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Biological Chemistry

Editor-in-Chief: Brüne, Bernhard

Editorial Board Member: Buchner, Johannes / Ludwig, Stephan / Sies, Helmut / Turk, Boris / Wittinghofer, Alfred

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Characterisation and glucoregulatory actions of a novel acylated form of the (Pro3)GIP receptor antagonist in type 2 diabetes

Victor A. Gault1 / Kerry Hunter2 / Nigel Irwin3 / Brett Greer4 / Brian D. Green5 / Patrick Harriott6 / Finbarr P.M. O'Harte7 / Peter R. Flatt8









Corresponding author

Citation Information: Biological Chemistry. Volume 388, Issue 2, Pages 173–179, ISSN (Online) 1437-4315, ISSN (Print) 1431-6730, DOI: 10.1515/BC.2007.019, January 2007

Publication History

June 21, 2006
September 29, 2006
Published Online:


In this study, we tested the biological activity of a novel acylated form of (Pro3)glucose-dependent insulinotropic polypetide [(Pro3)GIP] prepared by conjugating palmitic acid to Lys16 to enhance its efficacy in vivo by promoting binding to albumin and extending its biological actions. Like the parent molecule (Pro3)GIP, (Pro3)GIPLys16PAL was completely stable to the actions of DPP-IV and significantly (p<0.01 to p<0.001) inhibited GIP-stimulated cAMP production and cellular insulin secretion. Furthermore, acute administration of (Pro3)GIPLys16PAL also significantly (p<0.05 to p<0.001) countered the glucose-lowering and insulin-releasing actions of GIP in ob/ob mice. Daily injection of (Pro3)GIPLys16PAL (25 nmol/kg bw) in 14–18-week-old ob/ob mice over 14 days had no effect on body weight, food intake or non-fasting plasma glucose and insulin concentrations. (Pro3)GIPLys16PAL treatment also failed to significantly alter the glycaemic response to an i.p. glucose load or test meal, but insulin concentrations were significantly reduced (1.5-fold; p<0.05) after the glucose load. Insulin sensitivity was enhanced (1.3-fold; p<0.05) and pancreatic insulin was significantly reduced (p<0.05) in the (Pro3)GIPLys16PAL-treated mice. These data demonstrate that acylation of Lys16 with palmitic acid in (Pro3)GIP does not improve its biological effectiveness as a GIP receptor antagonist.

Keywords: antihyperglycaemic activity; DPP IV; fatty acid-linked peptides; GIP receptor antagonists; insulin secretion; obese diabetic (ob/ob) mice

Citing Articles

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P L McClean, N Irwin, K Hunter, V A Gault, and P R Flatt
British Journal of Pharmacology, 2009, Volume 155, Number 5, Page 690
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Cell Biochemistry and Biophysics, 2010, Volume 56, Number 2-3, Page 59

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