[HTML][HTML] Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor

D Masiello, S Cheng, GJ Bubley, ML Lu… - Journal of Biological …, 2002 - ASBMB
Prostate cancers (PCa) that relapse after androgen deprivation therapy invariably express
high levels of androgen receptor (AR) and AR-regulated genes. Most do not respond to
secondary hormonal therapies, including AR antagonists, and the mechanisms of AR
activation in these clinically androgen-independent tumors are unclear. Bicalutamide, the
most widely used AR antagonist, is a competitive antagonist shown previously to stabilize
AR association with cytosolic heat shock protein complexes. This study found nuclear AR …