Miners JO

Slow tight binding inhibition of CYP17A1 by abiraterone redefines its kinetic selectivity and dosing regimen

Substantial evidence underscores the clinical efficacy of inhibiting cytochrome P450 17A1 (CYP17A1)-mediated androgen biosynthesis by abiraterone for treatment of prostate oncology. Previous structural analysis and in vitro assays revealed inconsistencies surrounding the nature and potency of CYP17A1 inhibition by abiraterone.