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Dipeptidyl peptidase-IV (DPP-IV) is an enzyme responsible for the inactivation of the glucoregulatory incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). In this report, we show that the hypolipidemic agent atorvastatin is a competitive inhibitor of porcine DPP-IV in vitro, with K(i)=57.8+/-2.3 microM. These results may have implications in the development of novel DPP-IV inhibitors based on the use of atorvastatin as a lead compound for the treatment of type 2 diabetes.

Citation

Tony Taldone, S William Zito, Tanaji T Talele. Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin. Bioorganic & medicinal chemistry letters. 2008 Jan 15;18(2):479-84

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PMID: 18068977

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