Glucagon-like peptide 1 receptor

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Function

Glucagon-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].

Relevance

GLP-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 highlights

The 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:

3D structures of glucagon-like peptide receptor

Glucagon-like peptide receptor 3D structures

References

  1. ↑ 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
  2. ↑ 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
  3. ↑ 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
  4. ↑ 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

Human GLP-1R extracellular domain (deepskyblue) complex with GLP-1 peptide (green) and a pyranose derivative (PDB code 3iol)

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