Selective androgen receptor modulators activate the canonical prostate cancer androgen receptor program and repress cancer growth.

ABSTRACT: Prostate cancer (PC) is driven by androgen receptor (AR) activity, a master regulator of prostate development and homeostasis. Frontline therapies for metastatic PC deprive the AR of the activating ligands testosterone (T) and dihydrotestosterone (DHT) by limiting their biosynthesis or blocking AR binding. Notably, AR signaling is dichotomous, inducing growth at lower activity levels, while suppressing growth at higher levels. Recent clinical studies have exploited this effect by administration of supraphysiological concentrations of T, resulting in clinical responses and improvements in quality of life. However, the use of T as a therapeutic agent in oncology is limited by poor drug-like properties as well as rapid and variable metabolism. Here, we investigated the antitumor effects of se

SUBMITTER: Nyquist MD 

PROVIDER: S-EPMC8121509 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature