Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein …

…, J Wang, XH Chen, XH Ren, J Liu, JG Lv, J Zhu…

文献索引：Zheng, Can-Hui; Yang, Hui; Zhang, Meng; Lu, Shi-Hai; Shi, Duo; Wang, Juan; Chen, Xiu-Hua; Ren, Xiao-Hui; Liu, Jia; Lv, Jia-Guo; Zhu, Ju; Zhou, You-Jun Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 39 - 44

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被引用次数: 14

摘要

On the basis of the comparison of the structure of the Bim BH3: Bcl-xL complex and that of the ABT-737: Bcl-xL complex, a series of class A compounds were designed. These compounds had the basic skeleton of ABT-737 and the h2 residues of Bim BH3. These residues had shown themselves to be relevant to Bim BH3's broad-spectrum binding properties in saturation mutagenesis assays. Unlike ABT-737, which is a selective ...