[HTML][HTML] Direct regulation of androgen receptor activity by potent CYP17 inhibitors in prostate cancer cells
HS Soifer, N Souleimanian, S Wu… - Journal of Biological …, 2012 - ASBMB
TOK-001 and abiraterone are potent 17-heteroarylsteroid (17-HAS) inhibitors of Cyp17, one
of the rate-limiting enzymes in the biosynthesis of testosterone from cholesterol in prostate
cancer cells. Nevertheless, the molecular mechanism underlying the prevention of prostate
cell growth by 17-HASs still remains elusive. Here, we assess the effects of 17-HASs on
androgen receptor (AR) activity in LNCaP and LAPC-4 cells. We demonstrate that both TOK-
001 and abiraterone reduced AR protein and mRNA expression, and antagonized AR …
of the rate-limiting enzymes in the biosynthesis of testosterone from cholesterol in prostate
cancer cells. Nevertheless, the molecular mechanism underlying the prevention of prostate
cell growth by 17-HASs still remains elusive. Here, we assess the effects of 17-HASs on
androgen receptor (AR) activity in LNCaP and LAPC-4 cells. We demonstrate that both TOK-
001 and abiraterone reduced AR protein and mRNA expression, and antagonized AR …