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

TitleIdentification of a molecular activator for insulin receptor with potent anti-diabetic effects
Authors
Issue Date2011
Citation
Journal of Biological Chemistry, 2011, v. 286, n. 43, p. 37379-37388 How to Cite?
AbstractInsulin 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.Tosearch 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. © 2011 by The American Society for Biochemistry and Molecular Biology, Inc.
Persistent Identifierhttp://hdl.handle.net/10722/225048
ISSN
2015 Impact Factor: 4.258
2015 SCImago Journal Rankings: 3.151

 

DC FieldValueLanguage
dc.contributor.authorHe, Kunyan-
dc.contributor.authorChan, Chi Bun-
dc.contributor.authorLiu, Xia-
dc.contributor.authorJia, Yonghui-
dc.contributor.authorLuo, Hongbo R.-
dc.contributor.authorFrance, Stefan A.-
dc.contributor.authorLiu, Yang-
dc.contributor.authorWilson, W. David-
dc.contributor.authorYe, Keqiang-
dc.date.accessioned2016-04-18T11:16:37Z-
dc.date.available2016-04-18T11:16:37Z-
dc.date.issued2011-
dc.identifier.citationJournal of Biological Chemistry, 2011, v. 286, n. 43, p. 37379-37388-
dc.identifier.issn0021-9258-
dc.identifier.urihttp://hdl.handle.net/10722/225048-
dc.description.abstractInsulin 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.Tosearch 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. © 2011 by The American Society for Biochemistry and Molecular Biology, Inc.-
dc.languageeng-
dc.relation.ispartofJournal of Biological Chemistry-
dc.titleIdentification of a molecular activator for insulin receptor with potent anti-diabetic effects-
dc.typeArticle-
dc.description.natureLink_to_subscribed_fulltext-
dc.identifier.doi10.1074/jbc.M111.247387-
dc.identifier.pmid21908618-
dc.identifier.scopuseid_2-s2.0-80054825497-
dc.identifier.volume286-
dc.identifier.issue43-
dc.identifier.spage37379-
dc.identifier.epage37388-
dc.identifier.eissn1083-351X-

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