Androgen receptor antagonism by divalent ethisterone conjugates in castrate-resistant prostate cancer cells.

ABSTRACT: Sustained treatment of prostate cancer with androgen receptor (AR) antagonists can evoke drug resistance, leading to castrate-resistant disease. Elevated activity of the AR is often associated with this highly aggressive disease state. Therefore, new therapeutic regimens that target and modulate AR activity could prove beneficial. We previously introduced a versatile chemical platform to generate competitive and non-competitive multivalent peptoid oligomer conjugates that modulate AR activity. In particular, we identified a linear and a cyclic divalent ethisterone conjugate that exhibit potent anti-proliferative properties in LNCaP-abl cells, a model of castrate-resistant prostate cancer. Here, we characterize the mechanism of action of these compounds utilizing confocal microscopy, time-r

SUBMITTER: Levine PM 

PROVIDER: S-EPMC3874888 | biostudies-literature | 2012 Oct

REPOSITORIES: biostudies-literature