Ontology highlight
ABSTRACT:
SUBMITTER: Alyamani M
PROVIDER: S-EPMC5533090 | biostudies-literature | 2017 Jul
REPOSITORIES: biostudies-literature
Alyamani Mohammad M Li Zhenfei Z Berk Michael M Li Jianneng J Tang Jingjie J Upadhyay Sunil S Auchus Richard J RJ Sharifi Nima N
Cell chemical biology 20170622 7
Galeterone is a steroidal CYP17A1 inhibitor, androgen receptor (AR) antagonist, and AR degrader, under evaluation in a phase III clinical trial for castration-resistant prostate cancer (CRPC). The A/B steroid ring (Δ<sup>5</sup>,3β-hydroxyl) structure of galeterone is identical to that of cholesterol, which makes endogenous steroids with the same structure (e.g., dehydroepiandrosterone and pregnenolone) substrates for the enzyme 3β-hydroxysteroid dehydrogenase (3βHSD). We found that galeterone i ...[more]