BTB-1: A Small Molecule Inhibitor of the Mitotic Motor Protein Kif18A

被引：52

作者：

Catarinella, Mario ^{[1
]}

Gruener, Tamara ^{[2
]}

Strittmatter, Tobias ^{[1
]}

Marx, Andreas ^{[1
]}

Mayer, Thomas U. ^{[1
]}

机构：

[1] Univ Konstanz, Konstanz Res Sch Chem Biol, D-78457 Constance, Germany

[2] London Res Inst, Lincolns Inn Fields Labs, London WC2A 3PX, England

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2009年 / 48卷 / 48期

关键词：

antiproliferation; enzymes; inhibitors; mitosis; molecular motors; KINESIN EG5; CHROMOSOME ALIGNMENT; CELL-DIVISION; SPINDLE; POLO-LIKE-KINASE-1; MICROTUBULES;

D O I：

10.1002/anie.200904510

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Turning the motor off: A malachite green based assay leads to the identification of BTB-1 (see picture), the first small-molecule inhibitor of the mitotic motor protein Kif18A. BTB-1 reversibly inhibits the ATPase activity of the recombinant motor domain of Kif18A in vitro (see picture; red microtubules, blue/black structure = Kif18A) and will be a valuable tool to dissect the mechanochemical properties of Kif18A. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：9072 / 9076

页数：5

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