Isoform-Selective Chemical Inhibition of mDia-Mediated Actin Assembly

被引：19

作者：

Gauvin, Timothy J. ^{[1
]}

Fukui, Jami ^{[2
]}

Peterson, Jeffrey R. ^{[2
]}

Higgs, Henry N. ^{[1
]}

机构：

[1] Dartmouth Med Sch, Dept Biochem, Hanover, NH 03755 USA

[2] Fox Chase Canc Ctr, Philadelphia, PA 19111 USA

来源：

BIOCHEMISTRY | 2009年 / 48卷 / 40期

基金：

美国国家卫生研究院;

关键词：

FORMINS; PROTEINS;

D O I：

10.1021/bi901354z

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Formins are potent actin assembly factors. Diaphanous formins, including mDial, mDia2, and mDia3 in mammals, are implicated in mitosis and cytokinesis, but no chemical interactors have been reported. We developed an in vitro screen for inhibitors of actin assembly by mDial and identified an inhibitor of mDial and mDia2 that does not inhibit mDia3 at the concentrations tested. These results establish the druggability of mDia formins and introduce a first-generation inhibitor.

引用

页码：9327 / 9329

页数：3

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