Glucagon-like polypeptide

The most modern technologies have been utilized to discover a way of exploiting the possibility of GLP-1 (glucagon-like polypeptide 1) for the treatment of NIDDM. This demonstrates how discoveries of novel binding pockets... 

Antidiabetic Drugs other than Insulin. Table 3 Actions of the incretin hormones GIP (glucose-dependent insulinotropic polypeptide, gastric inhibitory peptide) and GLP-1 (glucagon-like peptide-1)... 

R. P. Pauly, F. Rosche, M. Wermann, C. H. McIntosh, R. A. Pederson, and H. U. Demuth. Investigation of Glucose-Dependent Insulinotropic Polypeptide-(l-42) and Glucagon-like Peptide-1-(7-36) Degradation In Vitro by Dipeptidyl Peptidase IV Using Matrix-Assisted... 

Improved stability with simultaneous preservation of activity has been demonstrated with analogues of glucagon-like peptide-1 and gastric inhibitory polypeptide, two hormones that stimulate the release of insulin. Glucagon-like peptide-1 (GLP-1) is a 30-residue gastrointestinal hormone, ami-dated at the C-terminus that has potential as a treatment for type-2 diabetes. However, GLP-1 is rapidly degraded by dipeptidyl-peptidase IV (EC... 

The approval of sitagliptin (1) by the U.S. FDA in 2006 established dipeptidyl peptidase IV (DPP-4) inhibitors as an important new therapy for the treatment of type 2 diabetes.4 7 DPP-4 inhibitors stimulate insulin secretion indirectly by enhancing the action of the incretin hormones glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (G1P). GLP-1 and G1P stimulate insulin secretion in a... 

Fig. 1. Peptide structures of the two main incretin hormones, glucose-dependent insulinotropic polypeptide (gastric inhibitory polypeptide, GIP), and glucagon-like peptide 1 (GLP-1). Amino acids shared between both peptides are shown in dark blue, and amino acids unique to GIP and GLP-1 are shown in light and dark green, respectively. The red arrow indicates the position of cleavage by dipeptidyl peptidase-4 (DPP-4), the alanine residue in position 2, which is recognized by DPP-4, is highlighted by a red margin.

Nauck MA, Bartels E, 0rskov C, Ebert R, Creutzfeldt W. Additive insulinotropic effects of exogenous synthetic human gastric inhibitory polypeptide and glucagon-like peptide-l-(7-36) amide infused at near-physiological insulinotropic hormone and glucose concentrations. J Clin Endocrinol Metab 1993 76 912-917. 

Mentlein R, Gallwitz B, Schmidt WE. Dipeptidyl-peptidase IV hydrolyses gastric inhihitory polypeptide, glucagon-like peptide-1 (7-36) amide, peptide histidine methionine and is responsible for then-degradation in human serum. Eur 1 Biochem 1993 214 829-835. 

Meier 11, Nauck MA, Kranz D, Holst 11, Deacon CF, Gaeckler D, et al. Secretion, degradation, and elimination of glucagon-like peptide 1 and gastric inhibitory polypeptide in patients with chronic renal insufficiency and healthy control subjects. Diabetes 2004 53 654-662. 

Ding WG, Renstrom E, Rorsman P, Bnschard K, Gromada J. Glucagon-like peptide I and glncose-dependent insulinotropic polypeptide stimulate Ca2H-induced secretion in rat alpha-cells by a protein kinase A-mediated mechanism. Diabetes 1997 46 792-800. 

Fehmann HC, Gdke R, Goke B. Cell and molecular biology of the incretin hormones glucagon-like peptide-I and glucose-dependent insulin releasing polypeptide. EndocrRev 1995 16 390-410. 

Hlebowicz, J., A. Hlebowicz, S. Lindstedt, et al. 2009. Effects of 1 and 3 g cinnamon on gastric emptying, satiety, and postprandial blood glucose, insulin, glucose-dependent insulinotropic polypeptide, glucagon-like peptide 1, and ghrelin concentrations in healthy subjects. Am. J. Clin. Nutr. 89(3) 815-821. 

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