Glucagon-like peptide 1 receptor
FunctionGlucagon-like peptide 1 receptor (GLP-1R) mediates the action of glucagon-like peptides (GLP-1) which are hormones involved in nutrient intake, gastrointestinal motility, islet hormone secretion, cell proliferation and apoptpsis[1]. RelevanceGLP-1R agonists are used in treatment of type 2 diabetes[2]. GLP-1 analogues can cross the brain-blood barrier and stimulate the GLP-1R in the brain. This stimulation is affecting mitochondrial functioning, protein aggregation, neuroinflammation, synaptic plasticity, learning and memory in models of Parkinson Disease and Alzheimer Disease[3]. It is a member of the glucagon receptor family of G protein-coupled receptors. Structural highlightsThe 3D structure of the complex of GLP-1R and GLP-1 shows the GLP-1 peptide as a kinked helix. The ampiphilic GLP-1 helix shows and interactions with GLP-1R on opposite faces[4]. . See also: |
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3D structures of glucagon-like peptide 1 receptor3D structures of glucagon-like peptide 1 receptor
Updated on 04-August-2021
5nx2 - hGLP-1R + peptide agonist - human
6orv - hGLP-1R + agonist - Cryo EM
7lci, 7lcj, 7lck - hGLP-1R + inhibitor - Cryo EM
3iol - hGLP-1R extracellular domain 24-139 + GLP-1
5otu, 5otw, 5otv, 5otx - hGLP-1R extracellular domain 24-139 + GLP-1 (mutant)
5ott, 3c59, 3c5t - hGLP-1R extracellular domain + extendin-4
4zgm - hGLP-1R extracellular domain + semaglutide peptide
6gb1 - hGLP-1R extracellular domain + peptide
5e94 - hGLP-1R extracellular domain + antibody
6ln2 - hGLP-1R/rubredoxin + antibody
5vex - hGLP-1R extracellular domain + modulator
6kk1, 6kk7, 6kjv - hGLP-1R residues 128-437/endolysin (mutant)
5vew - hGLP-1R residues 128-431/endolysin + modulator
7e14 - hGLP-1R + G protein + GS + nanobody + guanine nucleotide-binding protein - Cryo EM
6x19, 6x1a, 7c2e - hGLP-1R + nanobody + guanine nucleotide-binding protein + agonist - Cryo EM
6b3j - hGLP-1R + exendin-p5 + nanobody + guanine nucleotide-binding protein + agonist - Cryo EM
6xox - hGLP-1R + ScfV + nanobody + guanine nucleotide-binding protein + agonist - Cryo EM
7duq - hGLP-1R + GLP-1 + nanobody + guanine nucleotide-binding protein + inhibitor - Cryo EM
6vcb - hGLP-1R + GLP-1 + nanobody + guanine nucleotide-binding protein + modulator - Cryo EM
6x18 - hGLP-1R + glucagon + nanobody + guanine nucleotide-binding protein - Cryo EM
7ki0 - hGLP-1R + semaglutide + nanobody + guanine nucleotide-binding protein - Cryo EM
7ki1 - hGLP-1R + taspoglutide + nanobody + guanine nucleotide-binding protein - Cryo EM
7d68 - hGLP-2R + pro-glucagon + nanobody + guanine nucleotide-binding protein - Cryo EM
ReferencesReferences
- ↑ Brubaker PL, Drucker DJ. Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels. 2002;8(3-4):179-88. PMID:12529935
- ↑ Donnelly D. The structure and function of the glucagon-like peptide-1 receptor and its ligands. Br J Pharmacol. 2012 May;166(1):27-41. doi: 10.1111/j.1476-5381.2011.01687.x. PMID:21950636 doi:http://dx.doi.org/10.1111/j.1476-5381.2011.01687.x
- ↑ Athauda D, Foltynie T. The glucagon-like peptide 1 (GLP) receptor as a therapeutic target in Parkinson's disease: mechanisms of action. Drug Discov Today. 2016 May;21(5):802-18. doi: 10.1016/j.drudis.2016.01.013. Epub, 2016 Feb 3. PMID:26851597 doi:http://dx.doi.org/10.1016/j.drudis.2016.01.013
- ↑ Underwood CR, Garibay P, Knudsen LB, Hastrup S, Peters GH, Rudolph R, Reedtz-Runge S. Crystal structure of glucagon-like peptide-1 in complex with the extracellular domain of the glucagon-like peptide-1 receptor. J Biol Chem. 2010 Jan 1;285(1):723-30. Epub 2009 Oct 27. PMID:19861722 doi:10.1074/jbc.M109.033829