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

Kush Dalal, Mani Roshan-Moniri, Aishwariya Sharma, Huifang Li, Fuqiang Ban, Mohamed Hessein, Michael Hsing, Kriti Singh, Eric LeBlanc, Scott Dehm, Emma S. Tomlinson Guns, Artem Cherkasov, Paul S. Rennie

Research output: Contribution to journalArticlepeer-review

59 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)26417-26429
Number of pages13
JournalJournal of Biological Chemistry
Volume289
Issue number38
DOIs
StatePublished - Sep 19 2014

Bibliographical note

Publisher Copyright:
© 2014 by The American Society for Biochemistry and Molecular Biology, Inc.

Fingerprint Dive into the research topics of 'Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer'. Together they form a unique fingerprint.

Cite this