De Mol…Salvatella {ACS Chem Biol 11: 2499}

EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor. ACS Chem Biol. 2016 Sep 16;11(9):2499-505. doi: 10.1021/acschembio.6b00182.
Castration-resistant prostate cancer is the condition suffered by patients refractory to the first line treatment. EPI-001 is a compound active against it that modulates the activity of the androgen receptor, a nuclear receptor essential for disease progression. Here we show that it interacts with a region of the transactivation domain of this receptor that is key for the ability of prostate cells to proliferate in the absence of androgens, a feature of this disease.