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Article: Identification of a small molecular insulin receptor agonist with potent antidiabetes activity

TitleIdentification of a small molecular insulin receptor agonist with potent antidiabetes activity
Authors
Issue Date2014
Citation
Diabetes, 2014, v. 63, n. 4, p. 1394-1409 How to Cite?
AbstractInsulin replacement therapy is a widely adopted treatment for all patients with type 1 diabetes and some with type 2 diabetes. However, injection of insulin has suffered from problems such as tissue irritation, abscesses, discomfort, and inconvenience. The use of orally bioactive insulin mimetics thus represents an ideal treatment alternative. Here we show that a chaetochromin derivative (4548-G05) acts as a new nonpeptidyl insulin mimetic. 4548-G05 selectively activates an insulin receptor (IR) but not insulin-like growth factor receptor-I or other receptor tyrosine kinases. Through binding to the extracellular domain of the IR, 4548-G05 induces activation of the receptor and initiates the downstream Akt and extracellular signal-related kinase pathways to trigger glucose uptake in C2C12 myotubes. Moreover, it displays a potent blood glucose-lowering effect when administrated orally in normal, type 1 diabetic, and type 2 diabetic mice models. Therefore, 4548-G05 may represent a novel pharmacological agent for antidiabetes drug development. © 2014 by the American Diabetes Association.
Persistent Identifierhttp://hdl.handle.net/10722/225059
ISSN
2015 Impact Factor: 8.784
2015 SCImago Journal Rankings: 5.185

 

DC FieldValueLanguage
dc.contributor.authorQiang, Guifen-
dc.contributor.authorXue, Shenghui-
dc.contributor.authorYang, Jenny J.-
dc.contributor.authorDu, Guanhua-
dc.contributor.authorPang, Xiaobin-
dc.contributor.authorLi, Xiaoting-
dc.contributor.authorGoswami, Devrishi-
dc.contributor.authorGriffin, Patrick R.-
dc.contributor.authorOrtlund, Eric A.-
dc.contributor.authorChan, Chi Bun-
dc.contributor.authorYe, Keqiang-
dc.date.accessioned2016-04-18T11:16:39Z-
dc.date.available2016-04-18T11:16:39Z-
dc.date.issued2014-
dc.identifier.citationDiabetes, 2014, v. 63, n. 4, p. 1394-1409-
dc.identifier.issn0012-1797-
dc.identifier.urihttp://hdl.handle.net/10722/225059-
dc.description.abstractInsulin replacement therapy is a widely adopted treatment for all patients with type 1 diabetes and some with type 2 diabetes. However, injection of insulin has suffered from problems such as tissue irritation, abscesses, discomfort, and inconvenience. The use of orally bioactive insulin mimetics thus represents an ideal treatment alternative. Here we show that a chaetochromin derivative (4548-G05) acts as a new nonpeptidyl insulin mimetic. 4548-G05 selectively activates an insulin receptor (IR) but not insulin-like growth factor receptor-I or other receptor tyrosine kinases. Through binding to the extracellular domain of the IR, 4548-G05 induces activation of the receptor and initiates the downstream Akt and extracellular signal-related kinase pathways to trigger glucose uptake in C2C12 myotubes. Moreover, it displays a potent blood glucose-lowering effect when administrated orally in normal, type 1 diabetic, and type 2 diabetic mice models. Therefore, 4548-G05 may represent a novel pharmacological agent for antidiabetes drug development. © 2014 by the American Diabetes Association.-
dc.languageeng-
dc.relation.ispartofDiabetes-
dc.titleIdentification of a small molecular insulin receptor agonist with potent antidiabetes activity-
dc.typeArticle-
dc.description.natureLink_to_subscribed_fulltext-
dc.identifier.doi10.2337/db13-0334-
dc.identifier.pmid24651808-
dc.identifier.scopuseid_2-s2.0-84897841275-
dc.identifier.volume63-
dc.identifier.issue4-
dc.identifier.spage1394-
dc.identifier.epage1409-
dc.identifier.eissn1939-327X-

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