Structure/function studies of glucagon-like peptide-1 and exendin 4
نویسنده
چکیده
The GLP-1 receptor and its peptide ligands. Glucagon-like peptide 1 (7-36) amide (GLP-1) is a 30 amino acid peptide produced in intestinal L cells and released into the bloodstream in response to food intake. It is a potent ‘incretin’, in that it increases glucose-dependent secretion of insulin by pancreatic β-cells. GLP-1 has also been shown to stimulate pro-insulin gene transcription in the pancreatic β-cells, slow down gastric emptying time and reduce food intake. As a result of these actions, GLP-1 has received much attention as a possible therapeutic agent in the treatment of type II diabetes and obesity. Unlike the sulphonylureas, the actions of GLP-1 are glucose-dependent and do not produce hypoglycemic side effects. However, GLP-1 is rapidly degraded in vivo by dipeptidyl peptidase IV (DPP IV), and has a half-life of 2 min. Hence, future therapeutic agents would have to be physiologically more stable than GLP-1.
منابع مشابه
Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain.
The glucagon-like peptide-1 receptor (GLP-1R) belongs to Family B1 of the seven-transmembrane G protein-coupled receptors, and its natural agonist ligand is the peptide hormone glucagon-like peptide-1 (GLP-1). GLP-1 is involved in glucose homeostasis, and activation of GLP-1R in the plasma membrane of pancreatic beta-cells potentiates glucose-dependent insulin secretion. The N-terminal extracel...
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