A small molecular scaffold for selective inhibition of Wip1 phosphatase

被引：14

作者：

Bang, Jeong ^{[1
]}

Yamaguchi, Hiroshi ^{[1
]}

Durell, Stewart R. ^{[1
]}

Appella, Ettore ^{[1
]}

Appella, Daniel H. ^{[2
]}

机构：

[1] NCI, Cell Biol Lab, Bethesda, MD 20892 USA

[2] NIDDK, Bioorgan Chem Lab, NIH, DHHS, Bethesda, MD 20892 USA

来源：

CHEMMEDCHEM | 2008年 / 3卷 / 02期

关键词：

enzyme inhibition; organic synthesis; pyrrole; small molecules; Wip1;

D O I：

10.1002/cmdc.200700281

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(Figure Presented) Inhibiting Wip1. Using a pyrrole-based scaffold, we developed a series of small molecules that mimic the three-dimensional arrangement of the polar and hydrophobic functional groups of the best cyclic peptide inhibitor.Iterative optimization cycles of design, synthesis, and kinetic testing has lead to a selective inhibitor of Wip1. The picture shows the structure of the best inhibitor bound to the active site of the enzyme. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：230 / 232

页数：3

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