Use of a retroinverso p53 peptide as an inhibitor of MDM2

被引：58

作者：

Sakurai, K

Chung, HS

Kahne, D ^{[1
]}

机构：

[1] Harvard Univ, Dept Chem & Biol Chem, Cambridge, MA 02138 USA

[2] Harvard Univ, Sch Med, Dept Biol Chem & Mol Pharmacol, Boston, MA 02115 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2004年 / 126卷 / 50期

关键词：

D O I：

10.1021/ja044883w

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

An N-terminal helical region of the tumor suppressor p53 binds in a hydrophobic cleft of the oncoprotein MDM2. A retroinverso isomer of the natural N-terminal helical peptide was found to interact with MDM2 using the same hydrophobic residues, Phe, Trp, and Leu. We propose that the retroinverso d-peptide adopts a right-handed helical conformation to achieve functional mimicry of the p53 peptide. Copyright © 2004 American Chemical Society.

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页码：16288 / 16289

页数：2

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