Background
CYP17A1, also known as cytochrome P450C17, is a steroidogenic enzyme belonging to the P450 cytochrome superfamily of monooxygenases. In humans, CYP17A1 expression is abundantly expressed in the adrenal cortex, where it plays a central role in the androgen synthesis pathway. CYP17A1 is the primary target of abiraterone, a synthetic steroid used in the treatment of castration-resistant prostate cancer. Abiraterone is converted to the more active form D4A, which antagonizes androgen receptor signaling by inhibiting CYP17A1 and other steroidogenic enzymes. This suppresses the synthesis of 5α-dihydrotestosterone, which is a driver of castration-resistant prostate cancer cell growth.
References
[1] Missaghian, E. et al. (2009) J Endocrinol 202, 99-109.
[2] Tee, M.K. and Miller, W.L. (2013) J Biol Chem 288, 23903-13.
[3] Li, Z. et al. (2015) Nature 523, 347-51.
[4] Thoma, C. (2015) Nat Rev Urol 12, 363.
