A potent and orally active antagonist of multiple inhibitor of apoptosis proteins (IAPs) (SM-406/AT-406) in clinical development for cancer treatment

We report the discovery and characterization of SM-406 (compound 2), a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). This compound binds to XIAP, cIAP1 and cIAP2 proteins with K(i) values of 66.4 nM, 1.9 nM and 5.1 nM, respectively. Comp...

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Main Authors: Cai, Qian, Sun, Haiying, Peng, Yuefeng, Lu, Jianfeng, Nikolovska-Coleska, Zaneta, McEachern, Donna, Liu, Liu, Qiu, Su, Yang, Chao-Yie, Miller, Rebecca, Yi, Han, Zhang, Tao, Sun, Duxin, Kang, Sanmao, Guo, Ming, Leopold, Lance, Yang, Dajun, Wang, Shaomeng
פורמט: Artigo
שפה:Inglês
יצא לאור: 2011
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Article
גישה מקוונת:https://ncbi.nlm.nih.gov/pmc/articles/PMC3520070/
https://ncbi.nlm.nih.gov/pubmed/21443232
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm101505d
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