111/j.1600-0765.2008.01132.x
Structure of West Nile virus NS3 protease: Ligand stabilization of the catalytic conformation
Robin, Gautier, Chappell, Keith, Stoermer, Martin J., Hu, Shu-Hong, Young, Paul R., Fairlie, David P. and Martin, Jennifer L. (2009). Structure of West Nile virus NS3 protease: Ligand stabilization of the catalytic conformation. Journal of Molecular Biology, 385 (5), 1568-1577. doi: 10.1016/j.jmb.2008.11.026
Histone deacetylase inhibitors in inflammatory disease
Halili, M. A., Andrews, M, Sweet, M. and Fairlie, D. P. (2009). Histone deacetylase inhibitors in inflammatory disease. Current Topics in Medicinal Chemistry, 9 (3), 309-319. doi: 10.2174/156802609788085250
Targeting histone deacetylase inhibitors for anti-malarial therapy
Andrews, K. T, Tran, T. N., Wheatley, N. and Fairlie, David (2009). Targeting histone deacetylase inhibitors for anti-malarial therapy. Current Topics in Medicinal Chemistry, 9 (3), 292-308. doi: 10.2174/156802609788085313
Halili, Maria A., Ruiz-Gomez, Gloria, Le, Giang T., Abbenante, Giovanni and Fairlie, David P. (2009). Complement component C2, inhibiting a latent serine protease in the classical pathway of complement activation. Biochemistry, 48 (35), 8466-8472. doi: 10.1021/bi900679r
West Nile Virus NS2B/NS3 protease as an antiviral target
Chappell, K. J., Stoermer, M. J., Fairlie, D. P. and Young, P. R. (2008). West Nile Virus NS2B/NS3 protease as an antiviral target. Current Medicinal Chemistry, 15 (27), 2771-2784. doi: 10.2174/092986708786242804
Hoang, H.N., Bryant, G.K., Kelso, M.J., Beyer, R.L., Appleton, T.G. and Fairlie, D.P. (2008). Linkage isomerism in the binding of pentapeptide Ac-His(ALA)3His-NH2 to (Ethylenediamine)Palladium(II): Effect of the binding mode on peptide conformation. Inorganic Chemistry, 47 (20), 9439-9449. doi: 10.1021/ic800970p
Stoermer, Martin J., Chappell, Keith J., Liebscher, Susann, Jensen, Christina M., Gan, Chun H., Gupta, Praveer K., Xu, Wei-Jun, Young, Paul R. and Fairlie, David P. (2008). Potent cationic inhibitors of West Nile Virus NS2B/NS3 protease with serum stability, cell permeability and antiviral activity. Journal of Medicinal Chemistry, 51 (18), 5714-5721. doi: 10.1021/jm800503y
Cyclooligomerization of a helix-bearing template into macrocycles bearing multiple helices
Beyer, Rene´e L., Singh, Yogendra and Fairlie, David P. (2008). Cyclooligomerization of a helix-bearing template into macrocycles bearing multiple helices. Organic Letters, 10 (16), 3481-3484. doi: 10.1021/ol801040c
Chappell, Keith J., Stoermer, Martin J., Fairlie, David P. and Young, Paul R. (2008). Mutagenesis of the West Nile virus NS2B cofactor domain reveals two regions essential for protease activity. Journal of General Virology, 89 (4), 1010-1014. doi: 10.1099/vir.0.83447-0
Potent antimalarial activity of histone deacetylase inhibitor analogues
Andrews, K. T., Tran, T. N., Lucke, A. J., Kahnberg, P., Le, G. T., Boyle, G. M., Gardiner, D. L., Skinner-Adams, T. S. and Fairlie, D. P. (2008). Potent antimalarial activity of histone deacetylase inhibitor analogues. Antimicrobial agents and chemotherapy, 52 (4), 1454-1461. doi: 10.1128/AAC.00757-07
Marcon, L., Kozak, D., Battersby, B.J., Chappell, K., Fairlie, D., Young, P.R. and Trau, M. (2008). A dual-purpose synthetic colloidal platform for protease mapping: substrate profiling for Dengue and West Nile virus proteases. Analytical Biochemistry, 2008 (376), 151-153. doi: 10.1016/j.ab.2008.01.034
Tyndall, Joel D. A., Pattenden, Leonard K., Reid, Robert C., Hu, Shu-Hong, Alewood, Dianne, Alewood, Paul F., Walsh, Terry, Fairlie, David P. and Martin, Jennifer L. (2008). Crystal structures of highly constrained Substrate and Hydrolysis products bound to HIV-1 Protease. Implications for the Catalytic Mechanism. Biochemistry, 47 (12), 3736-3744. doi: 10.1021/bi7023157
Clean Or dirty - Just how selective do drugs need to be?
Abbenante, Giovanni, Reid, Robert C. and Fairlie, David P. (2008). Clean Or dirty - Just how selective do drugs need to be?. Australian Journal of Chemistry, 61 (9), 654-660. doi: 10.1071/CH08186
Hepta and octapeptide agonists of protease-activated receptor 2
Devlin, M. G., Pfeiffer, B., Flanagan, B. M., Beyer, R., Cocks, T. M and Fairlie, D. P. (2007). Hepta and octapeptide agonists of protease-activated receptor 2. Journal of Peptide Science, 13 (12), 856-861. doi: 10.1002/psc.912
A refined agonist pharmacophore for protease activated receptor 2
Barry, Grant D., Suen, Jacky Y., Low, Heng Boon, Pfeiffer, Bernhard, Flanagan, Bernadine, Halili, Maria, Le, Giang T. and Fairlie, David P. (2007). A refined agonist pharmacophore for protease activated receptor 2. Bioorganic & Medicinal Chemistry Letters, 17 (20), 5552-5557. doi: 10.1016/j.bmcl.2007.08.026
Profiling the enzymatic properties and inhibition of human complement factor B
Le, G. T, Abbenante, G. and Fairlie, D. P (2007). Profiling the enzymatic properties and inhibition of human complement factor B. Journal of Biological Chemistry, 282 (48), 34809-34816. doi: 10.1074/jbc.M705646200
Organic azide inhibitors of cysteine proteases (vol 128, pg 12396, 2006)
Le, Giang Thanh, Abbenante, Giovanni, Madala, Praveen K., Hoang, Huy N. and Fairlie, David P. (2007). Organic azide inhibitors of cysteine proteases (vol 128, pg 12396, 2006). Journal of the American Chemical Society, 129 (30), 9532-9532. doi: 10.1021/ja076897i
Chappell, K. J., Stoermer, M. J., Fairlie, D. P. and Young, P. R. (2007). Generation and characterization of proteolytically active and highly stable truncated and full-length recombinant West Nile virus NS3. Protein Expression and Purification, 53 (1), 87-96. doi: 10.1016/j.pep.2006.10.022
Fairlie, David (2007). Erratum: Latest developments in the treatment of inflammatory disease (Current Medicinal Chemistry (2005) vol. 12 (25) (2923-224)). Current Medicinal Chemistry, 14 (8) doi: 10.2174/092986707780362989
Bogoyevitch, M. A and Fairlie, D. P (2007). A new paradigm for protein kinase inhibition: blocking phosphorylation without directly targeting ATP binding. Drug Discovery Today, 12 (15-16), 622-633. doi: 10.1016/j.drudis.2007.06.008
Function, structure and therapeutic potential of complement C5a receptors
Monk, PN, Scola, A. M., Madala, P. and Fairlie, D. P. (2007). Function, structure and therapeutic potential of complement C5a receptors. British Journal of Pharmacology, 152 (4), 429-448. doi: 10.1038/sj.bjp.0707332
Arumugam, T. V, Tang, S. C, Lathia, J. D, Cheng, A, Mughal, M. R, Chigurupati, S, Magnus, T, Chan, S. L, Jo, D. G, Ouyang, X, Fairlie, D. P, Granger, D. N, Vortmeyer, A, Basta, M and Mattson, M. P (2007). Intravenous immunoglobulin (IVIG) protects the brain against experimental stroke by preventing complement-mediated neuronal cell death. Proceedings of The National Academy of Sciences of The United States of America, 104 (35), 14104-14109. doi: 10.1073/pnas.0700506104
Nonpeptidic ligands for peptide-activated G protein-coupled receptors
Blakeney, J. S, Reid, R. C, Le, G. T and Fairlie, D. P (2007). Nonpeptidic ligands for peptide-activated G protein-coupled receptors. Chemical Reviews, 107 (7), 2960-3041. doi: 10.1021/cr050984g
Gouvea, I. E, Izidoro, M. A, Judice, W. A. S, Cezari, M. H. S, Caliendo, G., Santagada, V., dos Santos, C. N. D, Queiroz, M. H, Juliano, M. A, Young, P. R, Fairlie, D. P and Juliano, L. (2007). Substrate specificity of recombinant dengue 2 virus NS2B-NS3 protease: Influence of natural and unnatural basic amino acids on hydrolysis of synthetic fluorescent substrates. Archives of Biochemistry and Biophysics, 457 (2), 187-196. doi: 10.1016/j.abb.2006.11.005
The role of the N-terminal domain of the complement fragment receptor C5L2 in ligand binding
Scola, A. M., Higginbottom, A., Partridge, L, J., Reid, R. C., Woodruff, T., Taylor, S. M., Fairlie, D. P. and Monk, P. N. (2007). The role of the N-terminal domain of the complement fragment receptor C5L2 in ligand binding. Journal of Biological Chemistry, 282 (6), 3664-3671. doi: 10.1074/jbc.M609178200
Unexpected photolytic decomposition of alkyl azides under mild conditions
Abbenante, G., Le, G. and Fairlie, D. P. (2007). Unexpected photolytic decomposition of alkyl azides under mild conditions. Chemical Communications, 2007 (43), 4501-4503. doi: 10.1039/b708134k
Gregory, Laura S., Kelly, Wendy L., Reid, Robert C., Fairlie, David P. and Forwood, Mark R. (2006). Inhibitors of cyclo-oxygenase-2 and secretory phospholipase A2 preserve bone architecture following ovariectomy in adult rats. Bone, 39 (1), 134-142. doi: 10.1016/j.bone.2005.12.017
Levick, Scott, Loch, David, Rolfe, Barbara, Reid, Robert C., Fairlie, David P., Taylor, Stephan M. and Brown, Lindsay (2006). Antifibrotic activity of an inhibitor of group IIA secretory phospholipase A(2) in young spontaneously hypertensive rats. Journal of Immunology, 176 (11), 7000-7007. doi: 10.4049/jimmunol.176.11.7000
Andrews, Katherine T., Fairlie, David P., Madala, Praveen K., Ray, John, Wyatt, David M., Hilton, Petrina M., Melville, Lewis A., Beattie, Lynette, Gardiner, Donald L., Reid, Robert C., Stoermer, Martin J., Skinner-Adams, Tina, Berry, Colin and McCarthy, James S. (2006). Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria. Antimicrobial Agents And Chemotherapy, 50 (2), 639-648. doi: 10.1128/AAC.50.2.639-648.2006
Agonists and antagonists of protease activated receptors (PARs)
Barry, GD, Le, GT and Fairlie, DP (2006). Agonists and antagonists of protease activated receptors (PARs). Current Medicinal Chemistry, 13 (3), 243-265. doi: 10.2174/092986706775476070
Current Status of Short Synthetic Peptides as Vaccines
Hans, D., Young, P. R. and Fairlie, D. (2006). Current Status of Short Synthetic Peptides as Vaccines. Medicinal Chemistry, 2 (6), 627-646. doi: 10.2174/1573406410602060627
Kahnberg, P. C., Lucke, A., Glenn, M. P., Boyle, G. M., Tyndall, J. D., Parsons, P. G. and Fairlie, D. P. (2006). Design, Synthesis, Potency and Cytoselectivity of Anticancer Agents Derived by Parallel Synthesis from alpha-Aminosuberic Acid. Journal of Medicinal Chemistry, 49 (26), 7611-7622. doi: 10.1021/jm050214x
Chappell, K. J., Stoermer, M. J., Fairlie, D. P. and Young, P. R. (2006). Insights to substrate binding and processing by West Nile Virus NS3 protease through combined modeling, protease mutagenesis, and kinetic studies. Journal of Biological Chemistry, 281 (50), 38448-38458. doi: 10.1074/jbc.M607641200
Modular alpha-helical mimetics with antiviral activity against respiratory syncitial virus
Shepherd, Nicholas E., Hoang, Huy N., Desai, Vishal S., Letouze, Eric, Young, Paul R. and Fairlie, David P. (2006). Modular alpha-helical mimetics with antiviral activity against respiratory syncitial virus. Journal of The American Chemical Society, 128 (40), 13284-13289. doi: 10.1021/ja064058a
New Cysteine Derivatives with Antiproliferative Activity on Melanoma Cells
Lucke, A., Boyle, G. M., Parsons, P. G. and Fairlie, D. (2006). New Cysteine Derivatives with Antiproliferative Activity on Melanoma Cells. Medicinal Chemistry, 2 (2), 123-132. doi: 10.2174/157340606776056124
New insights into growth hormone action
Waters, M. J., Hoang, H. N., Fairlie, D. P., Pelekanos, R. A. and Brown, R. J. (2006). New insights into growth hormone action. Journal of Molecular Endocrinology, 36 (1), 1-7. doi: 10.1677/jmr.1.01933
Organic Azide Inhibitors of Cysteine Proteases
Le, G. T., Abbenante, G., Madala, P. K., Hoang, H. N. and Fairlie, D. P. (2006). Organic Azide Inhibitors of Cysteine Proteases. Journal of the American Chemical Society, 128 (38), 12396-12397. doi: 10.1021/ja0637649
Protease-activated receptor-2 peptides activate neurokinin-1 receptors in the mouse isolated trachea
Abey, HT, Fairlie, DP, Moffatt, JD, Balzary, RW and Cocks, TM (2006). Protease-activated receptor-2 peptides activate neurokinin-1 receptors in the mouse isolated trachea. Journal of Pharmacology And Experimental Therapeutics, 317 (2), 598-605. doi: 10.1124/jpet.105.097121
Singh, Y, Hoang, HN, Flanagan, B and Fairlie, DP (2006). Self-condensation of a thiazole-peptide bearing a 21-membered loop into a library of giant macrocycles with multiple orthogonal loops. Organic Letters, 8 (6), 1053-1056. doi: 10.1021/ol052842e
Nonpeptide ligands that target peptide-activated GPCRs in inflammation
Blakeney, JS and Fairlie, DP (2005). Nonpeptide ligands that target peptide-activated GPCRs in inflammation. Current Medicinal Chemistry, 12 (25), 3027-3042. doi: 10.2174/092986705774462888
Therapeutic targets in inflammatory disease
Hume, David A. and Fairlie, David P. (2005). Therapeutic targets in inflammatory disease. Current Medicinal Chemistry, 12 (25), 2925-2929. doi: 10.2174/092986705774462923
Higginbottom, Adrian, Cain, Stuart A., Woodruff, Trent M., Proctor, Lavinia M., Madala, Praveen K., Tyndall, Joel D. A., Taylor, Stephen M., Fairlie, David P. and Monk, Peter N. (2005). Comparative agonist/antagonist responses in mutant human C5a receptors define the ligand binding site. Journal of Biological Chemistry, 280 (18), 17831-17840. doi: 10.1074/jbc.M410797200
Woodruff, Trent M., Arumugam, Thiruma V., Shiels, Ian A., Newman, Michelle L., Ross, Paul A., Reid, Robert C., Fairlie, David P. and Taylor, Stephen M. (2005). A potent and selective inhibitor of group IIa secretory phospholipase A2 protects rats from TNBS-induced colitis. International Immunopharmacology, 5 (5), 883-892. doi: 10.1016/j.intimp.2005.01.003
Single turn peptide alpha helices with exceptional stability in water
Shepherd, N. E., Hoang, H. N., Abbenante, G. and Fairlie, D. P. (2005). Single turn peptide alpha helices with exceptional stability in water. Journal of The American Chemical Society, 127 (9), 2974-2983. doi: 10.1021/ja0456003
Chappell, Keith J., Nall, Tessa A., Stoermer, Martin J., Fang, Ning-Xia, Tyndall, Joel D. A., Fairlie, David P. and Young, Paul R. (2005). Site-directed mutagenesis and kinetic studies of the West Nile virus NS3 protease identify key enzyme-substrate interactions. Journal of Biological Chemistry, 280 (4), 2896-2903. doi: 10.1074/jbc.M409931200
Over 100 peptide-activated GPCRS recognize turn motifs in ligands
Fairlie, D. P., Tyndall, J. D. A., Abbenante, G. and Pfeiffer, B. (2005). Over 100 peptide-activated GPCRS recognize turn motifs in ligands. Abstracts of Papers of The American Chemical Society, 229, U106-U106.
Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure
Tyndall, J. D. A., Pfeiffer, B., Abbenante, G. and Fairlie, D. P. (2005). Over one hundred peptide-activated G protein-coupled receptors recognize ligands with turn structure. Chemical Reviews, 105 (3), 793-826. doi: 10.1021/cr040689g
Protease inhibitors in the clinic
Abbenante, Giovanni and Fairlie , David P. (2005). Protease inhibitors in the clinic. Medicinal Chemistry, 1 (1), 71-104. doi: 10.2174/1573406053402569
Proteases universally recognize beta strands in their active sites
Tyndall, JDA, Nall, T and Fairlie, DP (2005). Proteases universally recognize beta strands in their active sites. Chemical Reviews, 105 (3), 973-999. doi: 10.1021/cr040669e
Singh, Y, Stoermer, MJ, Lucke, AJ, Guthrie, T and Fairlie, DP (2005). Structural mimicry of two cytochrome b(562) interhelical loops using macrocycles constrained by oxazoles and thiazoles. Journal of The American Chemical Society, 127 (18), 6563-6572. doi: 10.1021/ja0455300
Tumour necrosis factor alpha converting enzyme
Fairlie, D (2005). Tumour necrosis factor alpha converting enzyme. Current Medicinal Chemistry, 12 (25), 2923-2924. doi: 10.2174/092986705774462897
van den Brenk, Anna L., Tyndall, Joel D. A., Cusack, Rodney M., Jones, Alun, Fairlie, David P., Gahan, Lawrence R. and Hanson, Graeme R. (2004). Formation of mononuclear and chloro-bridged binuclear copper(II) complexes of patellamide D, a naturally occurring cyclic peptide: influence of anion and solvent. Journal of Inorganic Biochemistry, 98 (11), 1857-1866. doi: 10.1016/j.jinorgbio.2004.08.005
Arumugam, Thiruma V., Woodruff, Trent M., Stocks, Shelli Z., Proctor, Lavinia M., Pollitt, Sandra, Shiels, Ian A., Reid, Robert C., Fairlie, David P. and Taylor, Stephen M. (2004). Protective effect of a human C5a receptor antagonist against hepatic ischaemia-reperfusion injury in rats. Journal of Hepatology, 40 (6), 934-941. doi: 10.1016/S0168-8278(04)00066-2
Arumugam, Thiruma V., Woodruff, Trent M., Stocks, Shelli Z., Proctor, Lavinia M., Pollitt, Sandra, Shiels, Ian A., Reid, Robert C., Fairlie, David P., Taylor, Stephen M. and M. Colombo (2004). Protective effect of a human C5a receptor antagonist against hepatic ischaemia-reperfusion injury in rats. Journal of Hepatology, 40 (6), 934-941. doi: 10.1016/j.jhep.2004.02.017
Alpha-turn mimetics: short peptide alpha-Helices composed of cyclic metallopentapeptide modules
Kelso, Michael J., Beyer, Renée L., Hoang, Huy N., Lakdawala, Ami S., Snyder, James P., Oliver, Warren V., Robertson, Tom A., Appleton, Trevor G. and Fairlie, David P. (2004). Alpha-turn mimetics: short peptide alpha-Helices composed of cyclic metallopentapeptide modules. Journal of The American Chemical Society, 126 (15), 4828-4842. doi: 10.1021/ja037980i
Proctor, Lavinia M., Arumugam, Thiruma V., Shiels, Ian, Reid, Robert C., Fairlie, David P. and Taylor, Stephen M . (2004). Comparative anti-inflammatory activities of antagonists to C3a and C5a receptors in a rat model of intestinal ischaemia/reperfusion injury. British Journal of Pharmacology, 142 (4), 756-764. doi: 10.1038/sj.bjp.0705819
Antiproliferative and phenotype-transforming antitumor agents derived from cysteine
Glenn, MP, Kahnberg, P, Boyle, GM, Hansford, KA, Hans, D, Martyn, AC, Parsons, PG and Fairlie, DP (2004). Antiproliferative and phenotype-transforming antitumor agents derived from cysteine. Journal of Medicinal Chemistry, 47 (12), 2984-2994. doi: 10.1021/jm030222i
Loughlin, WA, Tyndall, JDA, Glenn, MP and Fairlie, DP (2004). Beta-strand mimetics. Chemical Reviews, 104 (12), 6085-6117. doi: 10.1021/cr040648k
Shepherd, N. E., Abbenante, G. and Fairlie, D. P. (2004). Consecutive cyclic pentapeptide modules form short alpha-helices that are very stable to water and denaturants. Angewandte Chemie-international Edition, 43 (20), 2687-2690. doi: 10.1002/anie.200352659
Reid, Robert C., Pattenden, Lenard K., Tyndall, Joel D. A., Martin, Jennifer L., Walsh, Terry and Fairlie, David P. (2004). Countering cooperative effects in protease inhibitors using constrained b-strand-mimicking templates in focused combinatorial libraries. Journal of Medicinal Chemistry, 47 (7), 1641-1651. doi: 10.1021/jm030337m
Nall, T. A., Chappell, K. J., Stoermer, M. J., Fang, N. X., Tyndall, J. D. A., Young, P. R. and Fairlie, D. P. (2004). Enzymatic characterization and homology model of a catalytically active recombinant West Nile virus NS3 protease. Journal of Biological Chemistry, 279 (47), 48535-48542. doi: 10.1074/jbc.M406810200
Beyer, Renee L., Hoang, Huy N., Appleton, Trevor G. and Fairlie, David P. (2004). Metal Clips Induce Folding of a Short Unstructured Peptide into an a-Helix via Turn Conformations in Water. Kinetic versus Thermodynamic Products. Journal of The American Chemical Society, 126 (46), 15096-15105. doi: 10.1021/ja0453782
March, Darren R., Proctor, Lavinia M., Stoermer, Martin J., Sbaglia, Robert, Abbenante, Giovanni, Reid, Robert C., Woodruff, Trent M., Wadi, Khemar, Paczkowski, Natalii, Tyndall, Joel D. A., Taylor, Stephen M. and Fairlie, David P. (2004). Potent cyclic antagonists of the complement C5a receptor on human polymorphonulcear leukocytes. Relationships between structures and activity. Molecular Pharmacology, 65 (4), 868-879. doi: 10.1124/mol.65.4.868
Woodruff, Trent M., Arumugam, Thiruma V., Shiels, Ian A., Reid, Robert C., Fairlie, David P. and Taylor, Stephen M. (2004). Protective effects of a potent C5a receptor antagonist on experimental acute limb ishemia-reperfusion in rats. Journal of Surgical Research, 116 (1), 81-90. doi: 10.1016/j.jss.2003.04.001
Woodruff, Trent M., Arumugam, Thiruma V., Shiels, Ian A., Reid, Robert C., Fairlie, David P. and Taylor, Stephen M. (2003). A potent human C5a receptor antagonist protects against disease pathology in a rat model of inflammatory bowel disease. Journal of Immunology, 171 (10), 5514-5520. doi: 10.4049/jimmunol.171.10.5514
Cusack, Rodney M., Grondahl, Lisbeth, Fairlie, David P., Hanson, Graeme R. and Gahan, Lawrence R. (2003). Studies of the interaction of Potassium(I), Calcium(II), Magnesium(II), and Copper(II) with Cyclosporin A. Journal of Inorganic Biochemistry, 97 (2), 191-198. doi: 10.1016/S0162-0134(03)00288-5
Arumugam, Thiruma V., Arnold, Naomi, Proctor, Lavinia M., Newman, Michelle, Reid, Robert C., Hansford, Karl A., Fairlie, David P., Shiels, Ian A. and Taylor, Stephen M. (2003). Comparative protection against rat intestinal reperfusion injury by a new inhibitor of sPLA2, COX-1 and COX-2 selective inhibitors, and an LTC4 receptor antagonist. British Journal of Pharmacology, 140 (1), 71-80. doi: 10.1038/sj.bjp.0705402
Reid, Robert C., Abbenante, Giovanni, Taylor, Stephen M. and Fairlie, David P. (2003). A convergent solution-phase synthesis of the macrocycle Ac-Phe-[Orn-Pro-D-Cha-Trp-Arg], a potent new antiinflammatory drug. Journal of Organic Chemistry, 68 (11), 4464-4471. doi: 10.1021/jo034228r
A cyclic metallopeptide induces alpha helicity in short peptide fragments of thermolysin
Kelso, Michael J., Hoang, Huy N., Oliver, Warren, Sokolenko, Nikolai, March, Darren R., Appleton, Trevor G. and Fairlie, David P. (2003). A cyclic metallopeptide induces alpha helicity in short peptide fragments of thermolysin. Angewandte Chemie International Edition, 42 (4), 421-424. doi: 10.1002/anie.200390128
A small molecule C5a receptor antagonist protects kidneys from ischemia/reperfusion injury in rats
Arumugam, T. V., Shiels, I. A., Strachan, A. J., Abbenante, G., Fairlie, D. P. and Taylor, S. M. (2003). A small molecule C5a receptor antagonist protects kidneys from ischemia/reperfusion injury in rats. Kidney International, 63 (1), 134-142. doi: 10.1046/j.1523-1755.2003.00737.x
Conformationally homogeneous cyclic tetrapeptides: Useful new three-dimensional scaffolds
Glenn, MP, Kelso, MJ, Tyndall, JDA and Fairlie, DP (2003). Conformationally homogeneous cyclic tetrapeptides: Useful new three-dimensional scaffolds. Journal of The American Chemical Society, 125 (3), 640-641. doi: 10.1021/ja029205t
Cycloadditions of isobenzofuran to a constrained template bearing neighboring dienophiles
Stoermer, M. J., Butler, D. N., Warrener, R. N., Weerasuria, K. D. V. and Fairlie, D. P. (2003). Cycloadditions of isobenzofuran to a constrained template bearing neighboring dienophiles. Chemistry-a European Journal, 9 (9), 2068-2071. doi: 10.1002/chem.200204619
Hansford, Karl A., Reid, Robert C., Clark, Chris I., Tyndall, Joel D. A., Whitehouse, Michael W., Guthrie, Tom, McGeary, Ross P., Schafer, Karl, Martin, Jennifer L. and Fairlie, David P. (2003). D-Tyrosine as a chiral precusor to potent inhibitors of human nonpancreatic secretory phospholipase A(2) (IIa) with antiinflammatory activity. Chembiochem, 4 (2-3), 181-185. doi: 10.1002/cbic.200390029
Lucke, AJ, Tyndall, JDA, Singh, Y and Fairlie, DP (2003). Designing supramolecular structures from models of cyclic peptide scaffolds with heterocyclic constraints. Journal of Molecular Graphics & Modelling, 21 (5), 341-355. doi: 10.1016/S1093-3263(02)00181-X
Williamson, A. L., Brindley, P. J., Abbenante, G., Datu, B. J. D., Prociv, P., Berry, C., Girdwood, K., Pritchard, D. I., Fairlie, D. P., Hotez, P. J., Zhan, B. and Loukas, A. (2003). Hookworm aspartic protease, Na-APR-2, cleaves human hemoglobin and serum proteins in a host-specific fashion. Journal of Infectious Diseases, 187 (3), 484-494. doi: 10.1086/367708
Tumor cell-specific cytotoxicity by targeting cell cycle checkpoints
Warrener, R, Beamish, H, Burgess, A, Waterhouse, NJ, Giles, N, Fairlie, DP and Gabrielli, B (2003). Tumor cell-specific cytotoxicity by targeting cell cycle checkpoints. Faseb Journal, 17 (9), 1550-1570. doi: 10.1096/fj.02-1003fje
Woodruff, Trent M., Strachan, Anna J., Dryburgh, Nathan, Shiels, Ian A., Reid, Robert C., Fairlie, David P. and Taylor, Stephen M. (2002). Antiarthritic activity of an orally active C5a receptor antagonist against antigen-induced monarticular arthritis in the rat. Arthritis and Rheumatism, 46 (9), 2476-2485. doi: 10.1002/art.10449
Williamson, Angela L., Brindley, Paul J., Abbenante, Giovanni, Prociv, Paul, Berry, Colin, Girdwood, Karen, Pritchard, David I., Fairlie, David P., Hotez, Peter J., Dalton, John P. and Loukas, Alex C. (2002). Cleavage of hemoglobin by hookworm cathespin D aspartic proteases and its potential contribution to host specificity. The FASEB Journal, 16 (10), 1458-1460. doi: 10.1096/fj.02-0181fje
Arumugam, Thiruma V., Shiels, Ian A., Woodruff, Trent M., Reid, Robert C., Fairlie, David P. and Taylor, Stephen M. (2002). Protective effect of a new C5a receptor antagonist against Ischemia-reperfusion injury in the rat small intestine. Journal of Surgical Research, 103 (2), 260-267. doi: 10.1006/jsre.2002.6369
Arakaki, T. L., Fang, N. X., Fairlie, D. P., Young, P. R. and Martin, J. L. (2002). Catalytically active Dengue virus NS3 protease forms aggregates that are separable by size exclusion chromatography. Protein Expression And Purification, 25 (2), 241-247. doi: 10.1016/S1046-5928(02)00005-0
Reid, RC, Kelso, MJ, Scanlon, MJ and Fairlie, DP (2002). Conformationally constrained macrocycles that mimic tripeptide beta-strands in water and aprotic solvents. Journal of The American Chemical Society, 124 (20), 5673-5683. doi: 10.1021/ja0256461
Cusack, R. M., Grondahl, L., Fairlie, D. P., Gahan, L. R. and Hanson, G. R. (2002). Cyclic octapeptides containing thiazole. Effect of stereochemistry and degree of flexibility on calcium binding properties. Journal of The Chemical Society-perkin Transactions 2 (3), 556-563. doi: 10.1039/b109168a
Deactivation of the chlorosulfonate ion coordinated to pentaamminecobalt(III)
Fairlie, DP, Dutton, BH, Mckeon, JA and Jackson, WG (2002). Deactivation of the chlorosulfonate ion coordinated to pentaamminecobalt(III). Inorganic Reaction Mechanisms, 4 (3-4), 197-208. doi: 10.1080/1028662021000062626
Strachan, Anna J., Shiels, Ian A., Reid, Robert C., Fairlie, David P. and Taylor, Stephen M. (2002). Inhibition of immune-complex mediated dermal inflammation in rats following either oral or topical administration of a small molecule C5a receptor antagonist (vol 134, pg 1778, 2001). British Journal of Pharmacology, 135 (2), 579-580. doi: 10.1038/sj.bjp.0704531
Mimetics of the Peptide beta-Strand
Glenn, Matthew P. and Fairlie, David P. (2002). Mimetics of the Peptide beta-Strand. Mini-Reviews in Medicinal Chemistry, 2 (5), 433-445. doi: 10.2174/1389557023405747
Mimetics of the peptide b-strand
Glenn, M. P. and Fairlie, D. P. (2002). Mimetics of the peptide b-strand. Mini reviews in Medicinal Chemistry, 2, 433-445.
Mimetics of the peptide beta-strand.
Glenn M.P. and Fairlie D.P. (2002). Mimetics of the peptide beta-strand.. Mini reviews in medicinal chemistry, 2 (5), 433-445.
Singh, Y, Stoermer, MJ, Lucke, AJ, Glenn, MP and Fairlie, DP (2002). Regioselective synthesis of antiparallel loops on a macrocyclic scaffold constrained by oxazoles and thiazoles. Organic Letters, 4 (20), 3367-3370. doi: 10.1021/ol026463m
Synthesis and structural properties of patellamide a derivatives and their copper(II) compounds
Bernhardt, P. V., Comba, P., Fairlie, D. P., Gahan, L. R., Hanson, G. R. and Lotzbeyer, L. (2002). Synthesis and structural properties of patellamide a derivatives and their copper(II) compounds. Chemistry-a European Journal, 8 (7), 1527-1536. doi: 10.1002/1521-3765(20020402)8:7<1527::AID-CHEM1527>3.3.CO;2-6
Glenn, MP, Pattenden, LK, Reid, RC, Tyssen, DP, Tyndall, JDA, Birch, CJ and Fairlie, DP (2002). beta-strand mimicking macrocyclic amino acids: Templates for protease inhibitors with antiviral activity. Journal of Medicinal Chemistry, 45 (2), 371-381. doi: 10.1021/jm010414i
Leung, D., Schroder, K., White, H., Fang, N. X., Stoermer, M. J., Abbenante, G., Martin, J. L., Young, P. R. and Fairlie, D. P. (2001). Activity of recombinant dengue 2 virus NS3 protease in the presence of a truncated NS2B co-factor, small peptide substrates, and inhibitors. Journal of Biological Chemistry, 276 (49), 45762-45771. doi: 10.1074/jbc.M107360200
Strachan, Anna J., Shiels, Ian A., Reid, Robert C., Fairlie, David P., Taylor, Stephen M. and R. A. North (2001). Inhibition of immune-complex mediated dermal inflammation in rats following either oral or topical administration of a small molecule C5a receptor antagonist. British Journal of Pharmacology, 134 (12), 1778-1786. doi: 10.1038/sj.bjp.0704417
Fairlie, DP (2001). Protease inhibitors. Current Medicinal Chemistry, 8 (8), U2-U2.
Woodruff, Trent M., Strachan, Anna J., Sanderson, Sam D., Monk, Peter N., Wong, Allan K., Fairlie, David P. and Taylor, Stephen M. (2001). Species dependence for binding of small molecule agonist and antagonists to the C5a receptor on polymorphonuclear leukocytes. Inflammation, 25 (3), 171-177. doi: 10.1023/A:1011036414353
Tyndall, JDA and Fairlie, DP (2001). Macrocycles mimic the extended peptide conformation recognized by aspartic, serine, cysteine and metallo proteases. Current Medicinal Chemistry, 8 (8), 893-907. doi: 10.2174/0929867013372715
Cain, S. A., Woodruff, T. M., Taylor, S. M., Fairlie, D. P., Sanderson, S. D. and Monk, P. N. (2001). Modulation of ligand selectivity by mutation of the first extracellular loop of the human C5a receptor. Biochemical Pharmacology, 61 (12), 1571-1579. doi: 10.1016/S0006-2952(01)00608-6
Singh, Y., Sokolenko, N., Kelso, M. J., Gahan, L. R., Abbenante, G. and Fairlie, D. P. (2001). Novel Cylindrical, Conical, and Macrocyclic Peptides from the Cyclooligomerization of Functionalized Thiazole Amino Acids. Journal of the American Chemical Society, 123 (2), 333-334. doi: 10.1021/ja002666z
Fairlie, D. P. (2001). Preface. Current Medicinal Chemistry, 8 (8) doi: 10.2174/0929867013372724
Proteolysis of human hemoglobin by schistosome cathepsin D
Brindley, P. J., Kalinna, B. H., Wong, J. Y. M., Bogitsh, B. J., King, L. T., Smyth, D. J., Verity, C. K., Abbenante, G., Brinkworth, R. I., Fairlie, D. P., Smythe, M. L., Milburn, P. J., Bielefeldt-Ohmann, H., Zheng, Y. and McManus, D. P. (2001). Proteolysis of human hemoglobin by schistosome cathepsin D. Molecular And Biochemical Parasitology, 112 (1), 103-112. doi: 10.1016/S0166-6851(00)00351-0
An efficient Fmoc strategy for the rapid synthesis of peptide para-nitroanilides
Abbenante, J., Leung, D., Bond, T. J. and Fairlie, D. P. (2000). An efficient Fmoc strategy for the rapid synthesis of peptide para-nitroanilides. Letters in Peptide Science, 7 (6), 347-351. doi: 10.1023/A:1013016323676
Strachan, Anna J., Woodruff, Trent M., Haaima, Gerald, Fairlie, David P. and Taylor, Stephen M. (2000). A new small molecule C5a receptor antagonist inhibits the reverse- passive Arthus reaction and endotoxic shock in rats. Journal of Immunology, 164 (12), 6560-6565. doi: 10.4049/jimmunol.164.12.6560
Qiu, Ling, Burgess, Andrew, Fairlie, David P., Leonard, Helen, Parsons, Peter G. and Gabrielli, Brian G. (2000). Histone deacetylase inhibitors trigger a G2 checkpoint in normal cells that is defective in tumor cells. Molecular Biology of the Cell, 11 (6), 2069-2083. doi: 10.1091/mbc.11.6.2069
Poulsen, Sally-Ann, Watson, Andrew A., Fairlie, David P. and Craik, David J. (2000). Solution structures in aqueous SDS micelles of two amyloid beta peptides of A beta(1-28) mutated at the alpha-secretase cleavage site (K16E, K16F). Journal of Structural Biology, 130 (2-3), 142-152. doi: 10.1006/jsbi.2000.4267
Andrews, Kathy T., Walduck, Anna, Kelso, Mike J., Fairlie, David P., Saul, Allan and Parsons, Peter G. (2000). Anti-malarial effect of histone deacetylation inhibitors and mammalian tumour cytodifferentiating agents Anna Walduck, Mike J. Kelso, David P. Fairlie, Allan Saul, Peter G. Parsons. International Journal for Parasitology, 30 (6), 761-768. doi: 10.1016/S0020-7519(00)00043-6
Protease inhibitors: Current status and future prospects
Leung, D., Abbenante, G. and Fairlie, D. P. (2000). Protease inhibitors: Current status and future prospects. Journal of Medicinal Chemistry, 43 (3), 305-341. doi: 10.1021/jm990412m
Inhibitors of beta-amyloid formation based on the beta-secretase cleavage site
Abbenante, G., Kovacs, D. M., Leung, D. L., Craik, D. J., Tanzi, R. E. and Fairlie, D. P. (2000). Inhibitors of beta-amyloid formation based on the beta-secretase cleavage site. Biochemical And Biophysical Research Communications, 268 (1), 133-135. doi: 10.1006/bbrc.2000.2098
Cell phenotype as a target of drug therapy in chronic inflammatory diseases
Shiels, I. A., Taylor, S. M. and Fairlie, D. P. (2000). Cell phenotype as a target of drug therapy in chronic inflammatory diseases. Medical Hypotheses, 54 (2), 193-197. doi: 10.1054/mehy.1999.0017
Strachan, A. J., Woodruff, T.M., Haaima, G., Fairlie, D. P. and Taylor, S. M. (2000). A new small molecule C5a receptor antagonist inhibits the reverse-passive arthus reaction and endotoxic shock in rats. Journal of Immunology, 164 (4), 6560-6565.
Atwood, C. S., Scarpa, R. C., Huang, X., Moir, R. D., Jones, W. D., Fairlie, D. P., Tanzi, R. E. and Bush, A. I. (2000). Characterization of copper interactions with alzheimer amyloid bpeptides: Identification of an attomolar-affinity copper binding site on Amyloid 1-42. Journal of Neurochemistry, 75 (3), 1219-1233. doi: 10.1046/j.1471-4159.2000.0751219.x
Fairlie, D. P., Tyndall, J. D. A., Reid, R. C., Wong, A. K., Abbenante, G., Scanlon, M. J., March, D. R., Bergman, D. A., Chai, C. L. L. and Burkett, B. A. (2000). Conformational selection of inhibitors and substrates by proteolytic enzymes: Implications for drug design and polypeptide processing. Journal of Medicinal Chemistry, 43 (7), 1271-1281. doi: 10.1021/jm990315t
Cusack, R. M., Grondahl, L., Abbenante, G., Fairlie, D. P., Gahan, L. R., Hanson, G. R. and Hambley, T. W. (2000). Conformations of cyclic octapeptides and the influence of heterocyclic ring constraints upon calcium binding. Journal of The Chemical Society-perkin Transactions 2 (2), 323-331. doi: 10.1039/a906090a
Haynes, DR, Harkin, DG, Bignold, LP, Hutchens, MJ, Taylor, SM and Fairlie, DP (2000). Inhibition of C5a-induced neutrophil chemotaxis and macrophage cytokine production In Vitro by a new C5a receptor antagonist. Biochemical Pharmacology, 60 (5), 729-733. doi: 10.1016/S0006-2952(00)00361-0
Rauk, A., Armstrong, D. A. and Fairlie, D. P. (2000). Is oxidative damage by b- amyloid and prion peptides mediated by hydrogen atom transfer from glycine a-carbon to methionine sulfur within b- sheets?. Journal of American Chemical Society, 122 (40), 9761-9767. doi: 10.1021/ja994436u
Regulators of the anaphylatoxin C5a
Taylor, SM and Fairlie, DP (2000). Regulators of the anaphylatoxin C5a. Expert Opinion in Therapeutic Patents, 10 (4), 449-458. doi: 10.1517/13543776.10.4.449
Small peptides do not inhibit human non-pancreatic secretory phospholipase-A 2 (Type IIA)
Clark, C. I., Reid, R. C., McGeary, R. P., Schafer, K. and Fairlie, D. P. (2000). Small peptides do not inhibit human non-pancreatic secretory phospholipase-A 2 (Type IIA). Bioichemistry BIophysical Research Communications, 274 (3), 831-834. doi: 10.1006/bbrc.2000.3221
Tyndall, J. D. A., Reid, R. C., Tyssen, D. P., Jardine, D. K., Todd, B., Passmore, M., March, D. R., Pattenden, L., Bergman, D. A., Alewood, D., Hu, S., Alewood, P.F., Birch, C. J., Martin, J. L. and Fairlie, D. (2000). Synthesis, stability, antiviral activity, and protease-bound structures of substrate-mimicking constrained macrocyclic inhibitors of HIV-1 protease. Journal of Medicinal Chemistry, 43 (19), 3495-3504. doi: 10.1021/jm000013n
Kelso, M. J., Hoang, H. N., Appleton, T. G. and Fairlie, D. (2000). The first solution structure of a single a-helical turn. A pentapeptide a -Helix stabilized by a metal clip. Journal of Americal Chemical Society, 122 (42), 10488-10489. doi: 10.1021/ja002416i
Huang, XD, Cuajungco, MP, Atwood, CS, Hartshorn, MA, Tyndall, JDA, Hanson, GR, Stokes, KC, Leopold, M, Multhaup, G, Goldstein, LE, Scarpa, RC, Saunders, AJ, Lim, J, Moir, RD, Glabe, C, Bowden, EF, Masters, CL, Fairlie, DP, Tanzi, RE and Bush, AI (1999). Cu(II) potentiation of Alzheimer A beta neurotoxicity - Correlation with cell-free hydrogen peroxide production and metal reduction. Journal of Biological Chemistry, 274 (52), 37111-37116. doi: 10.1074/jbc.274.52.37111
Brinkworth, R. I., Fairlie, D., Leung, D. and Young, P. R. (1999). Homology model of the dengue 2 virus NS3 protease: putative interactions with both substrate and NS2B cofactor.. Journal of General Virology, 80 (5), 1167-1177. doi: 10.1099/0022-1317-80-5-1167
Effects of a new C5a receptor antagonist on C5a- and endotoxin-induced neutropenia in the rat
Short, Anna, Wong, Allan K., Finch, Angela M., Haaima, Gerald, Shiels, Ian A., Fairlie, David P. and Taylor, Stephen M. (1999). Effects of a new C5a receptor antagonist on C5a- and endotoxin-induced neutropenia in the rat. British Journal of Pharmacology, 126 (2), 551-554. doi: 10.1038/sj.bjp.0702338
Qiu, L., Kelso, M., Hansen, C., West, M. L., Fairlie, D. and Parsons, P. (1999). Anti-tumour activity in vitro and in vivo of selective differentiating agents containing hydroxamate.. British Journal of Cancer, 80 (8), 1252-1258. doi: 10.1038/sj.bjc.6690493
Aqueous Dissolution of Alzheimer's Disease Ab Amyloid Deposits by Biometal Depletion
Cherny, R. A., Legg, J. T., McLean, C. A., Fairlie, D., Huang, X., Atwood, C.S., Beyreuther, K., Tanzi, R. E., Masters, C. L. and Bush, A. (1999). Aqueous Dissolution of Alzheimer's Disease Ab Amyloid Deposits by Biometal Depletion. Journal of Biological Chemistry, 274 (33), 23223-23228. doi: 10.1074/jbc.274.33.23223
Con formational homogeneity in molecular recognition by proteolytic enzymes
Tyndall, J. and Fairlie, D. (1999). Con formational homogeneity in molecular recognition by proteolytic enzymes. Journal of Molecular Recognition, 12 (6), 363-370. doi: 10.1002/(SICI)1099-1352(199911/12)12:6<363::AID-JMR478>3.3.CO;2-D
Cu (II ) Potentiation of Alzheimer Ab Neurotoxicity
Huang, X., Cuajungco, M. P., Atwood, C. S., Hartshorn, M. A., Tyndall, J. D., Hanson, G. R., Stokes, K. C., Leopold, M., Multhaup, G., Goldstein, L. E., Scarpa, R. C., Saunders, A. J., Lim, J., Moir, R. D., Glabe, C., Bowden, E. F., Masters, C. L., Fairlie, D., Tanzi, R. E. and Bush, A. I. (1999). Cu (II ) Potentiation of Alzheimer Ab Neurotoxicity. Jornal of Biological Chemistry, 274 (52), 37111-37116.
Sokolenko, N., Abbenante, G., Scanlon, M. J., Jones, A., Gahan, L. R., Hanson, G. R. and Fairlie, D. P. (1999). Cyclooligomerization of Thiazole-Containing Tetrapeptides. Symmetrical Macrocycles with up to 76 Amino Acids. Journal of the American Chemical Society, 121 (11), 2603-2604. doi: 10.1021/ja983354n
Development of C5a receptor antagonists
Wong, A., Taylor, S. M. and Fairlie, D. (1999). Development of C5a receptor antagonists. Investigational Drugs, 2 (7), 686-693.
Fairlie, D., Turner, M., Byriel, K., McKeon, J. A. and Jackson, G. W. (1999). Facile and steroselective condensation of acetone with ammonia ligands on cobalt ( III):structure of a N-bonded cyanate complex containing the 2-methyl-2-amino-4-imino-pentane ligand. Inorganica Chimica Acta, 290 (2), 133-138. doi: 10.1016/S0020-1693(99)00110-3
Grondahl, L., Sokolenko, N., Abbenante, G., Fairlie, D. P., Hanson, G. R. and Gahan, L. R. (1999). Interaction of zinc(II) with the cyclic octapeptides, cyclo[Ile(Oxn)-D-Val(Thz)](2) and ascidiacyclamide, a cyclic peptide from Lissoclinum patella. Journal of The Chemical Society-dalton Transactions (8), 1227-1234. doi: 10.1039/a808836e
Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a
Finch, A., Wong, A. K., Paczkowski, N. J., Wadi, S. K., Craik, D. J., Fairlie, D. and Taylor, S. M. (1999). Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. Journal of Medicinal Chemistry, 42 (6), 1965-1974. doi: 10.1021/jm9806594
Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease
Martin, J. L., Begun, J., Schindeler, A., Wickramasinghe, W. A., Alewood, D., Alewood, P. F., Bergman, D. A., Brinkworth, R. I., Abbenante, G., March, D. R., Reid, R. C., Fairlie, D. P. and Armstrong, Richard A. (1999). Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease. Biochemistry, 38 (25), 7978-7988. doi: 10.1021/bi990174x
Pharmacological characterization of antagonists of the C5a receptor
Paczkowski, NJ, Finch, AM, Whitmore, JB, Short, AJ, Wong, AK, Monk, PN, Cain, SA, Fairlie, DP and Taylor, SM (1999). Pharmacological characterization of antagonists of the C5a receptor. British Journal of Pharmacology, 128 (10), 1461-1466. doi: 10.1038/sj.bjp.0702938
The possible origin of free radicals from amyloid peptides in Alzheimer's disease
Bush, A. I., Huang, X. and Fairlie, D. (1999). The possible origin of free radicals from amyloid peptides in Alzheimer's disease. Neurobiology of Aging, 20 (3), 335-337. doi: 10.1016/S0197-4580(99)00058-5
X-ray absorption spectroscopy of cadmium phytochelatin and model systems
Pickering, I. J., Prince, R. C., George, G. N., Rauser, W. E., Wickramasinghe, W. A., Watson, A. A., Dameron, C., Dance, I. G., Fairlie, D. and Salt, D. E. (1999). X-ray absorption spectroscopy of cadmium phytochelatin and model systems. Biochimica Et Biophysica Acta, 1429 (2), 351-364. doi: 10.1016/S0167-4838(98)00242-8
Wong A.K., Jacobsen M.P., Winzor D.J. and Fairlie D.P. (1998). Template assembled synthetic proteins (TASPS). Are template size, shape, and directionality important in formation of four-helix bundles?. Journal of the American Chemical Society, 120 (16), 3836-3841. doi: 10.1021/ja971951o
Conformationally restricted cyclic peptides incorporating oxazoline and thiazole ring constraints.
Abbenante, G., Sokolenko, N. and Fairlie, D. P. (1998). Conformationally restricted cyclic peptides incorporating oxazoline and thiazole ring constraints.. Abstracts of Papers of The American Chemical Society, 216, U382-U382.
Wong, AK, Finch, AM, Pierens, GK, Craik, DJ, Taylor, SM and Fairlie, DP (1998). Small molecular probes for G-protein-coupled C5a receptors: Conformationally constrained antagonists derived from the C terminus of the human plasma protein C5a. Journal of Medicinal Chemistry, 41 (18), 3417-3425. doi: 10.1021/jm9800651
Coles, M, Bicknell, W, Watson, AA, Fairlie, DP and Craik, DJ (1998). Solution structure of amyloid beta-peptide(1-40) in a water-micelle environment. Is the membrane-spanning domain where we think it is?. Biochemistry, 37 (31), 11064-11077. doi: 10.1021/bi972979f
Watson, AA, Fairlie, DP and Craik, DJ (1998). Solution structure of methionine-oxidized amyloid beta-peptide (1-40). Does oxidation affect conformational switching?. Biochemistry, 37 (37), 12700-12706. doi: 10.1021/bi9810757
Comba, P, Cusack, R, Fairlie, DP, Gahan, LR, Hanson, GR, Kazmaier, U and Ramlow, A (1998). The solution structure of a copper(II) compound of a new cyclic octapeptide by EPR spectroscopy and force field calculations. Inorganic Chemistry, 37 (26), 6721-6727. doi: 10.1021/ic9809299
Simple cis-epoxide-based inhibitors of HIV-1 protease
Abell A.D., Hoult D.A., Bergman D.A. and Fairlie D.P. (1997). Simple cis-epoxide-based inhibitors of HIV-1 protease. Bioorganic & Medicinal Chemistry Letters, 7 (22), 2853-2856. doi: 10.1016/S0960-894X(97)10106-8
Parsons, P. G., Hansen, C., Fairlie, D. P., West, M. L., Danoy, P. A. C., Sturm, R. A., Dunn, I. S., Pedley, J. and Ablett, E. M. (1997). Tumor selectivity and transcriptional activation by azelaic bishydroxamic acid in human melanocytic cells. Biochemical Pharmacology, 53 (11), 1719-1724. doi: 10.1016/S0006-2952(97)00016-6
Activation of thiourea bound through sulfur to pentaammineruthenium(III): Structure and reactivity
Fairlie, DP, Wickramasinghe, WA, Byriel, KA and Taube, H (1997). Activation of thiourea bound through sulfur to pentaammineruthenium(III): Structure and reactivity. Inorganic Chemistry, 36 (11), 2242-2243. doi: 10.1021/ic9611397
Biphasic response of the metallothionein promoter to ultraviolet radiation in human melanoma cells
Hansen, C., Ablett, E., Green, A., Sturm, R. A., Dunn, I. S., Fairlie, D. P., West, M. L. and Parsons, P. G. (1997). Biphasic response of the metallothionein promoter to ultraviolet radiation in human melanoma cells. Photochemistry and Photobiology, 65 (3), 550-555. doi: 10.1111/j.1751-1097.1997.tb08603.x
Fairlie, David P., Jackson, W. Gregory, Skelton, Brian W., Wen, Huo, White, Allan H., Wickramasinghe, Wasantha A., Woon, Tai Chin and Taube, Henry (1997). Models for arginine-metal binding. Synthesis of guanidine and urea ligands through amination and hydration of a cyanamide ligand bound to platinum(II), osmium(III), and cobalt(III). Inorganic Chemistry, 36 (6), 1020-1028. doi: 10.1021/ic961138e
Oxygen versus nitrogen bonding of carboxamides to pentaammineruthenium(II/III)
Fairlie, David P., Ilan, Yigal and Taube, Henry (1997). Oxygen versus nitrogen bonding of carboxamides to pentaammineruthenium(II/III). Inorganic Chemistry, 36 (6), 1029-1037. doi: 10.1021/ic9611406
Organization of amino acids using a metallotriazacyclononane template
Watson, AA, Willis, AC and Fairlie, DP (1997). Organization of amino acids using a metallotriazacyclononane template. Inorganic Chemistry, 36 (5), 752-&. doi: 10.1021/ic960867r
Reid, R. C., Abbenante, G., March, D. R., Scanlon, M. and Fairlie, D. P. (1997). A novel strategy for the design of potent peptidomimetic inhibitors of proteolytic enzymes: Application to HIV-1 protease.. Abstracts of Papers of The American Chemical Society, 214, 177-MEDI.
Conformationally constrained cyclic mimetics of protein and peptide surfaces.
Wong, A. K., Reid, R. C., Abbenante, J. and Fairlie, D. P. (1997). Conformationally constrained cyclic mimetics of protein and peptide surfaces.. Abstracts of Papers of The American Chemical Society, 214 (1), 388-ORGN.
Conformationally constrained small molecule antagonists of C5a.
Wong, AK, Finch, AM, Pierens, GK, Taylor, SM and Fairlie, DP (1997). Conformationally constrained small molecule antagonists of C5a.. Abstracts of Papers of The American Chemical Society, 214, 9-MEDI.
The role of oxazoline and thiazole ring constraints in cyclic peptides of marine origin.
Abbenante, G., Sokolenko, N. and Fairlie, D. P. (1997). The role of oxazoline and thiazole ring constraints in cyclic peptides of marine origin.. Abstracts of Papers of The American Chemical Society, 214, 389-ORGN.
Structure-activity relationships for macrocyclic peptidomimetic inhibitors of HIV-1 protease.
Abbenante, G., Bergman, D. A., Brinkworth, R. I., March, D. R., Reid, R. C., Hunt, P. A., James, I. W., Dancer, R. J., Garnham, B., Stoermer, M. L. and Fairlie, D. P. (1996). Structure-activity relationships for macrocyclic peptidomimetic inhibitors of HIV-1 protease.. Bioorganic & Medicinal Chemistry Letters, 6 (21), 2531-2536. doi: 10.1016/0960-894X(96)00468-4
Abbenante, G., Fairlie, D. P., Gahan, L. R., Hanson, G. R., Pierens, G. K. and van den Brenk, A. L. (1996). Conformational control by thiazole and oxazoline rings in cyclic octapeptides of marine origin. Novel macrocyclic chair and boat conformations. Journal of the American Chemical Society, 118 (43), 10384-10388. doi: 10.1021/ja962260f
Reid, Robert C., March, Darren R., Dooley, Michael J., Bergman, Doug A., Abbenante, Giovanni and Fairlie, David P. (1996). A novel bicyclic enzyme inhibitor as a consensus peptidomimetic for the receptor-bound conformations of 12 peptidic inhibitors of HIV-1 protease. Journal of The American Chemical Society, 118 (36), 8511-8517. doi: 10.1021/ja960433v
Kennard, Colin H.L., Byriel, Karl A., Woon, Tai Chin and Fairlie, David P. (1996). Structure of a novel protonated oxadiazine: an unusual heterocycle from the cycloaddition of a ketone with nitriles. Chemical Communications (15), 1731-1732. doi: 10.1039/cc9960001731
March, D. R., Abbenante, G., Bergman, D. A., Brinkworth, R. I., Wickramasinghe, W., Begun, J., Martin, J. L. and Fairlie, D. P. (1996). Substrate-based cyclic peptidomimetics of Phe-Ile-Val that inhibit HIV-1 protease using a novel enzyme-binding mode. Journal of The American Chemical Society, 118 (14), 3375-3379. doi: 10.1021/ja953790z
van den Brenk, Anna L., Fairlie, David P., Gahan, Lawrence R., Hanson, Graeme R. and Hambley, Trevor W. (1996). A novel potassium-binding hydrolysis product of ascidiacyclamide, a cyclic peptide isolated from the ascidian lissoclinum patella. Inorganic Chemistry, 35 (5), 1095-1100. doi: 10.1021/ic9504755
Wong M.F., Huang P.P., Brinkworth R.I., Yashiro M., Mohan P., Fairlie D.P., Baba M. and Verma S. (1996). Non-peptide inhibitors of HIV-1 protease. Synthesis and structural evaluation of symmetric and non-symmetric naphthalenesulfonic acid analogues. European Journal of Medicinal Chemistry, 31 (3), 249-255. doi: 10.1016/0223-5234(96)89141-0
Hydroxyquinones are competitive non-peptide inhibitors of HIV-1 proteinase
Brinkworth R.I. and Fairlie D.P. (1995). Hydroxyquinones are competitive non-peptide inhibitors of HIV-1 proteinase. Biochimica et Biophysica Acta (BBA)/Protein Structure and Molecular, 1253 (1), 5-8. doi: 10.1016/0167-4838(95)00183-U
Abbenante, G, March, DR, Bergman, DA, Hunt, PA, Garnham, B, Dancer, RJ, Martin, JL and Fairlie, DP (1995). Regioselective Structural and Functional Mimicry of Peptides - Design of Hydrolytically-Stable Cyclic Peptidomimetic Inhibitors of Hiv-1 Protease. Journal of the American Chemical Society, 117 (41), 10220-10226. doi: 10.1021/ja00146a007
Nmr Solution Structure of the Rna-Binding Peptide From Human-Immunodeficiency-Virus (type-1) Rev
Scanlon, MJ, Fairlie, DP, Craik, DJ, Englebretsen, DR and West, ML (1995). Nmr Solution Structure of the Rna-Binding Peptide From Human-Immunodeficiency-Virus (type-1) Rev. Biochemistry, 34 (26), 8242-8249. doi: 10.1021/bi00026a005
Stoermer, Martin J. and Fairlie, David P. (1995). A selective and versatile synthesis of substituted chromones via addition of phenols to dimethyl acetylenedicarboxylate. Australian Journal of Chemistry, 48 (3), 677-686. doi: 10.1071/CH9950677
Watson A.A. and Fairlie D.P. (1995). Ammonia and carbon dioxide from urea. A multinuclear NMR study of the activation of urea by platinum(II). Inorganic Chemistry, 34 (11), 3087-3092. doi: 10.1021/ic00115a041
Macrocyclic peptidomimetics - Forcing peptides into bioactive conformations
Fairlie D.P., Abenante G. and March D.R. (1995). Macrocyclic peptidomimetics - Forcing peptides into bioactive conformations. Current Medicinal Chemistry, 2 (2), 654-686. doi: 10.2174/0929867302666220218001506
Targeting HIV-1 protease: A test of drug-design methodologies
West M.L. and Fairlie D.P. (1995). Targeting HIV-1 protease: A test of drug-design methodologies. Trends in Pharmacological Sciences, 16 (2), 67-75. doi: 10.1016/S0165-6147(00)88980-4
Amide-Iminol Tautomerism - Effect of Metalation
Fairlie, DP, Woo, TC, Wickramasinghe, WA and Willis, AC (1994). Amide-Iminol Tautomerism - Effect of Metalation. Inorganic Chemistry, 33 (26), 6425-6428. doi: 10.1021/ic00104a067
Anti-Inflammatory activity of a holothurian (sea cucumber) food supplement in rats
Whitehouse, M. W. and Fairlie, D. P. (1994). Anti-Inflammatory activity of a holothurian (sea cucumber) food supplement in rats. Inflammopharmacology, 2 (4), 411-417. doi: 10.1007/BF02678607
van den Brenk, Anna L., Byriel, Karl A., Fairlie, David P., Gahan, Lawrence R., Hanson, Graeme R., Hawkins, Clifford J., Jones, Alun, Kennard, Colin H. L., Moubaraki, Boujemaa and Murray, Keith S. (1994). Crystal Structure, Electrospray Ionization Mass Spectrometry, Electron Paramagnetic Resonance and Magnetic Susceptibility Study of [Cu2(ascidH2) (1,2-mCO3)(H2O)2].2H2O, the Biscopper (II) Complex of Ascidiacyclamide (ascidH4), a Cyclic Peptide Isolated fr. Inorganic Chemistry, 33 (16), 3549-3557. doi: 10.1021/ic00094a019
Binding of copper(II) to the cyclic octapeptide patellamide D
Van den Brenk, Anna L., Fairlie, David P., Hanson, Graeme R., Gahan, Lawrence R., Hawkins, Clifford J. and Jones, Alun (1994). Binding of copper(II) to the cyclic octapeptide patellamide D. Inorganic Chemistry, 33 (10), 2280-2289. doi: 10.1021/ic00088a034
Whitehouse, M. W., Fairlie, D. P. and Thong, Y. H. (1994). Anti-inflammatory activity of the isoquinoline alkaloid, tetrandrine, against established adjuvant arthritis in rats. Agents and Actions, 42 (3-4), 123-127. doi: 10.1007/BF01983477
ANGUS, PM, FAIRLIE, DP and JACKSON, WG (1993). SYNTHESIS, SOLUTION STRUCTURE, AND REACTIVITY OF OXYGEN-BOUND AMIDES ON COBALT(III), (VOL 32, PG 450, 1993). Inorganic Chemistry, 32 (19), 4168-4168. doi: 10.1021/ic00071a038
Alewood P.F., Bailey A.J., Brinkworth R.I., Fairlie D. and Jones A. (1993). Characterisation of TNF-α-related peptides by high-performance liquid chromatography-mass spectrometry and high-performance liquid chromatography-tandem mass spectrometry. Journal of Chromatography A, 646 (1), 185-191. doi: 10.1016/S0021-9673(99)87020-4
A new dinuclear amine-cobalt(III) complex containing two bridging amide ions
Angus P.M., Fairlie D.P., Gunasingam R., Zhu T. and Jackson W.G. (1993). A new dinuclear amine-cobalt(III) complex containing two bridging amide ions. Inorganica Chimica Acta, 209 (2), 123-127. doi: 10.1016/S0020-1693(00)85132-4
Seow, W. K., Nakamura, K., Sugimura, Y., Sugimoto, Y., Yamada, Y., Fairlie, D. P. and Thong, Y. H. (1993). Inhibitory effects of bisbenzylisoquinolines on synthesis of the inflammatory cytokines interleukin-1 and tumour necrosis factor-alpha. Mediators of Inflammation, 2 (3), 199-203. doi: 10.1155/S0962935193000262
Oxygen versus nitrogen coordination of a urea to (diethylenetriamine)platinum(II)
Woon, T. C., Wickramasinghe, W.A. and Fairlie, D. P. (1993). Oxygen versus nitrogen coordination of a urea to (diethylenetriamine)platinum(II). Inorganic Chemistry, 32 (10), 2190-2194. doi: 10.1021/ic00062a050
Synthesis, Solution Structure, and Reactivity of Oxygen-Bound Amides On Cobalt(Iii)
Angus, Patricia M., Fairlie, David P. and Jackson, W. Gregory (1993). Synthesis, Solution Structure, and Reactivity of Oxygen-Bound Amides On Cobalt(Iii). Inorganic Chemistry, 32 (4), 450-459. doi: 10.1021/ic00056a018
Designing metalloinhibitors for delivery to peptide receptors in enzymes
Fairlie D.P. (1993). Designing metalloinhibitors for delivery to peptide receptors in enzymes. Drug Design and Discovery, 10 (3), 183-197.
Flavones are inhibitors of HIV-1 proteinase
Brinkworth R.I., Stoermer M.J. and Fairlie D.P. (1992). Flavones are inhibitors of HIV-1 proteinase. Biochemical and Biophysical Research Communications, 188 (2), 631-637. doi: 10.1016/0006-291X(92)91103-W
Non-peptidic anti-aids agents: Inhibition of HIV-1 proteinase by disulfonates
Brinkworth R.I. and Bairlie D.P. (1992). Non-peptidic anti-aids agents: Inhibition of HIV-1 proteinase by disulfonates. Biochemical and Biophysical Research Communications, 188 (2), 624-630. doi: 10.1016/0006-291X(92)91102-V
Fairlie D.P., Whitehouse M.W. and Taylor R.M. (1992). Zinc monoglycerolate - a slow-release source of therapeutic zinc: solubilization by endogenous ligands. Agents and Actions, 36 (1-2), 152-158. doi: 10.1007/BF01991243
Amide complexes of (diethylenetriamine)platinum(II)
Woon T.C. and Fairlie D.P. (1992). Amide complexes of (diethylenetriamine)platinum(II). Inorganic Chemistry, 31 (20), 4069-4074. doi: 10.1021/ic00046a016
Inhibition of HIV-1 proteinase by metal ions
Woon T.C., Brinkworth R.I. and Fairlie D.P. (1992). Inhibition of HIV-1 proteinase by metal ions. International Journal of Biochemistry, 24 (6), 911-914. doi: 10.1016/0020-711X(92)90096-J
Transdermal delivery of inorganic complexes as metal drugs or nutritional supplements
Fairlie, D. P. and Whitehouse, M. W. (1991). Transdermal delivery of inorganic complexes as metal drugs or nutritional supplements. Drug Design and Discovery, 8 (2), 83-102.
Fairlie, David P., Angus, Patricia M., Fenn, M. David and Jackson, W. Gregory (1991). Factors Influencing the Nitrogen Vs Oxygen Bonding Mode of Amides Bound to Pentaamminecobalt(Iii) and the Kinetics and Mechanism of Rearrangement. Inorganic Chemistry, 30 (7), 1564-1569. doi: 10.1021/ic00007a026
Inhibition of HIV-1 proteinase by non-peptide carboxylates
Brinkworth, Ross I., Woon, Tai Chin and Fairlie, David P. (1991). Inhibition of HIV-1 proteinase by non-peptide carboxylates. Biochemical and Biophysical Research Communications, 176 (1), 241-246. doi: 10.1016/0006-291X(91)90915-T
Fairlie D.P. and Jackson W.G. (1990). A general synthetic route to pentaamminecobalt(III) complexes of N-bonded amides, ureas, carbamates, sulfinamides, sulfonamides and sulfamate. Inorganica Chimica Acta, 175 (2), 203-207. doi: 10.1016/S0020-1693(00)84828-8
FAIRLIE, DP (1990). CORRECTION. Inorganic Chemistry, 29 (18), 3630-3630. doi: 10.1021/ic00343a068
Linkage Isomeric Pentaamminecobalt(Iii) Complexes of Methanesulfinamide
Fairlie, DP, Jackson, WG and Thompson, KH (1990). Linkage Isomeric Pentaamminecobalt(Iii) Complexes of Methanesulfinamide. Inorganic Chemistry, 29 (17), 3145-3150. doi: 10.1021/ic00342a018
Fairlie, DP and Jackson, WG (1990). Nitrogen-Bonded and Oxygen-Bonded Urethane - Hydrolysis and Linkage Isomerization of [(Nh3)5Conh2Co2C2H5]3+ and [(Nh3)5Cooc(Nh2)Och2Ch3]3+. Inorganic Chemistry, 29 (17), 3139-3145. doi: 10.1021/ic00342a017
Homogeneous Catalysis - Catalytic Intramolecular Conversion of 1,4-Dialdehydes to Gamma-Lactones
Bergens, SH, Fairlie, DP and Bosnich, B (1990). Homogeneous Catalysis - Catalytic Intramolecular Conversion of 1,4-Dialdehydes to Gamma-Lactones. Organometallics, 9 (3), 566-571. doi: 10.1021/om00117a006
Amination of Coordinated Nitriles - Synthesis of Metal-Complexes of Amidines and Guanidines
Fairlie, DP and Jackson, WG (1990). Amination of Coordinated Nitriles - Synthesis of Metal-Complexes of Amidines and Guanidines. Inorganic Chemistry, 29 (1), 140-143. doi: 10.1021/ic00326a030
Angel, Robert L., Fairlie, David P. and Jackson, W. Gregory (1990). Linkage Isomerization of (Formamide-N)Pentaamminecobalt(Iii) and (Acetamide-N)Pentaamminecobalt(Iii) Ions in Water, Dimethyl-Sulfoxide, and Sulfolane. Inorganic Chemistry, 29 (1), 20-28. doi: 10.1021/ic00326a006
Fairlie, David P., Jackson, W. Gregory and McLaughlin, George M. (1989). Cobalt-Induced Facile Degradation of Phenylurea to Ammonia, Carbon-Dioxide, and Anilinium Ion and Other Reactions of Linkage Isomeric Cobalt(Iii) Complexes of Phenylurea. Inorganic Chemistry, 28 (10), 1983-1989. doi: 10.1021/ic00309a043
Fairlie D.P. and Jackson W.G. (1988). Reversible linkage isomerization of pentaamminecobalt(III) complexes of urea and its N-methyl derivatives. Inorganica Chimica Acta, 150 (1), 81-100. doi: 10.1016/S0020-1693(00)87628-8
Fairlie, David P. and Bosnich, B. (1988). Homogeneous Catalysis - Conversion of 4-Pentenals to Cyclopentanones by Efficient Rhodium-Catalyzed Hydroacylation. Organometallics, 7 (4), 936-945. doi: 10.1021/om00094a025
Fairlie, David P. and Bosnich, B. (1988). Homogeneous Catalysis - Mechanism of Catalytic Hydroacylation - the Conversion of 4-Pentenals to Cyclopentanones. Organometallics, 7 (4), 946-954. doi: 10.1021/om00094a026
Irritancy and anti-inflammatory activity of bis(η5-cyclopentadienyl)titanium(IV) complexes in rats
Fairlie D.P., Whitehouse M.W. and Broomhead J.A. (1987). Irritancy and anti-inflammatory activity of bis(η5-cyclopentadienyl)titanium(IV) complexes in rats. Chemico-Biological Interactions, 61 (3), 277-291. doi: 10.1016/0009-2797(87)90007-X
Synthesis, characterization, and reactivity of the (eta-2-acetone)pentaammineosmium(II) complex
Harman, WD, Fairlie, DP and Taube, H (1986). Synthesis, characterization, and reactivity of the (eta-2-acetone)pentaammineosmium(II) complex. Journal of the American Chemical Society, 108 (26), 8223-8227. doi: 10.1021/ja00286a018
Fairlie, DP and Taube, H (1985). Linkage isomerization of (urea)pentaammineruthenium(III) and inter- vs. intramolecular substitution on ruthenium(III). Inorganic Chemistry, 24 (20), 3199-3206. doi: 10.1021/ic00214a023
Dixon, NE, Fairlie, DP, Jackson, WG and Sargeson, AM (1983). Base-catalyzed hydration of cobalt(III)-coordinated dimethylcyanamide and linkage isomerization of the derived N-bound dimethylurea complex. Inorganic Chemistry, 22 (26), 4038-4046. doi: 10.1021/ic00168a043
Oxygen- and sulfur-bonded thiosulfatopentaamminecobalt(III)
Jackson W.G., Fairlie D.P. and Randall M.L. (1983). Oxygen- and sulfur-bonded thiosulfatopentaamminecobalt(III). Inorganica Chimica Acta, 70, 197-205. doi: 10.1016/S0020-1693(00)82802-9
Lymphoid suppression by cis-platinum(II)amines. What are the active agents?
Fairlie D.P. and Whitehouse M.W. (1982). Lymphoid suppression by cis-platinum(II)amines. What are the active agents?. Biochemical Pharmacology, 31 (6), 933-939. doi: 10.1016/0006-2952(82)90323-9
Roos I.A., Fairlie D.P. and Whitehouse M.W. (1981). A peculiar toxicity manifested by platinum(II)amines in rats: gastric distension after intraperitoneal administration. Chemico-Biological Interactions, 35 (1), 111-117. doi: 10.1016/0009-2797(81)90066-1
Boreham, CJ, Broomhead, JA and Fairlie, DP (1981). A 195Pt and 15N N.M.R. study of the anticancer drug, cis-diammine-dichloroplatinum(II), and its hydrolysis and oligomerization products. Australian Journal of Chemistry, 34 (3), 659-664. doi: 10.1071/CH9810659
cis-Platinum(II) amines: toxicities and immunosuppressant/anti-arthritic activities
Fairlie, D. P. and Whitehouse, M. W. (1981). cis-Platinum(II) amines: toxicities and immunosuppressant/anti-arthritic activities. Agents and Actions Supplements, 8, 399-434.
Platinum drugs - combined anti-lymphoproliferative and nephrotoxicity assay in rats
Aggarwal, SK, Broomhead, JA, Fairlie, DP and Whitehouse, MW (1980). Platinum drugs - combined anti-lymphoproliferative and nephrotoxicity assay in rats. Cancer Chemotherapy and Pharmacology, 4 (4), 249-258. doi: 10.1007/BF00255269
Broomhead J.A., Fairlie D.P. and Whitehouse M.W. (1980). cis-Platinum(II) amine complexes: some structure-activity relationships for immunosuppressive, nephrotoxic and gastrointestinal (side) effects in rats. Chemico-Biological Interactions, 31 (1), 113-132. doi: 10.1016/0009-2797(80)90144-1
Heterocycles for switching GPCR ligand conformation and activity
Fairlie, David, Reid, Robert, Rowley, Jessica, Wu, Kai-Chen, Yau, Mei-Kwan, Lim, Junxian and Iyer, Abishek (2019). Heterocycles for switching GPCR ligand conformation and activity. National Meeting of the American Chemical Society (ACS), Orlando, FL United States, 31 March-4 April 2019. Washington, DC United States: American Chemical Society.
Wang, H., Kjer-Nielsen, L., Shi, M., Souza, D. C., Pediongco, T., Cao, H., Kostenko, L., Lim, X., Eckle, S., Meeha, B., Wang, B., Zhu, T., Mak, J., Fairlie, D., Teng, M., Rossjohn, J., Yu, D., Groth, B., McCluskey, J., Strugnell, R., Corbett, A. and Chen, Z. (2019). IL-23 co-stimulation drives antigen-specific MAIT cell activation and enables vaccination against bacterial infection. 17th International Congress of Immunology (IUIS), Beijing, China, 19-23 October, 2019. Weinheim, Germany: WILEY. doi: 10.1002/eji.201970400
PAR-2 does not contribute to tubular damage or renal fibrosis in the obstructed kidney
Han, Y., Ma, F., Ozols, E., Chew, P., Vesey, D., Gobe, G., Morais, C., Lohman, R., Suen, J., Fairlie, D. and Nikolic-Paterson, D. (2018). PAR-2 does not contribute to tubular damage or renal fibrosis in the obstructed kidney. 54th Annual Scientific Meeting of the Australian and New Zealand Society of Nephrology (ANZSN), Sydney, Australia, 8–12 September 2018. Richmond, VIC, Australia: Wiley-Blackwell. doi: 10.1111/nep.13441
Ramnath, D., Irvine, K., Lukowski, S., Horsfall, L., Loh, K., Clouston, A., Patel, P., Iyer, A., Lampe, G., Stow, J., Schroder, K., Fairlie, D., Powell, J., Powell, E. and Sweet, M. (2018). RNA-sequencing analysis of biopsies from chronic liver disease patients identifies gene signatures associated with progressive liver disease. International Liver Congress (ILC), Paris, France, 11-15 April, 2018. Amsterdam, Netherlands: Elsevier BV. doi: 10.1016/S0168-8278(18)31040-7
Recipient mucosal-associated invariant T cells control graft-versus-host-disease within the colon
Varelias, Antiopi, Bunting, Mark, Ormerod, Kate, Koyama, Motoko, Olver, Stuart, Straube, Jasmin, Kuns, Rachel, Robb, Renee, Henden, Andrea, Cooper, Leanne, Lachner, Nancy, Gartlan, Kate, Lantz, Olivier J., Kjer-Nielsen, Lars, Mak, Jeffrey, Fairlie, David, Clouston, Andrew, McCluskey, James, Rossjohn, Jamie, Lane, Steven, Hugenholtz, Phil and Hill, Geoff (2018). Recipient mucosal-associated invariant T cells control graft-versus-host-disease within the colon. Immunology Meeting, Austin Tx, 4-8 May 2018. Bethesda, MD United States: American Association of Immunologists.
Stoermer, Martin J., Wickramasinghe, Wasantha A., Byriel, Karl A., Hockless, David C. R., Skelton, Brian W., Sobolev, Alexandre N., White, Alan H., Mak, Jeffrey Y. W. and Fairlie, David P. (2018). Stereoelectronic effects on dienophile separation influence the Diels–Alder synthesis of molecular clefts. 2018 Royal Society of Chemistry Twitter Conference, London, United Kingdom (held online), 6-7 March 2018. London, United Kingdom: Royal Society of Chemistry.
Activity of the histone deacetylase (HDAC) inhibitor AR-42 in a murine malaria model
Chua, Ming Jang, Do, Darren, Bachu, Prabhakar, Reid, Robert, Fairlie, David, Skinner-Adams, Tina and Andrews, Kathy (2017). Activity of the histone deacetylase (HDAC) inhibitor AR-42 in a murine malaria model. 66th Annual Meeting of the American Society of Tropical Medicine and Hygiene (ASTMH), Baltimore, MD United States, 5-09 November 2017. Deerfield, IL United States: American Society of Tropical Medicine and Hygiene.
Mucosal-associated invariant T cells are an important source of TNF in rheumatoid arthritis
Jansen, Diahann, Klinken, Elizabeth, Nel, Hendrik, Law, Soi Cheng, Koppejan, Hester, Hameetman, Marjolijn, Liu, Ligong, Corbett, Alexandra, Eckle, Sidonia, Fairlie, David, Toes, Rene E. M., van Gaalen, Floris, Rossjohn, Jamie, McCluskey, James and Thomas, Ranjeny (2017). Mucosal-associated invariant T cells are an important source of TNF in rheumatoid arthritis. 2017 ACR/ARHP Annual Meeting, San Diego, California, 3-8 November 2017. Hoboken, NJ, United States: John Wiley & Sons.
Vitamin B2 related molecules that activate T cells
Mak, Jeffrey, Xu, Weijun, Reid, Robert, Corbett, Alexandra, Meehan, Bronwyn, Wang, Huimeng, Chen, Zhenjun, Rossjohn, Jamie, McCluskey, James, Liu, Ligong and Fairlie, David (2017). Vitamin B2 related molecules that activate T cells. 254th National Meeting and Exposition of the American-Chemical-Society (ACS) on Chemistry's Impact on the Global Economy, Washington DC, USA, 20-24 August 2017. Washington DC, USA: American Chemical Society.
Jansen, Diahann, Klinken, Elizabeth, Nel, Hendrik, Law, Soi Cheng, Benham, Helen, Cummins, Lisa, Brown, Matthew, Kenna, Tony, Liu, Ligong, Fairlie, David, Rossjohn, Jamie, Morrison, Mark, Thomas, Ranjeny, Cuiv, Paraic O., McCluskey, James and Corbett, Alexandra (2016). Heightened MAIT Cell Sensitivity to MR1 Ligands Could Impact Control of Dysbiosis in Patients with Rheumatoid Arthritis and Ankylosing Spondylitis. 2016 ACR/ARHP Annual Meeting, Washington, DC, United States, 11-16 November 2016. Hoboken, NJ, United States: John Wiley & Sons. doi: 10.1002/art.39977
T cell activation by pyrimidine derivatives
Fairlie, David, Liu, Ligong, Mak, Jeffrey and Xu, Weijun (2016). T cell activation by pyrimidine derivatives. WASHINGTON: AMER CHEMICAL SOC.
Das Gupta, K., Shakespear, M., Tunny, K., Hohenhaus, D., Bokil, J. N., Iyer, A., Fairlie, A. D. and Sweet, J. M. (2016). Histone deacetylase 7 (HDAC7) regulates a sub-set of TLR-mediated pro-inflammatory responses in macrophages by both deacetylase-dependent and -independent mechanisms. International Congress of Immunology (ICI), Melbourne, Australia, 21-26 August 2016. Hoboken, NJ, United States: Wiley-Blackwell.
A broad family of MR1-restricted T cells
Gherardin, N. A., Keller, A. N., Woolley, R. E., Le Nours, J., Ritchie, D. S., Neeson, P. J., Birkinshaw, R. W., Eckle, S. B., Waddington, J. N., Liu, L., Fairlie, D. P., McCluskey, J., Pellicci, D. G., Uldrich, A. P., Rossjohn, J. and Godfrey, D., I (2016). A broad family of MR1-restricted T cells. International Congress of Immunology (ICI), Melbourne Australia, 21-26 August 2016. Germany: Wiley.
Common drugs modulate mucosal-associated invariant T cell function
Keller, A. N., Eckle, S. B. G., Xu, W., Liu, L., Hughes, V. A., Mak, J., Meehan, B., Pediongco, T., Birkinshaw, R. W., Chen, Z., Wang, H., Souza, C., Kostenko, L., Corbett, A. J., Purcell, A. W., Fairlie, D. P., McCluskey, J. and Rossjohn, J. (2016). Common drugs modulate mucosal-associated invariant T cell function. International Congress of Immunology (ICI), Melbourne, VIC, Australia, 21-26 August 2016. Germany: Wiley. doi: 10.1002/eji.201670200
Drugs/drug analogues modulate MAIT cell function in an MR1-dependent manner
Eckle, S. B. G., Keller, A. N., Xu, W., Meehan, B., Pediongco, T., Liu, L., Hughes, V. A., Mak, J. Y. W., Birkinshaw, R. W., Chen, Z., Wang, H., D'Souza, C., Kostenko, L., Corbett, A. J., Purcell, A. W., Fairlie, D. P., Rossjohn, J. and McCluskey, J. (2016). Drugs/drug analogues modulate MAIT cell function in an MR1-dependent manner. International Congress of Immunology (ICI), Melbourne, VIC, Australia, 21-26 August 2016. Weinheim, Germany: Wiley - VCH. doi: 10.1002/eji.201670200
McCluskey, J., Corbett, A. J., Eckle, S. B. G., Chen, Z., Wang, H., Sun, S., D'Souza, C., Kostenko, L., Reantragoon, R., Meehan, B., Birkinshaw, R. W., Liu, L., Patel, O., Mahony, J., Cao, H., Jackson, D., Williamson, N. A., Strugnell, R. A., Mak, J. Y. W., Van Sinderen, D., Fairlie, D. P., Kjer-Nielsen, L., Godfrey, D., I and Rossjohn, J. (2016). MAIT cells: Friend or Foe in recognising microbial vitamin metabolites presented by the MHC-I-related molecule MR1. International Congress of Immunology (ICI), Melbourne, Australia, August 21-26, 2016. Weinheim, Germany: Wiley. doi: 10.1002/eji.201670200
MR1 is an endoplasmic reticulum-resident sensor of vitamin B metabolites
McWilliam, H., Eckle, S., Theodossis, A., Liu, L., Chen, Z., Fairlie, D., Strugnell, R., Mintern, J., McCluskey, J., Rossjohn, J. and Villadangos, J. (2016). MR1 is an endoplasmic reticulum-resident sensor of vitamin B metabolites. International Congress of Immunology (ICI), Melbourne, Australia, 21-26 August 2016 . Weinheim, Germany: Wiley.
Tesch, G., Han, Y., Vesey, D., Gobe, G., Lohman, R., Suen, J., Fairlie, D. and Nikolic-Paterson, D. (2016). Pharmacological Inhibition of Protease-Activated Receptor 2 (Par2) Reduces Crescent Formation in Rat Anti-Gbm Disease. 15th Asian Pacific Congress of Nephrology (APCN) and 52nd ANZSN ASM, Perth, WA, Australia, 17–21 September 2016. Richmond, VIC, Australia: Wiley-Blackwell Publishing Asia. doi: 10.1111/nep.12887
Owens, E., Iyer, A., Morais, C., Lohman, R., Suen, J., Johnson, D., Nikolic-Paterson, D., Gobe, G., Fairlie, D. and Vesey, D. (2016). Protease activated-receptor-2 induced inflammation and fibrosis is mediated in part through activation of transforming growth factor-beta signalling. The 15th Asian Pacific Congress of Nephrology (APCN) and 52nd ANZSN ASM, Perth Western Australia, 17–21 September 2016. Richmond, VIC, Australia: Wiley-Blackwell Publishing Asia. doi: 10.1111/nep.12887
Thymic precursors to the mucosal-associated invariant T cell lineage
Godfrey, D., Koay, H. -F, Gherardin, N., Enders, A., Loh, L., Chen, Z., Corbett, A., Eckle, S., Meehan, B., d'Udekem, Y., Konstantinov, I, Lappas, M., Liu, L., Goodnow, C., Fairlie, D., Rossjohn, J., Kedzierska, K., Berzins, S., McCluskey, J., Uldrich, A. and Pellicci, D. (2016). Thymic precursors to the mucosal-associated invariant T cell lineage. International Congress of Immunology (ICI), Melbourne Australia, 21-26 August 2016. HOBOKEN: WILEY-BLACKWELL.
T cell activation by transitory neo-antigens derived from distinct microbial pathways
Birkinshaw, Richard W., Corbetta, Alexandra J., Eckle, Sidonia B. G., Liu, Ligong, Patel, Onisha, Mahony, Jennifer, Chen, Zhenjun, Reantragoon, Rangsima, Meehan, Bronwyn, Cao, Hanwei, Williamson, Nicholas A., Strugnell, Richard A., Van Sinderen, Douwe, Mak, Jeffrey Y. W., Fairlie, David P., Kjer-Nielsen, Lars, Rossjohn, Jamie and McCluskey, James (2015). T cell activation by transitory neo-antigens derived from distinct microbial pathways. 8th International Workshop on Antigen Processing and Presentation, Philadelphia Pa, Jun 10-13, 2014. OXFORD: PERGAMON-ELSEVIER SCIENCE LTD.
Potent small agonists of protease activated receptor 2
Yau, Mei Kwan, Suen, Jacky, Xu, Weijun, Lim, Junxian, Liu, Ligong, Adams, Mark, He, Yaowu, Hooper, John, Reid, Robert and Fairlie, David (2015). Potent small agonists of protease activated receptor 2. WASHINGTON: AMER CHEMICAL SOC.
T-cell antigen formed from distinct metabolic pathways
Mak, Jeffrey, Corbett, Alexandra, Eckle, Sidonia, Birkinshaw, Richard, Liu, Ligong, Patel, Onisha, Mahony, Jennifer, Chen, Zhenjun, Reantragoon, Rangsima, Meehan, Bronwyn, Cao, Hanwei, Williamson, Nicholas, Strugnell, Richard, Van Sinderen, Douwe, Fairlie, David, Kjer-Nielsen, Lars, Rossjohn, Jamie and McCluskey, James (2015). T-cell antigen formed from distinct metabolic pathways. WASHINGTON: AMER CHEMICAL SOC.
Antigen-specific MAIT cell subsets involved in TB immunity
Sakala, Isaac, Kjer-Nielsen, Lars, Eickhoff, Christopher, Wang, Xiaoli, Blazevic, Azra, Liu, Ligong, Fairlie, David, Rossjohn, Jamie, McCluskey, James, Fremont, Daved, Hansen, Ted and Hoft, Daniel (2015). Antigen-specific MAIT cell subsets involved in TB immunity. Annual Meeting of the American-Association-of-Immunologists (IMMUNOLOGY), New Orleans La, May 08-12, 2015. BETHESDA: AMER ASSOC IMMUNOLOGISTS.
Cyclic penta- and hexa leucine peptides without N-methylation are orally absorbed
Kok, Woan Mei, Hill, Timothy A., Lohman, Rink-Jan, Hoang, Huy N., Nielsen, Daniel S., Scully, Conor G., Schroeder, Christina I., Colless, Barbara, Bernhardt, Paul V., Edmonds, David, Griffith, David, Rotter, Charles, Ruggeri, Roger, Price, David, Liras, Spiros, Craik, David and Fairlie, David (2015). Cyclic penta- and hexa leucine peptides without N-methylation are orally absorbed. American Chemical Society Meeting, x, 2015. Washington, DC United States: American Chemical Society.
Downsizing Proteins Without Losing Potency or Function
Fairlie, David P. , Yau, Mei-Kwan , Hamidon, Johan K. , Singh, Ranee , Lim, Junxian , Suen, Jacky Y. , Rowley, Jessica A. , Lohman, Rink-Jan , Stoermer, Martin J. , Iyer, Abishek and Reid, Robert C. (2015). Downsizing Proteins Without Losing Potency or Function. American Peptide Symposium 2015, Orlando , Florida, United States, 20-25 June 2015. American Peptide Society. doi: 10.17952/24APS.2015.016
Targeting Host Complement C3a/C5a Receptors to Control of Acute Graft-Versus-Host Disease in Mice
Hung Nguyen, Heinrichs, Jessica Lauren, Fu, Jianing, Wu, Yongxia, Bastian, David, Schutt, Steven, Daenthanasanmak, Anusara, Dany, Mohammmed, Liu, Chen, Fairlie, David, Tomlinson, Stephen and Yu, Xue-Zhong (2015). Targeting Host Complement C3a/C5a Receptors to Control of Acute Graft-Versus-Host Disease in Mice. 57th Annual Meeting of the American-Society-of-Hematology, Orlando, FL, United States, 5-8 December 2015. Washington, DC, United States: American Society of Hematology.
Tetramer identification of functional mouse mucosal associated invariant T (MAIT) cells
Sakala, Isaac G., Kjer-Nielsen, Lars, Eickhoff, Christopher S., Wang, Xiaoli, Liu, Ligong, Fairlie, David P., Rossjohn, Jamie, McCluskey, James, Hoft, Daniel F. and Hansen, Ted H. (2015). Tetramer identification of functional mouse mucosal associated invariant T (MAIT) cells. 8th International Workshop on Antigen Processing and Presentation, Philadelphia Pa, Jun 10-13, 2014. Oxford United Kingdom: Pergamon Press.
Tetramer identification of functional mouse mucosal associated invariant T cells
Sakala, Isaac, Kjer-Nielsen, Lars, Eickhoff, Christopher, Wang, Xiaoli, Liu, Ligong, Fairlie, David, Rossjohn, Jamie, Hoft, Daniel and Hansen, Ted (2014). Tetramer identification of functional mouse mucosal associated invariant T cells. BETHESDA: AMER ASSOC IMMUNOLOGISTS.
Walden, Patricia M., Halili, Maria A., Archbold, Julia K., Lindahl, Fredrik, Fairlie, David P., Inaba, Kenji and Martin, Jennifer L. (2014). Characterization of the alpha-proteobacteria Wolbachia pipientis protein disulphide machinery reveals a regulatory mechanism absent in gamma-proteobacteria. 28th Annual Symposium of the Protein-Society, San Diego, California, 27-30 July 2014. Hoboken, NJ, United States : Wiley-Blackwell.
Novel inhibitors of DENV NS2B/NS3pro protease
Chow, Shiao Yun, Stoermer, Martin J., Chappell, Keith J., Young, Paul R. and Fairlie, David P. (2013). Novel inhibitors of DENV NS2B/NS3pro protease. 246th National Meeting of the American-Chemical-Society (ACS), Indianapolis in, Sep 08-12, 2013. WASHINGTON: AMER CHEMICAL SOC.
How MAIT cells control the growth of intracellular mycobacteria
Sakala, Isaac, Yankelevich, Wei-Jen, Kjer-Nielsen, Lars, Fairlie, David, Rossjohn, Jamie, McCluskey, James, Hoft, Daniel and Hansen, Ted (2013). How MAIT cells control the growth of intracellular mycobacteria. 100th Annual Meeting of the American Association of Immunologists, Honolulu Hi United States, May 03-07, 2013. Bethesda, MD United States: American Association of Immunologists.
Targeting Histone Deacetylase 1 (Hdac 1) to Suppress Both Inflammation and Bone Loss in Arthritis
Cantley, M., Fairlie, D., Bartold, M., Marino, V, Gupta, P. and Haynes, D. (2013). Targeting Histone Deacetylase 1 (Hdac 1) to Suppress Both Inflammation and Bone Loss in Arthritis. 54th Annual Scientific Meeting of the Australian Rheumatology Association in conjunction with the Rheumatology Health Professionals Association, Perth, WA Australia, 18 -22 May 2013. Richmond, VIC Australia: Wiley-Blackwell Publishing Asia. doi: 10.1111/imj.12139
Barbero, Sheila, Reid, Robert C., Stoermer, Martin J., Lohman, Rink J. and Fairlie, David P. (2013). Toward more orally bioavailable inhibitors of phospholipase A(2) GIIA (pla2g2a) to treat chronic inflammation. 246th National Meeting of the American-Chemical-Society (ACS), Indianapolis, IN, United States, 8-12 September 2013. Washington, DC, United States: American Chemical Society.
Concise synthesis of the thiazole-thiazoline fragment of largazole
Diness, Frederik, Nielsen, Daniel S. and Fairlie, David P. (2012). Concise synthesis of the thiazole-thiazoline fragment of largazole. 243rd National Spring Meeting of the American-Chemical-Society, San Diego Ca, Mar 25-29, 2012. WASHINGTON: AMER CHEMICAL SOC.
Fluorobenzene derivatives as multifunctional tools
Diness, Frederik, Begtrup, Mikael Begtrup and Fairlie, David P. (2012). Fluorobenzene derivatives as multifunctional tools. 243rd National Spring Meeting of the American-Chemical-Society, San Diego Ca, Mar 25-29, 2012. WASHINGTON: AMER CHEMICAL SOC.
Ligand-induced dimerisation of the complement C5aR and C5L2 receptors by C5a but not C5a-des Arg
Croker, Daniel E., Halai, Reena, Fairlie, David P. and Cooper, Matthew A. (2012). Ligand-induced dimerisation of the complement C5aR and C5L2 receptors by C5a but not C5a-des Arg. XXIV International Complement Workshop (ICW), Crete, Greece, 10-15 October 2012. Jena, Germany: Urban und Fischer Verlag. doi: 10.1016/j.imbio.2012.08.152
Shedding light on MHC class I antigen loading: A UV-labile peptide ligand approach
Theodossis, Alex, Ruiz-Gomez, Gloria, Gibb, Andrew, Welland, Andrew, Jones, Paul, Fairlie, David and Rossjohn, Jamie (2012). Shedding light on MHC class I antigen loading: A UV-labile peptide ligand approach. 7th International EMBO Workshop on Antigen Presentation and Processing, Amsterdam, Netherlands, 24-27 April 2012. Oxford, United Kingdom: Pergamon. doi: 10.1016/j.molimm.2012.02.094
Shedding light on MHC class I antigen loading: a UV-labile peptide ligand approach
Theodossis, A., Ruiz-Gomez, G., Gibb, A., Welland, A., Jones, P., Fairlie, D. and Rossjohn, J. (2012). Shedding light on MHC class I antigen loading: a UV-labile peptide ligand approach. 32nd European Peptide Symposium "Peptides 2012", Athens, Greece, 02-07 September 2012. West Sussex, United Kingdom: John Wiley and Sons. doi: 10.1002/psc.2447
Cantley, M. D., Fairlie, D. P., Bartold, P., Marino, V. and Haynes, D. R. (2011). Inhibiting Histone Deacetylases Expressed in Human Periodontal Tissues Prevents Bone Loss in An Animal Model of Periodontal Disease. IOF Regionals 2nd Asia-Pacific Osteoporosis and Bone Meeting / ANZBMS Annual Scientific Meeting held with the JSBMR, Gold Coast Australia, Sep 04-08, 2011. LONDON: SPRINGER LONDON LTD.
Novel agonists and antagonists for protease activated receptor 2
Yau, Annika M., Liu, Ligong, Reid, Robert C., Barry, Grant D., Suen, Jacky Y., Lohman, Rink-Jan, Le, Giang T., Cotterell, Adam and Fairlie, David P. (2011). Novel agonists and antagonists for protease activated receptor 2. National Meeting of the American Chemical Society (242nd, ACS, 2011), Denver, CO, U.S.A., 28 August-1 September 2011. WASHINGTON: AMER CHEMICAL SOC.
Towards orally bioavailable peptides and peptidomimetics
Fairlie, David P., Stoermer, Martin, Lucke, Andrew, Lohman, Rink-Jan, Liu, Ligong and Ruiz-Gomez, Gloria (2011). Towards orally bioavailable peptides and peptidomimetics. 241st National Meeting and Exposition of the American-Chemical-Society (ACS), Anaheim, CA, United States, 27-31 March 2011. Washington, DC, United States: American Chemical Society.
Modelling of the C5a receptor by iterative mutation
Holt, J. R., Monk, P. N., Fairlie, D. P. and Madala, P. Kumar (2010). Modelling of the C5a receptor by iterative mutation. 23rd International National Complement Workshop, New York Ny, Aug 01-05, 2010. OXFORD: PERGAMON-ELSEVIER SCIENCE LTD. doi: 10.1016/j.molimm.2010.05.061
Vesey David A., Suen, Jacky Yung, Johnson, David W. and Fairlie, David (2010). A Novel Protease-Activated Receptor-2 Antagonist Targeting Inflammation and Proliferation in Human Renal Tubular Epithelial Cells. Kidney Week, American society of Nephrology, Denver Colorado USA, November 16 - 21. Journal of the American Society of Nephrology:
Potent inhibitors of West Nile Virus NS2B/NS3 protease
Chappell, K. J., Fairlie, D. P., Gan, C. H., Gupta, P. K., Hu, S., Jensen, C. M., Liebscher, S., Martin, J. L., Robin, G., Stoermer M. J., Xu, W. and Young, P. R. (2010). Potent inhibitors of West Nile Virus NS2B/NS3 protease. 6th General Meeting of the International Proteolysis Society, Gold Coast, QLD, Australia, 26-30 October 2009. Berlin, Germany: Walter De Gruyter.
Protease-activated receptor-2 and renal carcinogenesis
Vesey, D., Rajandram, R., Blakeney, J., Suen, J., Johnson, D., Fairlie, D. and Gobe, G. (2010). Protease-activated receptor-2 and renal carcinogenesis. 46th Annual Scientific Meeting of the Australian and New Zealand Society of Nephrology, Perth Convention and Exhibition Centre, Perth, Western Australia, 12-15 September 2010. Richmond, Vic., Australia: Wiley-Blackwell Publishing Asia. doi: 10.1111/j.1440-1797.2010.01377_1.x
Liebscher, Susan, Chappell, K. J., Stoermer, Martin J., Watterson, Daniel, Webb, Richard I., Khromykh, Alexander A., Fairlie, David P. and Young, Paul R. (2010). Sneaking up on West Nile Virus NS2B/NS3 protease subcellular activity utilising dye-quenched substrates. PlusStrand 2010: The Ninth International Symposium on Positive-Strand RNA Viruses, Atlanta, GA, U.S.A., 17-21 May 2010.
Cantley, M. D., Fairlie, D. P., Bartold, M. P., Rainsford, K. D. and Haynes, D. R. (2009). Inhibition of both class I and class II histone deacetylases is required to effectively inhibit osteoclast bone resorption in vivo and in vitro. 2nd Joint Meeting of the International-Bone-and-Mineral-Society/Australian-New-Zealand-Bone-and-Mineral-Society, Sydney Australia, Mar 21-25, 2009. NEW YORK: ELSEVIER SCIENCE INC. doi: 10.1016/j.bone.2009.01.292
Liebscher, S., Chappell, K.J., Stoermer, M.J., Fairlie, D.P. and Young, P.R (2009). Antiviral activity in cell culture of potent inhibitors targeting the West Nile Virus NS2B/NS3 protease. 6th General Meeting of the International Proteolysis Society, Gold Coast , QLD, Australia, 26-30 October, 2009.
Regulating protein and peptide activated GPCRs
Fairlie, David P., Madala, Praveen K., Stoermer, Martin J., Suen, Jacky, Barry, Grant and Lohman, Rink-Jan (2009). Regulating protein and peptide activated GPCRs. 229th National Meeting of the American Chemical Society, San Diego, California, 13-17 March 2005. Washington DC, United States: American Chemical Society.
Madala, P. K., Stoermer, M., Tyndall, J. D. A., Monk, P. N., Higginbottom, A. and Fairlie, D. P. (2008). COMP 264-Unraveling the mechanism of antagonism for human C5a receptor: Comparison of three structurally different antagonists. 236th National Meeting of the American Chemical Society, Philadelphia, USA, 17-21 August, 2008. Washington, D. C., USA: American Chemical Society.
MEDI 256-Activation and inhibition of latent serine proteases, complement factors B and C2
Fairlie, DP, Le, GT, Halili, M, Ruiz-Gomez, G and Abbenante, J (2008). MEDI 256-Activation and inhibition of latent serine proteases, complement factors B and C2. 236th National Meeting of the American Chemical Society, Philadelphia PA, 17-21 August 2008. Atlanta, GA, USA: The American Chemical Society.
Andrews, Kathy T., Tran, Thanh N., Lucke, Andrew, Kahnberg, Pia, Lee, G. T., Skinner-Adams, Tina, Gardiner, Donald L. and Fairlie, David P. (2007). Plasmodium falciparum histone deacetylases: Enzymes involved in gene regulation as new antimalarial drug targets. 56th Annual Meeting of the American-Society-of-Tropical-Medicine-and-Hygiene, Philadelphia, PA United States, 04-08 November 2007. Deerfield, IL United States: American Society of Tropical Medicine and Hygiene.
Rice, Charles, Heinz, Franz X., Kuhn, Richard, Harris, Eva, Fairlie, David, Young, Paul, Flamand, Marie, Zinkernagel, Rolf, Halstead, Scott, Evans, Thomas G., Jans, David A. and Screaton, Gavin (2006). Discussion.
Rice, Charles, Padmanabhan, R. Pad, Canard, Bruno, Vasudevan, Subhash, Satchidanandam, Vijaya, Fairlie, David, Gamarnik, Andrea and Kuhn, Richard (2006). Discussion.
Fairlie, David, Gubler, Duane J., Holmes, Edward, Halstead, Scott, Hombach, Joachim, Harris, Eva, Hibberd, Martin, Vasudevan, Subhash, Evans, Thomas G., Keller, Thomas, Gu, Feng, Stephenson, John, Canard, Bruno, Malasit, Prida and Zinkernagel, Rolf (2006). Discussion.
Rice, Charles, Hibberd, Martin, Gu, Feng, Harris, Eva, Jans, David A., Farrar, Jeremy, Vasudevan, Subhash, Evans, Thomas G., Holmes, Edward, Fairlie, David and Keller, Thomas (2006). Discussion. Novartis Foundation.
Young, Paul, Keller, Thomas, Padmanabhan, R. Pad, Fairlie, David, Hibberd, Martin, Rice, Charles, Canard, Bruno, Vasudevan, Subhash, Screaton, Gavin, Harris, Eva, Gu, Feng, Halstead, Scott, Farrar, Jeremy, Holmes, Edward, Malasit, Prida and Evans, Thomas G. (2006). Discussion. Novartis Foundation.
Harris, Eva, Screaton, Gavin, Farrar, Jeremy, Hombach, Joachim, Halstead, Scott, Rice, Charles, Holmes, Edward, Satchidanandam, Vijaya, Young, Paul, Zinkernagel, Rolf, Flamand, Marie, Malasit, Prida and Fairlie, David (2006). Discussion. Novartis Foundation.
Rice, Charles, Heinz, Franz X., Young, Paul, Kuhn, Richard, Neyts, Johan, Keller, Thomas, Fairlie, David, Guber, Duane J. and Screaton, Gavin (2006). General discussion I.
MEDI 180-Effects of cyclization constraints on helix/turn peptide structures
Beyer, Renee L., Hoang, Huy N., Le, Giang T. and Fairlie, David P. (2006). MEDI 180-Effects of cyclization constraints on helix/turn peptide structures. WASHINGTON: AMER CHEMICAL SOC.
MEDI 181-Alpha helix induction in HIV REV34-50 by N-terminal nucleators
Beyer, Renee L., Kelso, Michael J., Reid, Robert C., Le, Giang T. and Fairlie, David P. (2006). MEDI 181-Alpha helix induction in HIV REV34-50 by N-terminal nucleators. WASHINGTON: AMER CHEMICAL SOC.
Defining the ligand binding site on the human C5a receptor
Monk, Peter N., Higginbottom, Adrian, Madala, Praveen K., Tyndall, Joel D. A., Stoermer, Martin and Fairlie, David P. (2006). Defining the ligand binding site on the human C5a receptor. 231st National Meeting of the American-Chemical-Society, Atlanta Ga, Mar 26-30, 2006. WASHINGTON: AMER CHEMICAL SOC.
Alpha helix induction in HIV REV34-50 by N-terminal nucleators
Beyer, Renee L., Kelso, Michael J., Reid, Robert C., Le, Giang T. and Fairlie, David P. (2006). Alpha helix induction in HIV REV34-50 by N-terminal nucleators. 232nd ACS National Meeting, San Francisco, CA, U.S.A., 10-14 September, 2006. American Chemical Society. doi: 10.1021/cen-v084n034.p055
Defining the ligand binding site on the human C5a receptor
Monk, Peter N., Higginbottom, Adrian, Madala, Praveen K., Tyndall, Joel D. A., Stoermer, Martin and Fairlie, David P. (2006). Defining the ligand binding site on the human C5a receptor. The 231st ACS National Meeting, Atlanta, GA, U.S.A., 26-30 March 2006. Washington, D.C.: American Chemical Society.
Desai, A., Khlentzos, A., Shepherd, N., Hoang, H. N., Letouze, E., Fairlie, D. and Young, P. R. (2006). Developing antiviral targets for RSV via mutational analysis of HRB and HRC domains using a novel fusion assay system. 13th International Conference of Negative Strand Viruses, Salamanca, 17-22 June, 2006.
Ng Mah Lee, Mary, Rice, Charles, Fairlie, David, Zinkernagel, Rolf, Young, Paul, Neyts, Johan, Hibberd, Martin, Holmes, Edward, Heinz, Franz X. and Stephenson, John (2006). Final discussion. Novartis Foundation Symposium 277: New treatment strategies for Dengue and other flaviviral diseases, *, 2006. John Wiley & Sons.
Chappell, K. J., Stoermer, M J, Fairlie, D and Young, P R (2006). Investigation of the West Nile virus NS3 protease by tandem use of site-directed mutagenesis and substrate modification. Australian Society for Microbiology Annual Scientific Meeting, Gold Coast, Qld, 2-6 July, 2006.
Multiple targets for antiviral inhibitors
Young, P. R., Chappell, K. J., Stoermer, M. J., Fairlie, D., Kampmann, T. and Kobe, B. (2006). Multiple targets for antiviral inhibitors. 7th Asia Pacific Congress of Virology, New Delhi, 13-15 Nov, 2006.
New Treatment Strategies for Dengue and other Flaviviral Diseases
Fairlie, D. (2006). New Treatment Strategies for Dengue and other Flaviviral Diseases. Norvatis foundations Symposium 277 on New Treatment Strategies for Dengue and other Flaviviral Diseases, Singapore, 26-27 September, 2005. Chichester, UK: John Wiley and Sons.
Peptide bundles: Loops, helices, strands and sheets
Fairlie, D., Singh, Y. and Sharpe, P. C. (2006). Peptide bundles: Loops, helices, strands and sheets. The American Chemical Society Meeting 2006, Atlanta, GA, USA, 26 -30 March, 2006. Washington: American Chemical Society.
Alpha-helix induction in short peptides using metal clips
Ma, M. T., Hoang, H. N., Beyer, R. L., Bryant, G. K., Appleton, T. G. and Fairlie, D. (2005). Alpha-helix induction in short peptides using metal clips. International Chemical Congress of Pacific Basin Societies (Pacifichem2005), Honolulu, Hawaii, 15 - 20 December 2005. WASHINGTON: AMER CHEMICAL SOC.
Chappell, K. J., Stoermer, M. J., Fairlie, D. and Young, P. R. (2005). Development of a catalytically active recombinant West Nile NS3 protease and the identification of key enzyme-substrate interactions by site-directed mutagenesis. 30th Lorne Conference on Protein Structure & Function, Lorne, 6-10 Feb, 2005.
Chappell, K. J., Stoermer, M. J., Fairlie, D. and Young, P. R. (2005). Development of a catalytically active recombinant West Nile NS3 protease and the identification of key enzyme-substrate interactions by site-directed mutagenesis. International Congress of Virology, San Francisco, 23-27 July, 2005.
Chappell, K. J., Stoermer, M. J., Fairlie, D. and Young, P. R. (2005). Development of a catalytically active recombinant West Nile virus NS3 protease and the identification of key enzyme-substrate and enzyme-cofactor interactions by site-directed mutagenesis. 3rd Australian Virology Group Meeting, Phillip Island, Vic., 9-12 Dec, 2005.
Modular alpha-helices: conformationally stable cyclic pentapeptides as alpha-turn mimetics
Shepherd, Nicholas E., Hoang, Huy N., Abbenante, Giovanni and Fairlie, David P. (2005). Modular alpha-helices: conformationally stable cyclic pentapeptides as alpha-turn mimetics. 3rd International Peptide Symposium/28th European Peptide Symposium, Prague, Czech Republic, 5-10 September 2004. Geneva, Switzerland: Kenes INT.
Cardiovascular structural and functional adaptations to group IIAsPLA2 inhibition
Levick, S., Taylor, S. M., Fairlie, D. and Brown, L. C. (2004). Cardiovascular structural and functional adaptations to group IIAsPLA2 inhibition. 2004 ISHR World Congress, Brisbane, Australia, 7-11/8/04. London: Academic Press.
Small molecules that mimic components of bioactive protein surfaces
Fairlie, DP (2004). Small molecules that mimic components of bioactive protein surfaces. Australia: CSIRO Publishing. doi: 10.1071/CH04074
Towards Modular Alpha-Helices: Comformationally Stable Cyclic Pentapeptides as Alpha-Turn Mimetics
Shepherd, N. E., Hoang, H., Abbenante, G. and Fairlie, D. P. (2004). Towards Modular Alpha-Helices: Comformationally Stable Cyclic Pentapeptides as Alpha-Turn Mimetics. 3rd International Peptide Symposium/28th European Peptide Symposium, Prague Czech Republic, Sep 05-10, 2004. GENEVA 1: JOHN WILEY & SONS LTD.
Template-assembled peptide loops, helices, sheets and nanofibres
Fairlie, DP, Singh, Y, Sharpe, P and Stoermer, M (2003). Template-assembled peptide loops, helices, sheets and nanofibres. 225th National Meeting of the American-Chemical-Society, New Orleans Louisiana, Mar 23-27, 2003. WASHINGTON: AMER CHEMICAL SOC.
Helix inducing metal clips in short peptides
Beyer, R. L., Kelso, M. J., Hoang, H. N., Appleton, T. G. and Fairlie, D. (2003). Helix inducing metal clips in short peptides. Proceedings of the First International Symposium on Biomolecuy, Awaji, Japan, 2-5 December, 2003. Tokyo, Japan: Maruzen Co. Ltd..
Short peptide alpha helices induced by multiple metal clips
Hoang, Huy N., Bryant, Gavin K., Kelso, Micheal J., Beyer, Renee L., Appleton, Trevor G. and Fairlie, David P. (2003). Short peptide alpha helices induced by multiple metal clips. 11th International Conference on Biological Inorganic Chemistry, Cairns, Australia, 19-23 July 2003. New York, USA: Elsevier. doi: 10.1016/S0162-0134(03)80638-4
Short peptide alpha helices induced by multiple metal clips
Hoang, Huy N., Bryant, Gavin K., Kelso, Micheal J., Beyer, Renee L., Appleton, Trevor G. and Fairlie, David P. (2003). Short peptide alpha helices induced by multiple metal clips. 11th International Conference on Biological Inorganic Chemistry, Cairns, Australia, 19-23 July, 2003. New York, USA: Elsevier. doi: 10.1016/S0162-0134(03)80638-4
Gahan, Lawrence R., Cusack, Rodney M., Grondahl, Lisbeth H., Fairlie, David P. and Hanson, Graeme R. (2003). Studies of the interaction of potassium(I), calcium(II), magnesium(II) and copper(II) with cyclosporin A. 11th International Conference on Biological Inorganic Chemistry, New York, USA, 19-23July, 2003. New York, USA: Elseiver. doi: 10.1016/S0162-0134(03)80624-4
Template-assembled peptide loops, helices, sheets, and nanofibers
Fairlie, David P ., Singh, Yogendra, Sharpe, Philip and Stoermer, Martin (2003). Template-assembled peptide loops, helices, sheets, and nanofibers. 225th ACS National Meeting, New Orleans, LA, United States, 23-27 March 2003.
Palladium induced alpha helicity in short peptides.
Kelso, MJ, Hoang, HN, Appleton, TG and Fairlie, DP (2002). Palladium induced alpha helicity in short peptides.. WASHINGTON: AMER CHEMICAL SOC.
A new C5a receptor antagonist inhibits monoarticular arthritis in the rat
Woodruff, T. M., Shiels, I. A., Fairlie, D. and Taylor, S. M. (2001). A new C5a receptor antagonist inhibits monoarticular arthritis in the rat. Complement Assoc. Diseases, Animal Models & Ther. Workshop, Santorini, Greece, 10-14 October, 2001. Aegean Conferences.
Construction and characterization of the dengue 2 virus NS3 protease and its mutants
Fang, N., Arakaki, T., Fairlie, D., Martin, J. L. and Young, P. R. (2001). Construction and characterization of the dengue 2 virus NS3 protease and its mutants. 1st Australian Virology Group Meeting, Fraser Island, Qld, 5-9 December, 2001.
Control of peptide conformation by Palladium(II) coordination
Appleton, T. G., Fairlie, D., Hoang, H. N., Kelso, M., March, D. R. and Oliver, W. (2001). Control of peptide conformation by Palladium(II) coordination. 10th International Conf on Bioinorganic Chemistry, Florence, Italy, 26-31 August, 2001. NEW YORK: ELSEVIER SCIENCE INC.
In vitro catalytic activity of recombinant forms of the dengue virus NS3 protease
Young, P. R., Fang, N., Leung, D., Arakaki, T., Stoermer, M. J., Fairlie, D. and Martin, J. L. (2001). In vitro catalytic activity of recombinant forms of the dengue virus NS3 protease. 6th International Symposium on Positive Strand Viruses, Paris, France, 28 May - 2 June, 2001.
Metal clips for folding peptides
Appleton, T. G., Hoang, H. N., Fairlie, D., Kelso, M. and Bryant, G. K. (2001). Metal clips for folding peptides. World Chemistry Congress, Brisbane, 1-6 July, 2001.
Prevention of ischemia/reperfusion injuries in rats by a new small molecule C5a receptor antagonist
Arumugum, T.V., Shiels, I. A., Fairlie, D. and Taylor, S. M. (2001). Prevention of ischemia/reperfusion injuries in rats by a new small molecule C5a receptor antagonist. Complement Associated Diseases, Animal Models and Ther. W/shop, Santorini, Greece, 10-14 October 2001. Aegean Conferences.
Complement and inflammation: New antagonists of C5a receptors.
Fairlie, DP (2000). Complement and inflammation: New antagonists of C5a receptors.. WASHINGTON: AMER CHEMICAL SOC.
Coordination with Pd(en)2+ imposes an a-helical structure on a pentapeptide
Appleton, T. G., Hoang, H. N. and Fairlie, D. (2000). Coordination with Pd(en)2+ imposes an a-helical structure on a pentapeptide. Pacifichem 2000, Honolulu, Hawaii, 14-19 December, 2000. American Chemical Society.
Expression and characterization of a catalytically active form of the Dengue virus NS3 protease
Young, P. R., Fang, N., Leung, D., Arakaki, T., Fairlie, D. and Martin, J. L. (2000). Expression and characterization of a catalytically active form of the Dengue virus NS3 protease. 1st Int Conf on Dengue and Dengue Haemorrhagic Fever, Chiang Mai, Thailand, 20-24 Nov, 2000.
Metallopeptides in Alzheimer's Disease
Hanson, G. R., Bush, A. R. I., Fairlie, D. and Tyndall, J. (2000). Metallopeptides in Alzheimer's Disease. Brisbane Inorganic Chemistry Symposium, Dept of Chemistry, Uni of Queensland, 30 November 2000. Brisbane (UQ): Dept of Chemistry, UQ.
The reaction between metal ions and short peptides
Hoang, H. N., Appleton, T. G. and Fairlie, D. (2000). The reaction between metal ions and short peptides. IC2000/11RACIC, Canberra, 6-11 Feb, 2000.
Stoermer, Martin and Fairlie, David (2000). Towards Arginine Mimetics. The First Brisbane Biological and Organic Chemistry Symposium, Griifith University, Brisbane, Queensland, Australia, 27th November 2000. doi: 10.6084/m9.figshare.7836131
Cyclic peptides as metal ion receptors
Cusack, R., Grondahl, L., Abbenante, J., Fairlie, D., Gahan, L. R., Hambley, T. W. and Hanson, G. R. (1999). Cyclic peptides as metal ion receptors. IC'99, Wellington, NZ, 31 January - 4 February 1999. Wellington, NZ: NZ Institute of Chemistry.
Homology model of the dengue 2 virus NS3 protease: Interactions with NS2B co-factor
White, H., Young, P. R., Brinkworth, R. I., Fairlie, D. and Leung, D. D. (1999). Homology model of the dengue 2 virus NS3 protease: Interactions with NS2B co-factor. XIth International Congress of Virology, Sydney, 9-13 August 1999. Sydney: International Union of Microbiological Societies.
Modelling Studies Of Molecular Receptors
Chalmers, David K., Stoermer, Martin J. and Fairlie, David P. (1998). Modelling Studies Of Molecular Receptors. Royal Australian Chemical Institute 16th National Organic Chemistry Conference, Leura, Blue Mountains, New South Wales, 12-17 July 1998.
The selective binding of metal ions by tolyporphins
Appleton, T. G., Prinsep, M. R., Fairlie, D. P., Lane, I. and Hanson, G. R. (1997). The selective binding of metal ions by tolyporphins. XXXI ICCC: International Conference on Coordination Chemistry, Vancouver, BC, Canada, 18–23 August 1996. Triangle Park, NC, U.S.A.: IUPAC Secretariat.
Cyclic Peptides as Metal Ion Receptors
Cusack, R. M., Abernante, J., Gahan, L. R., Fairlie, D. P. and Hanson, G. R. (1996). Cyclic Peptides as Metal Ion Receptors. RACI Inorganic Division, IC '96, Townsville, Queensland, Australia, 30 June - 4 July, 1996.
Effects of conformational constraints in cyclic octapeptides of marine origin
Abbenante, G., Fairlie, D. P., Sokolenko, N., Gahan, L. R., Cusack, R., Hanson, G. R. and Pierens, G. K. (1996). Effects of conformational constraints in cyclic octapeptides of marine origin. 10th Brisbane Organic Chemistry Symposium, Brisbane, QLD, Australia, 29 November 1996.
Hanson, G. R., van den Brenk, A. L., Gahan, L. R., Fairlie, D. P. and Hawkins, C. J. (1996). Multifrequency EPR studies of the mono- and bi-nuclear copper(II) complexes formed with the marine cyclic octapeptides patellamide D and ascidiacyclamide. EPR-95: Electron Paramagnetic Resonance 1995 Satellite Workshop Meeting of the 12th International Society of Magnetic Resonance Conference (ISMAR'95), Sydney, NSW, Australia, 13-15 July 1995. Berlin, Germany: Springer Wien.
Multifrequency EPR spectra of Cu(II) and Ag(II) tolyporphins
Lane, I., Prinsep, M., Hanson, G. R., Appleton, T. G. and Fairlie, D. (1995). Multifrequency EPR spectra of Cu(II) and Ag(II) tolyporphins. ISMAR 95: Twelfth Conference of the International Society of Magnetic Resonance, Sydney, NSW, Australia, 16-21 July 1995. Philadelphia, PA, U.S.A.: International Society of Magnetic Resonance (ISMAR).
The selective binding of tolyporphins to metal ions
Appleton, T. G., Prinsep, M. R., Fairlie, D. P., Lane, I., Hanson, G. R. and Moore, R. E. (1995). The selective binding of tolyporphins to metal ions. 10th National Convention RACI: The Royal Australian Chemical Institute's 10th National Convention: Chemistry Serving Society, Adelaide, SA, Australia, 27 September-2 October 1995. Adelaide, SA, Australia: ICI Australia.
ALEWOOD, PF, BAILEY, AJ, BRINKWORTH, RI, FAIRLIE, D and JONES, A (1993). CHARACTERIZATION OF TNF-ALPHA-RELATED PEPTIDES BY HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY MASS-SPECTROMETRY AND HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY TANDEM MASS-SPECTROMETRY. 12Th International Symp On High-Performance Liquid Chromatography of Proteins, Peptides and Polynucleotides, Sydney Australia, Nov 29-Dec 02, 1992. AMSTERDAM: ELSEVIER SCIENCE BV. doi: 10.1016/S0021-9673(99)87020-4
Mohan, P, Wong, MF, Verma, S, Huang, PP, Brinkworth, RI and Fairlie, DP (1993). Symmetrical and Nonsymmetrical Nonpeptide Inhibitors of Hiv-1 Protease - Naphthalenesulfonic Acid-Derivatives. WASHINGTON: AMER CHEMICAL SOC.
Tautomerism in Amide Complexes
Fairlie, DP and Woon, TC (1992). Tautomerism in Amide Complexes. WASHINGTON: AMER CHEMICAL SOC.
Stoermer, M.J., Wickramasinghe, W., Weerasuria, K.D.V., Fairlie, D., Butler, D. and Warrener, R. (1992). Design and synthesis of new cavitands which are stereochemically rigid, hydrophobic and internally functionalised. Royal Australian Chemical Institute National Conference 1992, Monash University, Melbourne, Australia, 28 Sept - 2 October 1992.
Synthesis of cavitands as catalytic environments
Stoermer, Martin J. and Fairlie, David P. (1991). Synthesis of cavitands as catalytic environments. 12th National Conference of the Royal Australian Chemical Institute, Division of Organic Chemistry, University of Queensland, Australia, 1991.
Supplementary Data tables for: Orally absorbed cyclic peptides
Nielsen, Daniel S., Shepherd, Nicholas E., Xu, Weijun, Lucke, Andrew J., Stoermer, Martin J. and Fairlie, David P. (2019). Supplementary Data tables for: Orally absorbed cyclic peptides. The University of Queensland. (Dataset) doi: 10.14264/uql.2019.213
Iyer, Abishek, Humphries, Tyrone LR, Owens, Evan P, Zhao, Kong-Nan, Masci, Paul P, Gobe, Glenda C, Johnson, David W, Paterson, David Nikolic, Fairlie, David P and Vesey, David A (2019). Supplementary Figure S1. The University of Queensland. (Dataset) doi: 10.14264/uql.2019.810
Reactivity of commercially available Fmoc amino acids: supplementary information
Lindahl, Fredrik, Hoang, Huy Ngoc, Fairlie, David P. and Cooper, Matthew A. (2015). Reactivity of commercially available Fmoc amino acids: supplementary information. The Royal Society of Chemistry. (Dataset)
Compounds and inhibitors of phospholipases
Reid, Robert C., Clark, Christopher I., Hansford, Karl, Stoermer, Martin J., McGeary, Ross P., Fairlie, David P. and Schafer, Karl (2007). Compounds and inhibitors of phospholipases. US7253194.
Clark, C. I., Fairlie, D. P., Hansford, K., McGeary, R. P., Reid, R. C. and Stoermer, M. J. (2007). New amino acid derivatives useful for the treatment of inflammatory disease or condition e.g. rheumatic arthritis.
Compounds and inhibitors of phospholipases
Reid, Robert C., Clark, Christopher I., Hansford, Karl, Stoermer, Martin J., McGeary, Ross P., Fairlie, David P. and Schafer, Karl (2004). Compounds and inhibitors of phospholipases. US2004033995.
Taylor, Steve, Shiels, Ian Alexander and Fairlie, David (2003). New cyclic peptide or peptidomimetic compounds, are G-protein coupled receptor antagonists useful for treating inflammatory disorders such as rheumatoid arthritis, reperfusion injury or dermal inflammation. WO/2003/033528.
Compounds and inhibitors of phospholipases
Reid, Robert C., Clark, Christopher I., Hansford, Karl, Stoermer, Martin J., McGeary, Ross P. and Fairlie, David P. (2002). Compounds and inhibitors of phospholipases. WO0208189.
Cyclic agonists and antagonists of c5a receptors and g protein-coupled receptors
Fairlie, David, Taylor, Stephen Maxwell, Finch, Angela Monique and Wong, Allan (1999). Cyclic agonists and antagonists of c5a receptors and g protein-coupled receptors. WO/1999/000406.
Developing a new type of drug for inflammatory lung disease
(2023–2025) NHMRC Development Grant
Modulating protein-protein interactions in disease
(2022–2026) NHMRC Investigator Grants
Targeting CEP55 in triple-negative breast cancer
(2022–2025) United States Congressionally Directed Medical Research Programs - Breast Cancer Research Program
ARC Centre of Excellence for Innovations in Peptide and Protein Science
(2021–2028) ARC Centres of Excellence
Advanced Nuclear Magnetic Resonance Technologies for Southeast Queensland
(2021–2023) ARC Linkage Infrastructure, Equipment and Facilities
(2019) UQ Major Equipment and Infrastructure
In vivo imaging system for tracking inflammation, infection, cancer, pain and bioactive molecules
(2019) UQ Major Equipment and Infrastructure
Preclinical Validation of a Novel Drug Lead to Treat Tuberculosis
(2018–2023) United States Congressionally Directed Medical Research Programs - Peer Reviewed Medical Research Program
A New Approach To Restoring Glucose Homeostasis
(2018–2022) NHMRC Project Grant
Compressing small peptides for cell absorption
(2018–2020) ARC Discovery Projects
Potent Small Molecule Modulators of a Complement Protein In Inflammation
(2018–2020) NHMRC Project Grant
(2018) UQ Major Equipment and Infrastructure
ACRF Cancer Ultrastructure and Function Facility
(2017–2024) Australian Cancer Research Foundation
Drug targets for liver inflammation and fibrosis
(2017–2022) UniQuest Pty Ltd
Modulating Protein-Protein Interactions In Disease
(2017–2021) NHMRC Research Fellowship
(2017–2020) Monash University
New chemicals for sheep blowfly control
(2017–2020) UniQuest Pty Ltd
Combating infectious diseases by harnessing macrophage functions
(2017–2019) NHMRC Project Grant
Small molecule activators of glucagon-like peptide receptor
(2017–2019) NHMRC Project Grant
Determine the therapeutic efficacy of CSL's drug candidate
(2017–2018) UniQuest Pty Ltd
Characterisation of PAR2 compounds
(2016–2018) UniQuest Pty Ltd
DsbA inhibitors: from hits to leads
(2016–2018) NHMRC Project Grant
Engineering peptides into superglues selective for target proteins
(2016–2018) ARC Discovery Projects
A nuclear magnetic resonance facility for modern molecular analysis
(2016–2017) ARC Linkage Infrastructure, Equipment and Facilities
Collaborative research program on stapled peptide therapeutics
(2016–2017) UniQuest Pty Ltd
(2016) UQ Major Equipment and Infrastructure
Integrative blood coagulation research core facility
(2016) UQ Major Equipment and Infrastructure
Development of antimalarial histone deacetylase inhibitors
(2015–2018) NHMRC Development Grant
Downsizing A Human Protein To Modulate Inflammatory Diseases
(2015–2017) NHMRC Project Grant
Engineering Cyclic Peptides For Oral Bioavailability
(2015–2017) ARC Discovery Projects
Targeting Protease Activated Receptor 2 In Immunometabolism And Obesity
(2015–2017) NHMRC Project Grant
Murine behavioural phenotyping facility
(2015) UQ Major Equipment and Infrastructure
ARC Centre of Excellence in Advanced Molecular Imaging (Monash lead institution)
(2014–2021) Monash University
Anti-Parasitic Drug Discovery in Epigenetics (A-PARADDISE) (EU FP7 grant administered by Inserm)
(2014–2017) Institut national de la santé et de la recherche médicale
IMB/Pfizer Collaborative Project on Peptide Therapeutics
(2014–2017) UniQuest Pty Ltd
(2014–2016) Griffith University
Continuous-Flow Hydrogenation Reactor (H-Cube Pro)
(2014) UQ Major Equipment and Infrastructure
Capturing New Drugs That Selectively Modulate PAR2 Signaling Pathways
(2013–2015) NHMRC Project Grant
Downsizing proteins to equipotent small molecules that activate cells
(2013–2015) ARC Discovery Projects
Inhibitors Of Class II HDACs In Inflammatory And Metabolic Disease
(2013–2015) NHMRC Project Grant
(2013–2014) Queensland Emory Development Alliance
NHMRC Research Fellowship (SPRF)
(2012–2016) NHMRC Research Fellowship
Flaviviral proteases as viable targets for antiinfective drugs
(2012–2015) NHMRC Project Grant
Small Molecule Modulators of Complement in Metabolism and Obesity
(2012–2015) NHMRC Project Grant
Profiling global inflammatory signatures for GPCRs in human macrophages
(2012–2014) NHMRC Project Grant
The Queensland-Pfizer Program for Diabetes and Cardiovascular Drug Discovery
(2012–2014) Queensland Government Smart Futures Co-Investment Fund
(2012–2013) ARC LIEF Collaborating/Partner Organisation Contributions
High- throughput Fourier Transform Infrared (FTIR) spectrometer.
(2012) UQ Major Equipment and Infrastructure
Innovations in peptide-based drug design
(2011–2014) ARC Linkage Projects
Auto-iTC200 microcalorimeter for high-throughput molecular interaction analyses
(2011) UQ Major Equipment and Infrastructure
Peptide Drug Synthesis and Purification Unit
(2011) UQ Major Equipment and Infrastructure
Real time cell analysis for biological and drug discovery applications
(2011) UQ Major Equipment and Infrastructure
(2010–2012) NHMRC Project Grant
(2010–2012) ARC Discovery Projects
Inhibitors of Secretory Phospholipases in Diet Induced Obese Rats
(2010–2012) NHMRC Project Grant
Protease activated receptor 2 antagonist in inflammatory disease
(2010–2012) NHMRC Development Grant
Protein And Peptide Alpha Turns
(2010–2012) ARC Discovery Projects
Advanced molecular discovery and characterisation facility
(2010–2011) ARC Linkage Infrastructure, Equipment and Facilities
Combinatorial chemistry (high throughput synthesizer and purification system)
(2010) UQ Major Equipment and Infrastructure
Resonant waveguide label-free plate sensor
(2010) UQ Major Equipment and Infrastructure
Protease Activated Receptor 2 : A New Drug Target For Inflammatory Diseases and Cancer
(2009–2012) NHMRC Project Grant
Towards selective targeting of HDACs for anti-inflammatory applications
(2009–2011) NHMRC Project Grant
Analytical flow cytometer for high throughput cell biology and drug discovery applications
(2009) UQ Major Equipment and Infrastructure
Microwave reactor for synthetic organic and medicinal chemistry
(2009) UQ Major Equipment and Infrastructure
Investigating A novel generic Approach to Anti-Infective Agents
(2008–2010) NHMRC Project Grant
Molecular characterization of dengue virus fusion and antiviral inhibitors
(2008–2010) NHMRC Project Grant
The mechanism of growth hormone receptor activation
(2008–2010) NHMRC Project Grant
Analytical and preparative enantioselective chromatography
(2008–2009) ARC Linkage Infrastructure, Equipment and Facilities
Profiling the pro- and anti-inflammatory functions of histone deacetylases in macrophages
(2008–2009) Cancer Council Queensland
DsbA inhibitors as potential antimicrobials
(2007–2009) NHMRC Project Grant
From Chemical Architecture to Protein Surfaces
(2007–2009) ARC Discovery Projects
Inhibitors Of West Nile Virus Protease As Antiviral Drugs
(2007–2009) NHMRC Project Grant
Targeting A Complement Receptor That Regulates Inflammatory Disease
(2007–2009) NHMRC Project Grant
An X-Ray Diffraction Facility for Molecular Structure Determination
(2007–2008) ARC Linkage Infrastructure, Equipment and Facilities
Chemical mimics of bioactive protein surfaces
(2006–2011) ARC Federation Fellowships
Smarter Diagnostics Through Selective Chemical Tagging
(2006–2009) Queensland Government Smart State Research Industry Partnerships Program
The West Nile Viral Protease, NS3: A Target for Antiviral Drug and Vaccine Design
(2006) UQ External Support Enabling Grant
Chemical Insights to Peptide Helix-Sheet-Nanofibre Equilibria
(2005–2007) ARC Discovery Projects
Development of novel and selective anticancer drugs derived from cysteine
(2005–2007) NHMRC Development Grant
ESEG_The rational design of non-covalent caspase inhibitors
(2005–2006) UQ External Support Enabling Grant
The West Nile viral protease NS3: a target for antiviral drug and vaccine design
(2005) NHMRC Project Grant
C3/C5 Convertase Inhibitors as a new class of anti-inflammatory drugs
(2004–2006) NHMRC Project Grant
Australian Computational Molecular Science Network
(2004) ARC Seed Funding for Research Networks
The Australian Protease Network
(2004) ARC Seed Funding for Research Networks
Agonists and antagonists of the human complement C3a receptor
(2003–2005) NHMRC Project Grant
Design And Development Of Small Molecules To Regulate Protease Activated Receptor Type 2
(2003–2005) NHMRC Project Grant
Virtual Screening In Structure-Based Drug Design For Malaria
(2003–2005) NHMRC Project Grant
Towards a clinical trial of anti-inflammatory drugs discovered by blocking enzymes.
(2003–2004) NHMRC Development Grant
(2002–2006) ARC Discovery Projects
Metal Clips for Folding Peptides
(2002–2004) ARC Discovery Projects
A Robotic NMR Spectrometer for Accelerated Drug Discovery
(2002) Research Infrastructure (Equip & Fac) Program
Towards new antiinflammatory drugs based on human immune defence
(2002) UQ External Support Enabling Grant
Design and Evaluation of Inhibitors of Phospholipases A2 as Anti-inflamatory Drugs
(2001–2003) NHMRC Project Grant
Mimicking Helical Turns of Proteins
(2001) University of Queensland Small Grants Scheme
Mimicking Helical Turns of Proteins.
(2001) ARC Australian Research Council (Large grants)
Applications of C5a antagonists in vivo
(2000–2002) NHMRC Project Grant
Design and development of inhibitors of the dengue virus protease as antiviral agents
(2000–2002) NHMRC Project Grant
Development of specific inhibitors of parasitic enzymes
(2000–2002) NHMRC Project Grant
Chemistry & Structural Biology of Metallopeptides in Alzheimer's Disease
(1999–2001) ARC Australian Research Council (Large grants)
Generic Technology for Enzyme Inhibition. Mimicking Protease-Binding Conformations of Peptides
(1999–2001) ARC Australian Research Council (Large grants)
(1999–2001) NHMRC Project Grant
Rational Design of Novel Antiretroviral Drugs to Overcome Resistance
(1999–2000) NHMRC Project Grant
Folding and reactivity of novel cyclic peptides containing unusual amino acids
(1998) ARC Australian Research Council (Small grants)
Approaches to the development of drugs for Alzheimer's disease
(1997–1999) NHMRC Project Grant
New differentiating agents selective for tumour cells
(1997–1998) Queensland Institute of Medical Research
Cyclic peptidomimetics that mimic protease-binding conformations of bioactive peptides
(1997) UQ External Support Enabling Grant
(1997) Asthma Foundation of Queensland
(1997) ARC Australian Research Council (Small grants)
Developing artificial antibodies
(1996–1998) NHMRC Project Grant - HIV/AIDS (CARG)
Approaches to the development of drugs for Alzheimer's disease
(1996) NHMRC Project - Special Initiative Grant
Approaches to the development of drugs for Alzheimer's disease
(1996) UQ External Support Enabling Grant
Folding and reactivity of novel cyclic peptides containing unusual amino acids
(1996) UQ External Support Enabling Grant
Synthesis structure and inhibition of an essential HIV regulatory protein REV
(1995–1997) Department Health & Family Services - CARG
Synthesis, structure and inhibition of an essential HIV regulatory protein REV
(1995–1997) NHMRC Project Grant - HIV/AIDS (CARG)
Design, synthesis and properties of new artificial receptors
(1995) University of Queensland New Staff Research Grant
Protein surface mimetics: Molecular toolkits for their construction
(1995) UQ External Support Enabling Grant
(1995) University of Queensland New Staff Research Grant
Peptide modulators for drug discovery
Doctor Philosophy — Principal Advisor
Other advisors:
Novel chemical approaches to drugs that selectively target immune cells
Doctor Philosophy — Principal Advisor
Other advisors:
New strategies in heterocyclic chemistry for drug discovery
Doctor Philosophy — Principal Advisor
Other advisors:
Novel activators and inhibitors of innate immune cells
Doctor Philosophy — Principal Advisor
Other advisors:
Design and synthesis of novel Major histocompatibility complex class I-Related protein ligands
Doctor Philosophy — Associate Advisor
Other advisors:
Combating bacterial infections through reprogramming of innate immunity
Doctor Philosophy — Associate Advisor
Other advisors:
Modulation of innate immune proteins in cancers
Doctor Philosophy — Associate Advisor
Other advisors:
G Protein-Coupled Receptors in Metabolism and Immunity
(2022) Doctor Philosophy — Principal Advisor
Novel mechanistic insights into oxytocin receptor signalling in breast cancer
(2021) Doctor Philosophy — Principal Advisor
Other advisors:
Targeting the oxytocin receptor for breast cancer imaging
(2021) Doctor Philosophy — Principal Advisor
Other advisors:
Towards Design and Synthesis of Novel HDAC Inhibitors
(2021) Doctor Philosophy — Principal Advisor
Towards Selective Inhibitors of HDAC1 and HDAC7
(2021) Doctor Philosophy — Principal Advisor
Detecting Oxytocin: Mass spectrometry and PET-tracer development
(2020) Doctor Philosophy — Principal Advisor
Other advisors:
GLP-1 Receptor Signaling By Novel GLP-1 Analogues
(2020) Doctor Philosophy — Principal Advisor
Other advisors:
Profiling novel experimental drug candidates for inflammatory diseases
(2020) Doctor Philosophy — Principal Advisor
Protease-Activated Receptor 2 Connects Metabolism to Inflammation in Human Epithelial Cells
(2020) Doctor Philosophy — Principal Advisor
Structure-function relationships of a ribityl uracil T-cell antigen
(2020) Master Philosophy — Principal Advisor
Other advisors:
Synthetic and Structural Studies of Small Cyclic Peptides
(2020) Doctor Philosophy — Principal Advisor
Other advisors:
Towards Inhibitors of HDAC1 with Antiparasitic Activity
(2020) Master Philosophy — Principal Advisor
Modulating Protease-Activated Receptor 2
(2018) Doctor Philosophy — Principal Advisor
Other advisors:
Computer Modeling of Protein-Ligand Interactions at Cell Surfaces
(2017) Doctor Philosophy — Principal Advisor
Heterocyclic agonists and antagonists for the C3a receptor
(2017) Doctor Philosophy — Principal Advisor
Towards ligand directed control of GLP-1R signalling
(2017) Doctor Philosophy — Principal Advisor
Characterising Novel and Potent Modulators of Complement Receptor C3aR
(2016) Doctor Philosophy — Principal Advisor
Structural Features in Orally Bioavailable Cyclic Peptides
(2016) Doctor Philosophy — Principal Advisor
Other advisors:
TOWARDS NEW DRUGS FOR TREATING COLITIS
(2016) Doctor Philosophy — Principal Advisor
Towards Cell Permeable Modulators of Protein-Protein Interactions
(2016) Doctor Philosophy — Principal Advisor
Other advisors:
Towards inhibitors of hydrolytic enzymes involved in inflammation
(2015) Doctor Philosophy — Principal Advisor
Other advisors:
Novel Agonists & Antagonists for Protease-Activated Receptor 2 and C3a Receptor
(2014) Doctor Philosophy — Principal Advisor
Properties of C5a Receptor on Human Macrophages
(2014) Doctor Philosophy — Principal Advisor
Other advisors:
Towards Serine Protease Inhibitors
(2014) Doctor Philosophy — Principal Advisor
Other advisors:
Links between inflammation and obesity
(2013) Doctor Philosophy — Principal Advisor
Molecular Pharmacology of C3aR Modulators
(2012) Doctor Philosophy — Principal Advisor
Short Helix-Constrained Peptides As RSV Fusion Inhibitors And Vaccine Candidates
(2012) Master Philosophy — Principal Advisor
Other advisors:
Towards HDAC Selective Inhibitors
(2012) Doctor Philosophy — Principal Advisor
Alpha Helices Mimetics
(2010) Doctor Philosophy — Principal Advisor
Regulation of inflammatory proteins
(2010) Doctor Philosophy — Principal Advisor
Other advisors:
Structural Studies of Cyclic Peptides
(2010) Doctor Philosophy — Principal Advisor
Other advisors:
Constraining short B cell epitopes as alpha helices
(2009) Doctor Philosophy — Principal Advisor
Other advisors:
Regulating Protease Activated Receptor 2
(2009) Doctor Philosophy — Principal Advisor
Agonists and Antagonists of Protease Activated Receptor-2 (PAR 2)
(2008) Doctor Philosophy — Principal Advisor
Computer Aided Drug Design: GPCRs and Proteases
(2008) Doctor Philosophy — Principal Advisor
Other advisors:
Design and Synthesis of HDAC inhibitors derived from a-aminosuberic acid
(2008) Master Philosophy — Principal Advisor
Ligands For C3a and C5a Receptors
(2008) Doctor Philosophy — Principal Advisor
Towards Constrained Alpha Helical Peptides
(2008) Doctor Philosophy — Principal Advisor
THE DESIGN, SYNTHESES AND STRUCTURES OF SMALL ALPHA-HELICAL PEPTIMOMIMETICS
(2006) Doctor Philosophy — Principal Advisor
MOLECULAR CHARACTERISTICS OF AGONISTS AND ANTAGONISTS OF TWO G-PROTEIN COUPLED RECEPTORS
(2005) Doctor Philosophy — Principal Advisor
MACROCYCLIC PSEUDOPEPTIDES AS MIMICS OF BIOACTIVE PROTEIN SURFACES
(2002) Doctor Philosophy — Principal Advisor
Other advisors:
NEW PROTEASE INHIBITORS AS PROBES OF BIOLOGICAL PROCESSES
(2002) Doctor Philosophy — Principal Advisor
Investigations of the effects of scanning focused ultrasound in mouse models of Alzheimer's disease.
(2017) Doctor Philosophy — Associate Advisor
Other advisors:
Characterisation of Human Macrophage Functions in Innate Immunity
(2015) Doctor Philosophy — Associate Advisor
Other advisors:
(2014) Doctor Philosophy — Associate Advisor
Stalking the West Nile Virus NS2B/NS3 protease as a target for infection control and as a key player in virus factories
(2013) Doctor Philosophy — Associate Advisor
Other advisors:
Modulation of the immune system in the metabolic syndrome
(2011) Doctor Philosophy — Associate Advisor
EFFECTS OF METAL BINDING ON PEPTIDE CONFORMATION
(2007) Doctor Philosophy — Associate Advisor
STRUCTURE-FUNCTION RELATIONSHIPS OF THE WEST NILE VIRUS PROTEASE NS3 AND ITS COFACTOR NS2B
(2007) Doctor Philosophy — Associate Advisor
Other advisors:
THE CHEMISTRY AND PHARMACOLOGY OF C3a AND C3a ANALOGUES
(2004) Doctor Philosophy — Associate Advisor
INVESTIGATIONS OF ENCAPSULATING LIGAND SYSTEMS AND THEIR METAL COMPLEXES
(2003) Doctor Philosophy — Associate Advisor
REACTIONS OF PLATINUM (II) COMPLEXES WITH SMALL PEPTIDES
(2003) Doctor Philosophy — Associate Advisor
Note for students: The possible research projects listed on this page may not be comprehensive or up to date. Always feel free to contact the staff for more information, and also with your own research ideas.
Targeting strategies for drug design
Selective binding of small molecules with proteins underpins most drug discovery. However, while a compound can be devised to interact with a single protein, this cannot drive the molecule into a specific location where functional modulation of the target protein only at that location is desired for therapy. Instead, designed compounds usually bind to the protein wherever it is expressed in the body and this can be deterimental to normal healthy physiology. This project will investigate a number of promising new approaches to directing protein-binding compounds to specific compartments of cells and organisms. It will require a combination of organic synthesis, medicinal chemistry, molecular modelling and chemical biology. The new approaches will be tested and optimised with the goal of inhibiting or activating desired proteins in specific compartments in order to modulate disease-causing protein functions without altering normal healthy physiology. Achieving these aims will require enthusiasm, a high degree of self-motivation, lateral thinking, strong chemical knowledge and hands-on skills in organic synthesis (solution and solid phase), NMR characterisation (including 2D NMR structure analysis), HPLC purification, mass spectrometry, and computer modelling. Some knowledge of enzyme assays and cell biology would be an advantage. The long term goal is to design new compounds and profile them for selective effects on target genes/proteins/cells/rodent models of inflammatory diseases and cancer. Outcomes will include new knowledge of protein function in disease; greater understanding of medicinal and organic chemistry in drug design, drug targeting, mechanisms and effectiveness of drug action; patentable methods and bioactive compounds; and new experimental leads to new medicines for development towards the clinic.