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    Biochemistry. 2009 Oct 13;48(40):9327-9.

    Isoform-selective chemical inhibition of mDia-mediated actin assembly.

    Source

    Department of Biochemistry, Dartmouth Medical School, Hanover, New Hampshire 03755, USA.

    Abstract

    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.

    PMID:
    19764708
    [PubMed - indexed for MEDLINE]
    PMCID: PMC2758331
    Free PMC Article

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