EPI-001 is a specific inhibitor of the AR (androgen receptor) without inhibiting PR or GR transcriptional activities.
EPI-001 is a specific inhibitor of the AR (androgen receptor) without inhibiting PR or GR transcriptional activities. EPI-001 selectively interacts with transactivation unit 5 (Tau-5) of the androgen receptor, which is essential for prostate cells to proliferate in the absence of androgens. EPI-001 is active against castration-resistant prostate cancer (CRPC) in xenografts.
ACS chemical biology, 11(9), 2499-2505 (2016-06-30)
Castration-resistant prostate cancer is the lethal condition suffered by prostate cancer patients that become refractory to androgen deprivation therapy. EPI-001 is a recently identified compound active against this condition that modulates the activity of the androgen receptor, a nuclear receptor
Castration-recurrent prostate cancer (CRPC) is suspected to depend on androgen receptor (AR). The AF-1 region in the amino-terminal domain (NTD) of AR contains most, if not all, of the transcriptional activity. Here we identify EPI-001, a small molecule that blocked
The androgen receptor (AR) is a driver of prostate cancer (PCa) cell growth and disease progression. Therapies for advanced PCa exploit AR dependence by blocking the production or action of androgens, but these interventions inevitably fail via multiple mechanisms including
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