Repression of BET activity sensitizes homologous recombination-proficient cancers to PARP inhibition

• Published in: Science translational medicine Vol. 9; no. 400
• Main Authors: Yang, Lu, Zhang, Youyou, Shan, Weiwei, Hu, Zhongyi, Yuan, Jiao, Pi, Jingjiang, Wang, Yueying, Fan, Lingling, Tang, Zhaoqing, Li, Chunsheng, Hu, Xiaowen, Tanyi, Janos L, Fan, Yi, Huang, Qihong, Montone, Kathleen, Dang, Chi V, Zhang, Lin
• Format: Journal Article
• Language: English
• Published: United States 26.07.2017
• Subjects: Acetanilides - therapeutic use; Animals; Antineoplastic Agents - therapeutic use; Azepines - therapeutic use; Benzodiazepines - therapeutic use; Breast Neoplasms - drug therapy; Cell Line, Tumor; DNA Damage - drug effects; DNA Damage - genetics; Drug Synergism; Female; Heterocyclic Compounds, 3-Ring - therapeutic use; Homologous Recombination - drug effects; Homologous Recombination - genetics; Humans; Ovarian Neoplasms - drug therapy; Phthalazines - therapeutic use; Piperazines - therapeutic use; Poly(ADP-ribose) Polymerase Inhibitors - therapeutic use; Triazoles - therapeutic use

Strategies to enhance response to poly(adenosine diphosphate-ribose) polymerase inhibitor (PARPi) in primary and acquired homologous recombination (HR)-proficient tumors would be a major advance in cancer care. We used a drug synergy screen that combined a PARPi, olaparib, with 20 well-characterized...