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De-novo designed library of benzoylureas as inhibitors of BCL-XL: synthesis, structural and biochemical characterization

…, JP Parisot, H Yang, IP Street, PM Colman…

文献索引:Brady, Ryan M.; Vom, Amelia; Roy, Michael J.; Toovey, Nathan; Smith, Brian J.; Moss, Rebecca M.; Hatzis, Effie; Huang, David C. S.; Parisot, John P.; Yang, Hong; Street, Ian P.; Colman, Peter M.; Czabotar, Peter E.; Baell, Jonathan B.; Lessene, Guillaume Journal of Medicinal Chemistry, 2014 , vol. 57, # 4 p. 1323 - 1343

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被引用次数: 12

摘要

The prosurvival BCL-2 proteins are attractive yet challenging targets for medicinal chemists. Their involvement in the initiation and progression of many, if not all, tumors makes them prime targets for developing new anticancer therapies. We present our approach based on de novo structure-based drug design. Using known structural information from complexes engaging opposing members of the BCL-2 family of proteins, we designed peptidomimetic ...