Design and application of an α-helix-mimetic scaffold based on an oligoamide-foldamer strategy:: Antagonism of the bak BH3/Bcl-xL complex

被引：238

作者：

Ernst, JT ^{[1
]}

Becerril, J ^{[1
]}

Park, HS ^{[1
]}

Yin, H ^{[1
]}

Hamilton, AD ^{[1
]}

机构：

[1] Yale Univ, Dept Chem, New Haven, CT 06520 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2003年 / 42卷 / 05期

关键词：

amides; helical structures; peptidomimetics; protein models; proteins;

D O I：

10.1002/anie.200390154

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The prevention of cell death by the antiapoptotic protein Bcl-xL has been linked to a number of cancers. Bcl-xl binds to the BH3 domain of the proapoptotic protein Bak, thus preventing programmed cell death. A competitive assay and docking studies have shown that the polyamide scaffold 1, which was synthesized based on a rational structure-based design, interferes with the Bak BH3/Bcl-xl complexation.

引用

页码：535 / +

页数：6

共 23 条

[1] BCL-2 FAMILY: Regulators of cell death [J].