A Myosin V Inhibitor Based on Privileged Chemical Scaffolds

被引：35

作者：

Islam, Kabirul ^{[2
]}

Chin, Harvey F. ^{[1
]}

Olivares, Adrian O. ^{[1
]}

Saunders, Lauren P. ^{[1
]}

De La Cruz, Enrique M. ^{[1
]}

Kapoor, Tarun M. ^{[2
]}

机构：

[1] Yale Univ, Dept Mol Biophys & Biochem, New Haven, CT 06520 USA

[2] Rockefeller Univ, Lab Chem & Cell Biol, New York, NY 10065 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2010年 / 49卷 / 45期

关键词：

inhibitors; kinases; motor proteins; privileged scaffolds; structure-activity relationships; SMALL-MOLECULE INHIBITOR; ACTIN-BINDING; MECHANISM; PROTEINS; ADP;

D O I：

10.1002/anie.201004026

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Switching the motor off: Privileged chemical scaffolds were used as a starting point for the development of a specific chemical inhibitor 1 of myosin-V, a key motor protein required for intracellular transport (see picture; ADP=adenosine diphosphate, ATP=adenosine triphosphate). The potency of 1, which does not compete directly with nucleotide binding, is comparable to that of other known motor-protein inhibitors used as probes in chemical biology. © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

引用

页码：8484 / 8488

页数：5

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