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
收藏
页码：9072 / 9076
页数：5
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