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    J Biol Chem. 2011 Oct 28;286(43):37379-88. Epub 2011 Sep 9.

    Identification of a molecular activator for insulin receptor with potent anti-diabetic effects.

    He K, Chan CB, Liu X, Jia Y, Luo HR, France SA, Liu Y, Wilson WD, Ye K.

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    Department of Pathology and Laboratory Medicine, Emory University School of Medicine, Atlanta, Georgia 30322, USA.

    Erratum in

    • J Biol Chem. 2012 Apr 13;287(16):13050.

    Abstract

    Insulin exerts its actions through the insulin receptor (IR) and plays an essential role in diabetes. The inconvenient daily injection and undesirable side-effects associated with insulin injection demand novel drugs for the diseases. To search for bioactive insulin mimetics, we developed an in vitro screening assay using phospho-IR ELISA. After screening the small molecule chemical libraries, we have obtained a compound (5,8-diacetyloxy-2,3-dichloro-1,4-naphthoquinone) that provokes IR activation by directly binding to the receptor kinase domain to trigger its kinase activity at micromolar concentrations. This compound selectively activates IR but not other receptors and sensitizes insulin's action. Moreover, it elevates glucose uptake in adipocytes and has oral hypoglycemic effect in wild-type C57BL/6J mice and db/db and ob/ob mice without demonstrable toxicity. Hence, this promising compound mimics the biological functions of insulin and is useful for further drug development for diabetes treatment.

    PMID:
    21908618
    [PubMed - indexed for MEDLINE]
    PMCID:
    PMC3199485
    [Available on 2012/10/28]

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