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Gene Review

GLP2R  -  glucagon-like peptide 2 receptor

Homo sapiens

Synonyms: GLP-2 receptor, GLP-2-R, GLP-2R, Glucagon-like peptide 2 receptor
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Disease relevance of GLP2R


High impact information on GLP2R


Biological context of GLP2R


Anatomical context of GLP2R


Associations of GLP2R with chemical compounds

  • Surprisingly, inhibitors of clathrin-dependent endocytosis failed to significantly decrease GLP-2R internalization, whereas cholesterol sequestration inhibited ligand-induced receptor internalization and potentiated homologous desensitization [8].
  • The hGLP-2R localized to both Triton X-100-soluble and -insoluble (lipid raft) cellular fractions and colocalized transiently with the lipid raft marker caveolin-1 [8].
  • In contrast, alanine replacement at positions 5,6,17, 20, 22, 23, 25, 26, 30, and 31 led to diminished GLP-2R binding [9].
  • Position 2 substitutions containing Asp, Leu, Lys, Met, Phe, Trp, and Tyr, and Ala substitutions at positions 12 and 21 exhibited normal to enhanced GLP-2R binding but greater than 75% reduction in receptor activation [9].
  • The majority of position 2 substitutions exhibited normal to enhanced GLP-2 receptor (GLP-2R) binding; in contrast, position 2 substitutions were less well tolerated in studies of receptor activation as only Gly, Ile, Pro, alpha-aminobutyric acid, D-Ala, or nor-Val substitutions exhibited enhanced GLP-2R activation [9].

Physical interactions of GLP2R


Regulatory relationships of GLP2R

  • Administration of GLP-2 to animals with experimental intestinal injury promotes regeneration of the gastrointestinal epithelial mucosa and confers resistance to apoptosis in an indirect manner via yet-to-be identified GLP-2 receptor-dependent regulators of mucosal growth and cell survival [11].

Other interactions of GLP2R


Analytical, diagnostic and therapeutic context of GLP2R


  1. The HeLa cell glucagon-like peptide-2 receptor is coupled to regulation of apoptosis and ERK1/2 activation through divergent signaling pathways. Koehler, J.A., Yusta, B., Drucker, D.J. Mol. Endocrinol. (2005) [Pubmed]
  2. Glucagon and glucagon-like peptide receptors as drug targets. Estall, J.L., Drucker, D.J. Curr. Pharm. Des. (2006) [Pubmed]
  3. GLP-2 receptor localizes to enteric neurons and endocrine cells expressing vasoactive peptides and mediates increased blood flow. Guan, X., Karpen, H.E., Stephens, J., Bukowski, J.T., Niu, S., Zhang, G., Stoll, B., Finegold, M.J., Holst, J.J., Hadsell, D., Hadsell, D.L., Nichols, B.L., Burrin, D.G. Gastroenterology (2006) [Pubmed]
  4. Enteroendocrine localization of GLP-2 receptor expression in humans and rodents. Yusta, B., Huang, L., Munroe, D., Wolff, G., Fantaske, R., Sharma, S., Demchyshyn, L., Asa, S.L., Drucker, D.J. Gastroenterology (2000) [Pubmed]
  5. The glucagon-like peptide-2 receptor C terminus modulates beta-arrestin-2 association but is dispensable for ligand-induced desensitization, endocytosis, and G-protein-dependent effector activation. Estall, J.L., Koehler, J.A., Yusta, B., Drucker, D.J. J. Biol. Chem. (2005) [Pubmed]
  6. Biological actions and therapeutic potential of the glucagon-like peptides. Drucker, D.J. Gastroenterology (2002) [Pubmed]
  7. The glucagon-like peptide-2 receptor mediates direct inhibition of cellular apoptosis via a cAMP-dependent protein kinase-independent pathway. Yusta, B., Boushey, R.P., Drucker, D.J. J. Biol. Chem. (2000) [Pubmed]
  8. Lipid raft-dependent glucagon-like peptide-2 receptor trafficking occurs independently of agonist-induced desensitization. Estall, J.L., Yusta, B., Drucker, D.J. Mol. Biol. Cell (2004) [Pubmed]
  9. Structural determinants for activity of glucagon-like peptide-2. DaCambra, M.P., Yusta, B., Sumner-Smith, M., Crivici, A., Drucker, D.J., Brubaker, P.L. Biochemistry (2000) [Pubmed]
  10. The truncated metabolite GLP-2 (3-33) interacts with the GLP-2 receptor as a partial agonist. Thulesen, J., Knudsen, L.B., Hartmann, B., Hastrup, S., Kissow, H., Jeppesen, P.B., Ørskov, C., Holst, J.J., Poulsen, S.S. Regul. Pept. (2002) [Pubmed]
  11. Minireview: Glucagon-like peptides regulate cell proliferation and apoptosis in the pancreas, gut, and central nervous system. Brubaker, P.L., Drucker, D.J. Endocrinology (2004) [Pubmed]
  12. Glucagon-like peptide (GLP)-2 reduces chemotherapy-associated mortality and enhances cell survival in cells expressing a transfected GLP-2 receptor. Boushey, R.P., Yusta, B., Drucker, D.J. Cancer Res. (2001) [Pubmed]
  13. Glucagon-like peptide 2. Drucker, D.J. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  14. Glucagon-like peptide 2: a nutrient-responsive gut growth factor. Burrin, D.G., Petersen, Y., Stoll, B., Sangild, P. J. Nutr. (2001) [Pubmed]
  15. Naturally occurring glucagon-like peptide-2 (GLP-2) receptors in human intestinal cell lines. Sams, A., Hastrup, S., Andersen, M., Thim, L. Eur. J. Pharmacol. (2006) [Pubmed]
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