Identification of Lead Compounds As Antagonists of Protein Bcl-xL with a Diversity-Oriented Multidisciplinary Approach
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- 作者：Simone Di Micco ; Romina Vitale ; Maurizio Pellecchia ; Michele F. Rega ; Renata Riva ; Andrea Basso ; Giuseppe Bifulco
- 刊名：Journal of Medicinal Chemistry
- 出版年：2009
- 出版时间：December 10, 2009
- 年：2009
- 卷：52
- 期：23
- 页码：7856-7867
- 全文大小：1511K
- 年卷期：v.52,no.23(December 10, 2009)
- ISSN：1520-4804
文摘
We report on the use of a diversity oriented synthesis (DOS) approach that resulted in the generation of a set of libraries of compounds presenting novel structural cores. These chemical cores have been employed to design potential antagonists of the antiapoptotic protein Bcl-xL through reiterated steps of molecular docking calculations followed by experimental verification of binding. Our data suggest that the DOS approach is suitable to generate novel scaffolds, which can be employed to target protein−protein interactions.