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Jin, Lingyan; Garcia, Jesse; Chan, Emily; de la Cruz, Cecile; Segal, Ehud; Merchant, Mark; Kharbanda, Samir; Raisner, Ryan; Haverty, Peter M.; Modrusan, Zora; Ly, Justin; Choo, Edna; Kaufman, Susan; Beresini, Maureen H.; Romero, F. Anthony; Magnuson, Steven; Gascoigne, Karen E.

Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer

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  • Media type: E-Article
  • Title: Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer
  • Contributor: Jin, Lingyan; Garcia, Jesse; Chan, Emily; de la Cruz, Cecile; Segal, Ehud; Merchant, Mark; Kharbanda, Samir; Raisner, Ryan; Haverty, Peter M.; Modrusan, Zora; Ly, Justin; Choo, Edna; Kaufman, Susan; Beresini, Maureen H.; Romero, F. Anthony; Magnuson, Steven; Gascoigne, Karen E.
  • imprint: American Association for Cancer Research (AACR), 2017
  • Published in: Cancer Research
  • Language: English
  • DOI: 10.1158/0008-5472.can-17-0314
  • ISSN: 1538-7445; 0008-5472
  • Origination:
  • Footnote:
  • Description: <jats:title>Abstract</jats:title> <jats:p>Resistance invariably develops to antiandrogen therapies used to treat newly diagnosed prostate cancers, but effective treatments for castration-resistant disease remain elusive. Here, we report that the transcriptional coactivator CBP/p300 is required to maintain the growth of castration-resistant prostate cancer. To exploit this vulnerability, we developed a novel small-molecule inhibitor of the CBP/p300 bromodomain that blocks prostate cancer growth in vitro and in vivo. Molecular dissection of the consequences of drug treatment revealed a critical role for CBP/p300 in histone acetylation required for the transcriptional activity of the androgen receptor and its target gene expression. Our findings offer a preclinical proof of concept for small-molecule therapies to target the CBP/p300 bromodomain as a strategy to treat castration-resistant prostate cancer. Cancer Res; 77(20); 5564–75. ©2017 AACR.</jats:p>
  • Access State: Open Access