Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer.

ABSTRACT: The androgen receptor (AR) is a transcription factor that has a pivotal role in the occurrence and progression of prostate cancer. The AR is activated by androgens that bind to its ligand-binding domain (LBD), causing the transcription factor to enter the nucleus and interact with genes via its conserved DNA-binding domain (DBD). Treatment for prostate cancer involves reducing androgen production or using anti-androgen drugs to block the interaction of hormones with the AR-LBD. Eventually the disease changes into a castration-resistant form of PCa where LBD mutations render anti-androgens ineffective or where constitutively active AR splice variants, lacking the LBD, become overexpressed. Recently, we identified a surfaced exposed pocket on the AR-DBD as an alternative drug-target site for

SUBMITTER: Dalal K 

PROVIDER: S-EPMC4176249 | biostudies-literature | 2014 Sep

REPOSITORIES: biostudies-literature