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

[Image: see text] 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...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Taylor, Alexander M., Côté, Alexandre, Hewitt, Michael C., Pastor, Richard, Leblanc, Yves, Nasveschuk, Christopher G., Romero, F. Anthony, Crawford, Terry D., Cantone, Nico, Jayaram, Hariharan, Setser, Jeremy, Murray, Jeremy, Beresini, Maureen H., de Leon Boenig, Gladys, Chen, Zhongguo, Conery, Andrew R., Cummings, Richard T., Dakin, Leslie A., Flynn, E. Megan, Huang, Oscar W., Kaufman, Susan, Keller, Patricia J., Kiefer, James R., Lai, Tommy, Li, Yingjie, Liao, Jiangpeng, Liu, Wenfeng, Lu, Henry, Pardo, Eneida, Tsui, Vickie, Wang, Jian, Wang, Yongyun, Xu, Zhaowu, Yan, Fen, Yu, Dong, Zawadzke, Laura, Zhu, Xiaoqin, Zhu, Xiaoyu, Sims, Robert J., Cochran, Andrea G., Bellon, Steve, Audia, James E., Magnuson, Steven, Albrecht, Brian K.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2016
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4867486/
https://ncbi.nlm.nih.gov/pubmed/27190605
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00075
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