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

doi:10.1074/jbc.M114.553818

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

Laboratory Medicine and Pathology

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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 language	English (US)
Pages (from-to)	26417-26429
Number of pages	13
Journal	Journal of Biological Chemistry
Volume	289
Issue number	38
DOIs	https://doi.org/10.1074/jbc.M114.553818
State	Published - Sep 19 2014

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

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Dalal, K., Roshan-Moniri, M., Sharma, A., Li, H., Ban, F., Hessein, M., Hsing, M., Singh, K., LeBlanc, E., Dehm, S., Tomlinson Guns, E. S., Cherkasov, A., & Rennie, P. S. (2014). Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer. Journal of Biological Chemistry, 289(38), 26417-26429. https://doi.org/10.1074/jbc.M114.553818

Dalal, K, Roshan-Moniri, M, Sharma, A, Li, H, Ban, F, Hessein, M, Hsing, M, Singh, K, LeBlanc, E, Dehm, S, Tomlinson Guns, ES, Cherkasov, A & Rennie, PS 2014, 'Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer', Journal of Biological Chemistry, vol. 289, no. 38, pp. 26417-26429. https://doi.org/10.1074/jbc.M114.553818

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AU - Ban, Fuqiang

AU - Hessein, Mohamed

AU - Hsing, Michael

AU - Singh, Kriti

AU - LeBlanc, Eric

AU - Dehm, Scott

AU - Tomlinson Guns, Emma S.

AU - Cherkasov, Artem

AU - Rennie, Paul S.

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

Abstract

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