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Gene Review

GLP1R  -  glucagon-like peptide 1 receptor

Homo sapiens

Synonyms: GLP-1 receptor, GLP-1-R, GLP-1R, Glucagon-like peptide 1 receptor
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Disease relevance of GLP1R


Psychiatry related information on GLP1R


High impact information on GLP1R


Biological context of GLP1R


Anatomical context of GLP1R


Associations of GLP1R with chemical compounds

  • The human GLP-1 receptor is functionally coupled to increases in intracellular cAMP in these cells: incubation of COS-7 cells expressing the human GLP-1 receptor with GLP-1 (7-36) amide gives rise to a 4-fold increase in cyclic AMP over basal levels, with an EC50 of 25pM [16].
  • A GLP-1 receptor (GLP-1R) polymorphism in which threonine 149 is substituted with a methionine residue has been recently identified in a patient with type 2 diabetes but was not found in non-diabetic control subjects [19].
  • Regulation of glucagon-like peptide-1 receptor and calcium-sensing receptor signaling by L-histidine [20].
  • Furthermore, the observation that T-0632 has almost 100-fold selectivity for the human versus the highly homologous rat GLP-1R provided an opportunity to map determinants of non-peptide binding [21].
  • A series of analogs of glucagon-like peptide-1 (GLP-1) was made replacing each amino acid with L-alanine to identify side-chain functional groups required for interaction with the GLP-1 receptor [22].

Physical interactions of GLP1R

  • The GLP-1R NT protein attached to beads bound GLP-1, but with lower affinity (inhibitory concentration (IC(50)): 4.5 x 10(-7) M) than wild-type (WT) GLP-1R (IC(50): 5.2 x 10(-9)M) [23].
  • Immunoprecipitation, sucrose sedimentation, and microscopy observations demonstrated that the GLP-1R localizes in lipid rafts and interacts with caveolin-1 [24].

Regulatory relationships of GLP1R


Other interactions of GLP1R


Analytical, diagnostic and therapeutic context of GLP1R


  1. Signal transduction of the GLP-1-receptor cloned from a human insulinoma. van Eyll, B., Lankat-Buttgereit, B., Bode, H.P., Göke, R., Göke, B. FEBS Lett. (1994) [Pubmed]
  2. 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) [Pubmed]
  3. Glucagon-like peptide-1 structure, function and potential use for NIDDM. Gefel, D., Barg, Y., Zimlichman, R. Isr. J. Med. Sci. (1997) [Pubmed]
  4. Non-linkage of the glucagon-like peptide 1 receptor gene with maturity onset diabetes of the young. Zhang, Y., Cook, J.T., Hattersley, A.T., Firth, R., Saker, P.J., Warren-Perry, M., Stoffel, M., Turner, R.C. Diabetologia (1994) [Pubmed]
  5. Engineering physiologically regulated insulin secretion in non-beta cells by expressing glucagon-like peptide 1 receptor. Wu, L., Nicholson, W., Wu, C.Y., Xu, M., McGaha, A., Shiota, M., Powers, A.C. Gene Ther. (2003) [Pubmed]
  6. Peripheral exendin-4 and peptide YY(3-36) synergistically reduce food intake through different mechanisms in mice. Talsania, T., Anini, Y., Siu, S., Drucker, D.J., Brubaker, P.L. Endocrinology (2005) [Pubmed]
  7. Antiobesity action of peripheral exenatide (exendin-4) in rodents: effects on food intake, body weight, metabolic status and side-effect measures. Mack, C.M., Moore, C.X., Jodka, C.M., Bhavsar, S., Wilson, J.K., Hoyt, J.A., Roan, J.L., Vu, C., Laugero, K.D., Parkes, D.G., Young, A.A. International journal of obesity (2005) (2006) [Pubmed]
  8. Enhancing central nervous system endogenous GLP-1 receptor pathways for intervention in Alzheimer's disease. Perry, T., Greig, N.H. Current Alzheimer research. (2005) [Pubmed]
  9. The Xenopus proglucagon gene encodes novel GLP-1-like peptides with insulinotropic properties. Irwin, D.M., Satkunarajah, M., Wen, Y., Brubaker, P.L., Pederson, R.A., Wheeler, M.B. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  10. Design of a Long Acting Peptide Functioning as Both a Glucagon-like Peptide-1 Receptor Agonist and a Glucagon Receptor Antagonist. Pan, C.Q., Buxton, J.M., Yung, S.L., Tom, I., Yang, L., Chen, H., Macdougall, M., Bell, A., Claus, T.H., Clairmont, K.B., Whelan, J.P. J. Biol. Chem. (2006) [Pubmed]
  11. Improvement of glucose tolerance and hepatic insulin sensitivity by oligofructose requires a functional glucagon-like Peptide 1 receptor. Cani, P.D., Knauf, C., Iglesias, M.A., Drucker, D.J., Delzenne, N.M., Burcelin, R. Diabetes (2006) [Pubmed]
  12. Leptin regulation of the anorexic response to glucagon-like Peptide-1 receptor stimulation. Williams, D.L., Baskin, D.G., Schwartz, M.W. Diabetes (2006) [Pubmed]
  13. Activation of glucagon-like Peptide-1 receptor signaling does not modify the growth or apoptosis of human pancreatic cancer cells. Koehler, J.A., Drucker, D.J. Diabetes (2006) [Pubmed]
  14. 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. Stoffel, M., Espinosa, R., Le Beau, M.M., Bell, G.I. Diabetes (1993) [Pubmed]
  15. The expression of GLP-1 receptor mRNA and protein allows the effect of GLP-1 on glucose metabolism in the human hypothalamus and brainstem. Alvarez, E., Martínez, M.D., Roncero, I., Chowen, J.A., García-Cuartero, B., Gispert, J.D., Sanz, C., Vázquez, P., Maldonado, A., de Cáceres, J., Desco, M., Pozo, M.A., Blázquez, E. J. Neurochem. (2005) [Pubmed]
  16. Cloning and functional expression of a human glucagon-like peptide-1 receptor. Graziano, M.P., Hey, P.J., Borkowski, D., Chicchi, G.G., Strader, C.D. Biochem. Biophys. Res. Commun. (1993) [Pubmed]
  17. 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., Bühler, L., Deng, S.P., Morel, P., Widmann, C. Diabetes (1993) [Pubmed]
  18. Agonist-induced internalization and recycling of the glucagon-like peptide-1 receptor in transfected fibroblasts and in insulinomas. Widmann, C., Dolci, W., Thorens, B. Biochem. J. (1995) [Pubmed]
  19. A human glucagon-like peptide-1 receptor polymorphism results in reduced agonist responsiveness. Beinborn, M., Worrall, C.I., McBride, E.W., Kopin, A.S. Regul. Pept. (2005) [Pubmed]
  20. Regulation of glucagon-like peptide-1 receptor and calcium-sensing receptor signaling by L-histidine. Leech, C.A., Habener, J.F. Endocrinology (2003) [Pubmed]
  21. A small molecule ligand of the glucagon-like peptide 1 receptor targets its amino-terminal hormone binding domain. Tibaduiza, E.C., Chen, C., Beinborn, M. J. Biol. Chem. (2001) [Pubmed]
  22. Structure-activity studies of glucagon-like peptide-1. Adelhorst, K., Hedegaard, B.B., Knudsen, L.B., Kirk, O. J. Biol. Chem. (1994) [Pubmed]
  23. Characterization of glucagon-like peptide-1 receptor-binding determinants. Xiao, Q., Jeng, W., Wheeler, M.B. J. Mol. Endocrinol. (2000) [Pubmed]
  24. Caveolin-1 regulates cellular trafficking and function of the glucagon-like Peptide 1 receptor. Syme, C.A., Zhang, L., Bisello, A. Mol. Endocrinol. (2006) [Pubmed]
  25. Enhancing incretin action for the treatment of type 2 diabetes. Drucker, D.J. Diabetes Care (2003) [Pubmed]
  26. Different domains of the glucagon and glucagon-like peptide-1 receptors provide the critical determinants of ligand selectivity. Runge, S., Wulff, B.S., Madsen, K., Bräuner-Osborne, H., Knudsen, L.B. Br. J. Pharmacol. (2003) [Pubmed]
  27. Human glucagon-like peptide-1 receptor gene in NIDDM. Identification and use of simple sequence repeat polymorphisms in genetic analysis. Tanizawa, Y., Riggs, A.C., Elbein, S.C., Whelan, A., Donis-Keller, H., Permutt, M.A. Diabetes (1994) [Pubmed]
  28. Glucagon and glucagon-like peptide receptors as drug targets. Estall, J.L., Drucker, D.J. Curr. Pharm. Des. (2006) [Pubmed]
  29. Biological activities of glucagon-like peptide-1 analogues in vitro and in vivo. Xiao, Q., Giguere, J., Parisien, M., Jeng, W., St-Pierre, S.A., Brubaker, P.L., Wheeler, M.B. Biochemistry (2001) [Pubmed]
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