Heterocyclic α-helix mimetics for targeting protein-protein interactions

被引：71

作者：

Biros, Shannon M.

Moisan, Lionel

Mann, Enrique

Carella, Alexandre

Zhai, Dayong

Reed, John C.

Rebek, Julius, Jr.

机构：

[1] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 16期

关键词：

alpha-helix mimetic; pyridzaine; Bak/Bcl-X-L; protein-protein interaction; Diels-Alder;

D O I：

10.1016/j.bmcl.2007.05.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

The design and synthesis of alpha-helix peptidomimetics using inverse electron demand Diels-Alder reactions is described. The potency of the resulting pyridazine-based library to disrupt the Bak/Bcl-X-L interaction was tested using an in vitro fluorescence polarization assay. (c) 2007 Elsevier Ltd. All rights reserved.

引用

收藏

页码：4641 / 4645

页数：5

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