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Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).

ABSTRACT: CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology. As part of our effort to explore the potential therapeutic implications of selectively targeting bromodomains, we set out to identify a CBP/EP300 bromodomain inhibitor that was potent both in vitro and in cellular target engagement assays and was selective over the other members of the bromodomain family. Reported here is a series of cell-potent and selective probes of the CBP/EP300 bromodomains, derived from the fragment screening hit 4-methyl-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one.

SUBMITTER: Taylor AM 

PROVIDER: S-EPMC4867486 | biostudies-other | 2016 May

REPOSITORIES: biostudies-other

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Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).

Taylor Alexander M AM   Côté Alexandre A   Hewitt Michael C MC   Pastor Richard R   Leblanc Yves Y   Nasveschuk Christopher G CG   Romero F Anthony FA   Crawford Terry D TD   Cantone Nico N   Jayaram Hariharan H   Setser Jeremy J   Murray Jeremy J   Beresini Maureen H MH   de Leon Boenig Gladys G   Chen Zhongguo Z   Conery Andrew R AR   Cummings Richard T RT   Dakin Leslie A LA   Flynn E Megan EM   Huang Oscar W OW   Kaufman Susan S   Keller Patricia J PJ   Kiefer James R JR   Lai Tommy T   Li Yingjie Y   Liao Jiangpeng J   Liu Wenfeng W   Lu Henry H   Pardo Eneida E   Tsui Vickie V   Wang Jian J   Wang Yongyun Y   Xu Zhaowu Z   Yan Fen F   Yu Dong D   Zawadzke Laura L   Zhu Xiaoqin X   Zhu Xiaoyu X   Sims Robert J RJ   Cochran Andrea G AG   Bellon Steve S   Audia James E JE   Magnuson Steven S   Albrecht Brian K BK  

ACS medicinal chemistry letters 20160315 5

CBP and EP300 are highly homologous, bromodomain-containing transcription coactivators involved in numerous cellular pathways relevant to oncology. As part of our effort to explore the potential therapeutic implications of selectively targeting bromodomains, we set out to identify a CBP/EP300 bromodomain inhibitor that was potent both in vitro and in cellular target engagement assays and was selective over the other members of the bromodomain family. Reported here is a series of cell-potent and  ...[more]

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