Understanding and Inhibiting P450 CYP24, a target for cancer chemotherapeutics (2008–2010)
Abstract:
Cytochrome CYP24 is an enzyme responsible for the degradation of the protective, active form of Vitamin D3 and is over-expressed in a number of cancer cell lines. CYP24 inhibitors are important anti-cancer targets. Here, the currently unknown mechanism of CYP24-mediated Vitamin D3 degradation will be elucidated using a unique combination of organic synthesis, spectroscopic, kinetic and computational methods. This knowledge will allow the design and synthesis of novel inhibitory compounds of CYP24 that will be evaluated in vitro and in vivo for their ability to inhibit Vitamin D3 metabolism and so act as potential anti-cancer chemotherapeutics.
