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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Vydáno v:ACS Med Chem Lett
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2016
On-line přístup: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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