Glucagon-like Peptide-1 Receptor (GLP1R) binds Glucagon-like peptide-1

Stable Identifier
Homo sapiens
Locations in the PathwayBrowser

Glucagon-like Peptide-1 is synthesized in intestinal L-cells in response to the presence of glucose and fatty acids absorbed from the intestine. Most GLP-1 is the GLP-1 (7-36) amidated form; some GLP-1 is the GLP-1 (7-37) form. GLP-1 circulates to the pancreas where it binds the Glucagon-like Peptide-1 Receptor (GLP-1R), a G-protein coupled receptor located on the plasma membrane of beta cells. GLP-1R is a seven-pass transmembrane protein and a member of the B family of GPCRs, which have N-terminal extracellular domains of 100-150 amino acids. GLP-1 interacts with the extracellular N-terminal region of GLP-1R.

Literature References
PubMed ID Title Journal Year
7589461 Stimulation of cloned human glucagon-like peptide 1 receptor expressed in HEK 293 cells induces cAMP-dependent activation of calcium-induced calcium release

Gromada, J, Rorsman, P, Dissing, S, Wulff, BS

FEBS Lett 1995
8404634 Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor

Dillon, JS, Tanizawa, Y, Wheeler, MB, Leng, XH, Ligon, BB, Rabin, DU, Yoo-Warren, H, Permutt, MA, Boyd AE, 3rd

Endocrinology 1993
15569269 Glucagon-like peptide-1: regulation of insulin secretion and therapeutic potential

Gromada, J, Brock, B, Schmitz, O, Rorsman, P

Basic Clin Pharmacol Toxicol 2004
12034449 In vitro folding, functional characterization, and disulfide pattern of the extracellular domain of human GLP-1 receptor

Bazarsuren, A, Grauschopf, U, Wozny, M, Reusch, D, Hoffmann, E, Schaefer, W, Panzner, S, Rudolph, R

Biophys Chem 2002
18287102 Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain

Runge, S, Thøgersen, H, Madsen, K, Lau, J, Rudolph, R

J Biol Chem 2008
19861722 Crystal structure of glucagon-like peptide-1 in complex with the extracellular domain of the glucagon-like peptide-1 receptor

Underwood, CR, Garibay, P, Knudsen, LB, Hastrup, S, Peters, GH, Rudolph, R, Reedtz-Runge, S

J Biol Chem 2009
8405712 Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor

Thorens, B, Porret, A, Buhler, L, Deng, SP, Morel, P, Widmann, C

Diabetes 1993
8138058 Tissue and plasma concentrations of amidated and glycine-extended glucagon-like peptide I in humans

Orskov, C, Rabenhøj, L, Wettergren, A, Kofod, H, Holst, JJ

Diabetes 1994
17306374 Mechanisms of action of glucagon-like peptide 1 in the pancreas

Doyle, ME, Egan, JM

Pharmacol Ther 2007
17444618 Differential structural properties of GLP-1 and exendin-4 determine their relative affinity for the GLP-1 receptor N-terminal extracellular domain

Runge, S, Schimmer, S, Oschmann, J, Schiødt, CB, Knudsen, SM, Jeppesen, CB, Madsen, K, Lau, J, Thøgersen, H, Rudolph, R

Biochemistry 2007
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