De-novo designed library of benzoylureas as inhibitors of BCL-XL: synthesis, structural and biochemical characterization
…, JP Parisot, H Yang, IP Street, PM Colman…
Index: 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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Citation Number: 12
Abstract
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 ...
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