Using a β-hairpin to mimic an α-helix:: Cyclic peptidomimetic inhibitors of the p53-HDM2 protein-protein interaction

被引：142

作者：

Fasan, R

Dias, RLA

Moehle, K

Zerbe, O

Vrijbloed, JW

Obrecht, D

Robinson, JA

机构：

[1] Univ Zurich, Inst Organ Chem, CH-8057 Zurich, Switzerland

[2] Polyphor AG, CH-4123 Allschwil, Switzerland

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2004年 / 43卷 / 16期

关键词：

antitumor agents; inhibitors; peptidomimetics; protein structures;

D O I：

10.1002/anie.200353242

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Inhibition of crucial protein-protein interactions, for example, between the p53 tumor suppressor (red in structure) and HDM2, a protein overexpressed in tumor cells, is possible with peptidomimetics having a β-hairpin structure (yellow) mimicking the α-helical protein epitope. These mimetics might be of direct value in the search for novel agents with tumor-suppressor activity.

引用

收藏

页码：2109 / 2112

页数：4

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