Identification of Lead Compounds As Antagonists of Protein Bcl-xL with a Diversity-Oriented Multidisciplinary Approach

被引：27

作者：

Di Micco, Simone ^{[2
]}

Vitale, Romina ^{[1
]}

Pellecchia, Maurizio ^{[3
]}

Rega, Michele F. ^{[3
]}

Riva, Renata ^{[1
]}

Basso, Andrea ^{[1
]}

Bifulco, Giuseppe ^{[2
]}

机构：

[1] Univ Genoa, Dipartimento Chim & Chim Ind, I-16146 Genoa, Italy

[2] Univ Salerno, Dipartimento Sci Farmaceut, I-84084 Fisciano, SA, Italy

[3] Burnham Inst Med Res, La Jolla, CA 92037 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 23期

关键词：

AMINO ACID-DERIVATIVES; BCL-2; FAMILY; REGULATORS; BINDING;

D O I：

10.1021/jm9010687

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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-x(L) 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.

引用

页码：7856 / 7867

页数：12

共 34 条

[31] Structure of Bcl-x(L)-Bak peptide complex: Recognition between regulators of apoptosis [J].