Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

Proteins of the bromodomain and extra-terminal (BET) family are epigenetics “readers” and promising therapeutic targets for cancer and other human diseases. We describe herein a structure-guided design of 1,4-oxazepines as a new class of BET inhibitors and our subsequent design, synthesis and evalua...

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Publicado en:J Med Chem
Main Authors: Qin, Chong, Hu, Yang, Zhou, Bing, Fernandez-Salas, Ester, Yang, Chao-Yie, Liu, Liu, McEachern, Donna, Przybranowski, Sally, Wang, Mi, Stuckey, Jeanne, Meagher, Jennifer, Bai, Longchuan, Chen, Zhuo, Lin, Mei, Yang, Jiuling, Xu, Fuming, Hu, Jiantao, Xing, Weiguo, Huang, Liyue, Li, Siwei, Wen, Bo, Sun, Duxin, Wang, Shaomeng
Formato: Artigo
Idioma:Inglês
Publicado: 2018
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC6545111/
https://ncbi.nlm.nih.gov/pubmed/30019901
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b00506
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