Glucagon-like peptide 1 receptor

Exenatide (synthetic exendin-4, from the saliva from a lizard), which has a 53% overlap with glucagon-like peptide-1 and which also binds to the glucagon-like peptide-1 receptor, has been investigated in a placebo-controlled study for 28 days in 116 patients with type 2 diabetes in addition to a sulfonylurea or metformin (1). The most common adverse effects were nausea (mostly only in the first week) and mild to moderate hypoglycemia, for which no treatment was needed. 

Sinclair EM, Drucker DJ. Glucagon-like peptide 1 receptor agonists and dipeptidyl peptidase IV inhibitors new therapeutic agents for the treatment of type 2 diabetes. Curr Opin Endocrinol Diabetes 2005 12 146-51. 

Widmann C, Burki E, Dolci W, et al. (1994) Signal transduction by the cloned glucagon-like peptide-1 receptor comparison with signaling by the endogenous receptors of beta cell lines. In Mol. Pharmacol. 45 1029—35. 

Burcelin R, Da Costa A, Drucker D, Thorens B. Glucose competence of the hepatoportal vein sensor reqnires the presence of an activated glucagon-like peptide-1 receptor. Diabetes 2001 50 1720-1728. 

Scrocchi LA, Brown TJ, MaClusky N, Brubaker PL, Auerbach AB, Joyner AL, et al. Glncose intolerance bnt normal satiety in mice with a nnU mutation in the glucagon-like peptide 1 receptor gene. Nat Med 1996 2 1254-1258. 

Kim JG, Baggio LL, Bridon DP, Castaigne JP, RobitaUle ME, Jette L, et al. Development and characterization of a glucagon-hke peptide 1-albumin conjugate the abihty to activate the glucagon-like peptide 1 receptor in vivo. Diabetes 2003 52 751-759. 

Gros R, You X, Baggio LL, Kabir MG, Sadi AM, Mungrue IN, et al. Cardiac function in mice lacking the glucagon-like peptide-1 receptor. Endocrinology 2003 144 2242-2252. 

Drucker DJ, Nauck MA. The incretin system glucagon-like peptide-1 receptor agonists and dipep-tidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 2006 368 1696-1705. 

Jorgensen, R., Martini, L., Schwartz, T. W., Filing, C. E. (2005). Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction A high-alEnity receptor phenotype. Molecular Endocrinology, 19(3), 812—823. http //dx.doi.org/10.1210/ tne.2004-0312. 

Glucagon Like Peptide-1 Receptor-Targeted Nanoparticles... 

Li W-X, Gou J-F, Tian J-H, Yan X, Yang L. Glucagon-like peptide 1 receptor agonists versus insulin glargine for type 2 diabetes mellitus a systematic review and meta-analysis of randomized controlled trials. Curr Ther Res 2010 71 211-37. 

Monami M, Marchionni N, Mannucci E. Glucagon-like peptide 1 receptor agonists in type 2 diabetes a meta-analysis of randomized clinical trials. Eur J Endocrinol 2009 160 909-17. 

Cani PD, Knauf C, Iglesias MA, Drucker DJ, Delzerme NM, Burcelin R. Improvement of glucose tolerance and hepatic insulin sensitivity by oligofructose requires a functional glucagon-like peptide 1 receptor. Diabetes. 2006 55 1484-1490. 

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