Isoform-selective chemical inhibition of mDia-mediated actin assembly.
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ABSTRACT:
SUBMITTER: Gauvin TJ
PROVIDER: S-EPMC2758331 | biostudies-literature | 2009 Oct
REPOSITORIES: biostudies-literature
Publications
Isoform-selective chemical inhibition of mDia-mediated actin assembly.
Gauvin Timothy J TJ Fukui Jami J Peterson Jeffrey R JR Higgs Henry N HN
Biochemistry 20091001 40
Formins are potent actin assembly factors. Diaphanous formins, including mDia1, 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 mDia1 and identified an inhibitor of mDia1 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. ...[more]
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