CYP26C1 Inhibitors

CYP26C1 inhibitors primarily belong to the class of compounds known as azoles. These molecules are characterized by a five-membered ring containing at least one nitrogen atom. The azole-based inhibitors, such as Talarozole, Ketoconazole, and Liarozole, bind to the heme iron in the cytochrome P450 enzyme's active site, thereby blocking the access of retinoic acid to this site and inhibiting its metabolism. This interference with the binding and subsequent metabolism of retinoic acid effectively reduces the activity of CYP26C1.

Non-azole compounds, such as 1-Aminobenzotriazole and 4-phenylimidazole, though not as specific as the azole-based compounds, can interact with the enzyme's active site or with the heme group itself. These interactions lead to changes in the enzyme's conformation, which can subsequently diminish its activity. Abiraterone, although primarily recognized as a CYP17 inhibitor, demonstrates the promiscuity of some inhibitors across the cytochrome P450 family.