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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...

Deskribapen osoa

Gorde:
Xehetasun bibliografikoak
Egile Nagusiak: 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
Formatua: Artigo
Hizkuntza:Inglês
Argitaratua: 2011
Gaiak:
Sarrera elektronikoa: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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