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Design, Synthesis and Evaluation of Potent, Non-Peptidic Mimetics of Second Mitochondria-derived Activator of Caspases

A series of new Smac mimetics have been designed, synthesized and evaluated. The most potent compound 10 binds to XIAP, cIAP-1 and cIAP-2 BIR3 proteins with K(i) values of 3.9, 0.37 and 0.25 nM, respectively. Compound 10 antagonizes XIAP in a cell-free functional assay and induces rapid cIAP-1 degra...

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Détails bibliographiques
Auteurs principaux: Sun, Wei, Nikolovska-Coleska, Zaneta, Qin, Dongguang, Sun, Haiying, Yang, Chao-Yie, Bai, Longchuang, Qiu, Su, Ma, Dawei, Wang, Shaomeng
Format: Artigo
Langue:Inglês
Publié: 2009
Sujets:
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC2795317/
https://ncbi.nlm.nih.gov/pubmed/19138149
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm801101z
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