Glucagon-like peptide 1 receptor

edit

Glucagon-like peptide 1 receptor
Identifiers
Symbols	GLP1R; MGC138331
External IDs	OMIM: 138032 MGI: 99571 HomoloGene: 1558 IUPHAR: GLP-1 GeneCards: GLP1R Gene
Gene Ontology Molecular function • G-protein coupled receptor activity • glucagon receptor activity • peptide receptor activity, G-protein coupled Cellular component • plasma membrane • integral to membrane Biological process • response to stress • signal transduction • G-protein coupled receptor protein signaling pathway • adenylate cyclase activation • elevation of cytosolic calcium ion concentration • learning and/or memory • regulation of heart contraction • cAMP-mediated signaling Sources: Amigo / EGO
RNA expression pattern
250px
250px
250px
More reference expression data
Orthologs
Species	Human	Mouse
Entrez	2740	14652
Ensembl	ENSG00000112164	ENSMUSG00000024027
UniProt	P43220	Q104P0
RefSeq (mRNA)	NM_002062	XM_001000702
RefSeq (protein)	NP_002053	XP_001000702
Location (UCSC)	Chr 6: 39.12 - 39.16 Mb	Chr 17: 30.63 - 30.66 Mb
PubMed search	[1]	[2]

The glucagon-like peptide 1 receptor (GLP1R) is a human gene which resides on chromosome 6. The protein encoded by this gene is a member of the glucagon receptor family of G protein-coupled receptors.

Ligand specificity

GLP1R binds specifically the glucagon-like peptide-1 (GLP1) and has much lower affinity for related peptides such as the gastric inhibitory polypeptide and glucagon.

Function and therapeutic potential

GLP1R is known to be expressed in pancreatic beta cells. Activated GLP1R stimulates the adenylyl cyclase pathway which results in increased insulin synthesis and release of insulin. Consequently GLP1R has been suggested as a potential target for the treatment of diabetes.

GLP1R is also expressed in the brain where it is involved in the control of appetite. Furthermore, mice which over express GLP1R display improved memory and learning.

See also

• Glucagon-like peptide-1
• Dipeptidyl peptidase-4

Further reading

• van Eyll B, Lankat-Buttgereit B, Bode HP; et al. (1994). "Signal transduction of the GLP-1-receptor cloned from a human insulinoma". FEBS Lett. 348 (1): 7–13. doi:10.1016/0014-5793(94)00553-2. PMID 7517895. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Gromada J, Rorsman P, Dissing S, Wulff BS (1995). "Stimulation of cloned human glucagon-like peptide 1 receptor expressed in HEK 293 cells induces cAMP-dependent activation of calcium-induced calcium release". FEBS Lett. 373 (2): 182–6. doi:10.1016/0014-5793(95)01070-U. PMID 7589461. CS1 maint: Multiple names: authors list (link)
• Wei Y, Mojsov S (1995). "Tissue-specific expression of the human receptor for glucagon-like peptide-I: brain, heart and pancreatic forms have the same deduced amino acid sequences". FEBS Lett. 358 (3): 219–24. doi:10.1016/0014-5793(94)01430-9. PMID 7843404. 
• Lankat-Buttgereit B, Göke R, Stöckmann F; et al. (1994). "Detection of the human glucagon-like peptide 1(7-36) amide receptor on insulinoma-derived cell membranes". Digestion. 55 (1): 29–33. doi:10.1159/000201119. PMID 8112494. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Graziano MP, Hey PJ, Borkowski D; et al. (1993). "Cloning and functional expression of a human glucagon-like peptide-1 receptor". Biochem. Biophys. Res. Commun. 196 (1): 141–6. doi:10.1006/bbrc.1993.2226. PMID 8216285. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Stoffel M, Espinosa R, Le Beau MM, Bell GI (1993). "Human glucagon-like peptide-1 receptor gene. Localization to chromosome band 6p21 by fluorescence in situ hybridization and linkage of a highly polymorphic simple tandem repeat DNA polymorphism to other markers on chromosome 6". Diabetes. 42 (8): 1215–8. doi:10.2337/diabetes.42.8.1215. PMID 8392011. CS1 maint: Multiple names: authors list (link)
• Dillon JS, Tanizawa Y, Wheeler MB; et al. (1993). "Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor". Endocrinology. 133 (4): 1907–10. doi:10.1210/en.133.4.1907. PMID 8404634. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Thorens B, Porret A, Bühler L; et al. (1993). "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". Diabetes. 42 (11): 1678–82. doi:10.2337/diabetes.42.11.1678. PMID 8405712. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Lankat-Buttgereit B, Göke B (1997). "Cloning and characterization of the 5' flanking sequences (promoter region) of the human GLP-1 receptor gene". Peptides. 18 (5): 617–24. doi:10.1016/S0196-9781(97)00001-6. PMID 9213353. 
• Frimurer TM, Bywater RP (1999). "Structure of the integral membrane domain of the GLP1 receptor". Proteins. 35 (4): 375–86. doi:10.1002/(SICI)1097-0134(19990601)35:4<375::AID-PROT1>3.0.CO;2-2. PMID 10382665. 
• Huypens P, Ling Z, Pipeleers D, Schuit F (2001). "Glucagon receptors on human islet cells contribute to glucose competence of insulin release". Diabetologia. 43 (8): 1012–9. doi:10.1007/s001250051484. PMID 10990079. CS1 maint: Multiple names: authors list (link)
• Hartley JL, Temple GF, Brasch MA (2001). "DNA cloning using in vitro site-specific recombination". Genome Res. 10 (11): 1788–95. doi:10.1101/gr.143000. PMC 310948 Freely accessible. PMID 11076863. CS1 maint: Multiple names: authors list (link)
• Xiao Q, Jeng W, Wheeler MB (2001). "Characterization of glucagon-like peptide-1 receptor-binding determinants". J. Mol. Endocrinol. 25 (3): 321–35. doi:10.1677/jme.0.0250321. PMID 11116211. CS1 maint: Multiple names: authors list (link)
• Bazarsuren A, Grauschopf U, Wozny M; et al. (2003). "In vitro folding, functional characterization, and disulfide pattern of the extracellular domain of human GLP-1 receptor". Biophys. Chem. 96 (2-3): 305–18. doi:10.1016/S0301-4622(02)00023-6. PMID 12034449. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Strausberg RL, Feingold EA, Grouse LH; et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241 Freely accessible. PMID 12477932. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Mungall AJ, Palmer SA, Sims SK; et al. (2003). "The DNA sequence and analysis of human chromosome 6". Nature. 425 (6960): 805–11. doi:10.1038/nature02055. PMID 14574404. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Tokuyama Y, Matsui K, Egashira T; et al. (2005). "Five missense mutations in glucagon-like peptide 1 receptor gene in Japanese population". Diabetes Res. Clin. Pract. 66 (1): 63–9. doi:10.1016/j.diabres.2004.02.004. PMID 15364163. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Gerhard DS, Wagner L, Feingold EA; et al. (2004). "The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)". Genome Res. 14 (10B): 2121–7. doi:10.1101/gr.2596504. PMC 528928 Freely accessible. PMID 15489334. CS1 maint: Explicit use of et al. (link) CS1 maint: Multiple names: authors list (link)
• Jorgensen R, Martini L, Schwartz TW, Elling CE (2005). "Characterization of glucagon-like peptide-1 receptor beta-arrestin 2 interaction: a high-affinity receptor phenotype". Mol. Endocrinol. 19 (3): 812–23. doi:10.1210/me.2004-0312. PMID 15528268. CS1 maint: Multiple names: authors list (link)
• Mahon MJ, Shimada M (2005). "Calmodulin interacts with the cytoplasmic tails of the parathyroid hormone 1 receptor and a sub-set of class b G-protein coupled receptors". FEBS Lett. 579 (3): 803–7. doi:10.1016/j.febslet.2004.12.056. PMID 15670850. 

External links

• "Glucagon Receptor Family: GLP-1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 
• MeSH glucagon-like+peptide+receptor