Background: The androgen receptor (AR) is a transcription factor regulating progression of prostate cancer.
Results: Developed compounds inhibit AR transcriptional activity in vitro and in vivo by selective targeting of the AR-DNA-binding domain (DBD).
Conclusion: By targeting the DBD, the compounds differ from conventional anti-androgens.
Significance: Anti-androgens with a novel mechanism of action have the potential to treat recurrent prostate cancer.
Bibliographical notePublisher Copyright:
© 2014 by The American Society for Biochemistry and Molecular Biology, Inc.