GLP-2 receptor

Target id: 250

Nomenclature: GLP-2 receptor

Family: Glucagon receptor family

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for GLP-2 receptor in GtoImmuPdb

Gene and Protein Information
class B G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 553 17p13.3 GLP2R glucagon like peptide 2 receptor 9
Mouse 7 512 11 B3 Glp2r glucagon-like peptide 2 receptor
Rat 7 550 10q24 Glp2r glucagon-like peptide 2 receptor 9
Previous and Unofficial Names
GLP-2R
Database Links
Specialist databases
GPCRDB glp2r_human (Hs), glp2r_mouse (Mm), glp2r_rat (Rn)
Other databases
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
glucagon-like peptide 2 {Sp: Human}
glucagon-like peptide 2-(3-33) {Sp: Human}
glucagon-like peptide 2 {Sp: Mouse}
glucagon-like peptide 2-(3-33) {Sp: Mouse}
glucagon-like peptide 2 {Sp: Rat}
glucagon-like peptide 2-(3-33) {Sp: Rat}

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
glucagon-like peptide 2 {Sp: Rat} Rn Full agonist 10.2 pKi 9
pKi 10.2 [9]
GLP-2-(1-29) (rat) Rn Partial agonist 9.5 pKi 9
pKi 9.5 [9]
[Tyr34]GLP-2 (human) Rn Full agonist 9.2 pKi 9
pKi 9.2 [9]
glucagon-like peptide 2 {Sp: Human} Rn Full agonist 8.8 pKi 9
pKi 8.8 [9]
glucagon-like peptide 2-(3-33) {Sp: Rat} Rn Partial agonist 6.6 pKi 9
pKi 6.6 [9]
glucagon-like peptide 2-(2-33) {Sp: Rat} Rn Partial agonist 6.1 pKi 9
pKi 6.1 [9]
glucagon-like peptide 2 {Sp: Human} Hs Full agonist 8.5 pIC50 10
pIC50 8.5 [10]
glucagon-like peptide 2-(3-33) {Sp: Human} Hs Partial agonist 7.4 pIC50 10
pIC50 7.4 [10]
teduglutide Hs Agonist - - 8
[8]
View species-specific agonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Adenylate cyclase stimulation
References: 
Tissue Distribution
Isolated rat small intestine mucosal cells.
Species:  Rat
Technique:  RT-PCR.
References:  12
Highest levels found in the jejunum.
Also found in duodenum, ileum, colon and stomach.
Undetectable in the brain, heart, kidney, liver, lung, muscle and spleen.
Species:  Rat
Technique:  RNase protection assay.
References:  9
Fetal, neonatal, weaned and adult stomach.
Small and large intestines.
Jejunum, ileum and colon (higher in fetal tissues than adult).
Species:  Rat
Technique:  RT-PCR.
References:  7
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays
Measurement of cAMP levels in isolated rat small intestinal mucosal cells expressing GLP-2 receptors.
Species:  Rat
Tissue:  Small intestinal mucosal cells.
Response measured:  Stimulation of cAMP production.
References:  12
Measurement of cAMP levels in COS cells transfected with the GLP-2 receptor.
Species:  Human
Tissue:  COS cells.
Response measured:  Increase in cAMP production.
References:  9
Measurement of cAMP levels in the stable GLP-2 receptor episomal expression line, rG2R.
Species:  Rat
Tissue:  rG2R episomal cell line.
Response measured:  Stimulation of cAMP production.
References:  9
Measurement of the activity of a cAMP-dependent reporter gene, CRE-β-galactosidase, in BHK cells endogenously expressing the GLP-2 receptor.
Species:  Rat
Tissue:  BHK fibroblast cells.
Response measured:  Increased activity of the reporter gene.
References:  13
Measurement of AP-1 luciferase reporter gene activity in BHK fibroblast cells endogenously expressing the GLP-2 receptor.
Species:  Rat
Tissue:  BHK fibroblast cells.
Response measured:  Induction of AP-1 luciferase activity.
References:  13
Physiological Functions
Promotes growth of the small intestine.
Species:  Mouse
Tissue:  Small intestine.
References:  5,11
Small bowel crypt cell proliferation.
Species:  Mouse
Tissue:  Small intestine.
References:  6
h[Gly2]GLP-2-treated mice show increased epithelial repair and reduced cell death in the crypt compartment.
Species:  Mouse
Tissue:  Small intestine.
References:  1
GLP-2 receptor activation maintains small bowel mucosal epithelium in perenteral nutrition fed rats.
Species:  Rat
Tissue:  Small intestine.
References:  3
Upregulation of small bowel hexose transport.
Species:  Rat
Tissue:  Jejunum.
References:  4
The GLP-2 receptor-mediated small bowel growth results in an increase in nutrient digestion and absorption.
Species:  Mouse
Tissue:  In vivo.
References:  2
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Apc+|ApcMin|Glp2r+|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2r+
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0000490 abnormal crypts of Lieberkuhn morphology PMID: 18829546 
Apc+|ApcMin|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2rtm1Ddr
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0000490 abnormal crypts of Lieberkuhn morphology PMID: 18829546 
Apc+|ApcMin|Glp2r+|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2r+
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0000488 abnormal intestinal epithelium morphology PMID: 18829546 
Apc+|ApcMin|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2rtm1Ddr
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0000488 abnormal intestinal epithelium morphology PMID: 18829546 
Apc+|ApcMin|Glp2r+|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2r+
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0003448 altered tumor morphology PMID: 18829546 
Apc+|ApcMin|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2rtm1Ddr
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0003448 altered tumor morphology PMID: 18829546 
Apc+|ApcMin|Glp2r+|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2r+
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0002404 increased intestinal adenoma incidence PMID: 18829546 
Apc+|ApcMin|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2rtm1Ddr
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0002404 increased intestinal adenoma incidence PMID: 18829546 
Apc+|ApcMin|Glp2r+|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2r+
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0008011 intestine polyps PMID: 18829546 
Apc+|ApcMin|Glp2rtm1Ddr ApcMin/Apc+,Glp2rtm1Ddr/Glp2rtm1Ddr
involves: C57BL/6J
MGI:2136733  MGI:88039  MP:0008011 intestine polyps PMID: 18829546 

References

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1. Boushey RP, Drucker DJ. (1999) Glucagon-like peptide 2 decreases mortality and reduces the severity of indomethacin-induced murine enteritis. Am. J. Physiol.277: E937-E947. [PMID:10567023]

2. Brubaker PL, Drucker DJ. (1997) Intestinal function in mice with small bowel growth induced by glucagon-like peptide-2. Am. J. Physiol.272: E1050-E1058. [PMID:9227451]

3. Chance WT, Balasubramaniam A. (1997) Prevention of parenteral nutrition-induced gut hypoplasia by coinfusion of glucagon-like peptide-2. Am. J. Physiol.273: 559-563. [PMID:9277438]

4. Cheeseman CI, Tsang R. (1996) The effect of gastric inhibitory polypeptide and glucagon like peptides on intestinal hexose transport. Am. J. Physiol. Gastrointest. Liver Physiol.271: G477-G482. [PMID:8843773]

5. Drucker DJ, Brubaker PL. (1996) Induction of intestinal epithelial proliferation by glucagon-like peptide 2. Proc. Natl. Acad. Sci. U.S.A.93: 7911-7916. [PMID:8755576]

6. Drucker DJ, Brubaker PL. (1997) Intestinal response to growth factors administered alone or in combination with h[Gly2]-Glucagon-like peptide 2. Am. J. Physiol.273: G1252-G2262. [PMID:9435550]

7. Lovshin J, Yusta B, Iliopoulos I, Migirdicyan A, Dableh L, Brubaker PL, Drucker DJ. (2000) Ontogeny of the glucagon-like peptide-2 receptor axis in the developing rat intestine. Endocrinology141: 4194-4201. [PMID:11089553]

8. McKeage K. (2015) Teduglutide: a guide to its use in short bowel syndrome. Clin Drug Investig35 (5): 335-40. [PMID:25859983]

9. Munroe DG, Gupta AK, Kooshesh F, Vyas TB, Rizkalla G, Wang H, Demchyshyn L, Yang ZJ, Kamboj RK, Chen H et al.. (1999) Prototypic G protein-coupled receptor for the intestinotrophic factor glucagon-like peptide 2. Proc. Natl. Acad. Sci. U.S.A.96 (4): 1569-73. [PMID:9990065]

10. Thulesen J, Knudsen LB, Hartmann B, Hastrup S, Kissow H, Jeppesen PB, Orskov C, Holst JJ, Poulsen SS. (2002) The truncated metabolite GLP-2 (3-33) interacts with the GLP-2 receptor as a partial agonist. Regul Pept103: 9-15. [PMID:11738243]

11. Tsai C-H, Drucker DJ. (1997) Intestinal growth-promoting properties of glucagon-like peptide 2 in mice. Am. J. Physiol.273: E77-E84. [PMID:9252482]

12. Walsh NA, Yusta B, DaCambra MP, Anini Y, Drucker DJ, Brubaker PL. (2003) Glucagon-like peptide-2 receptor activation in the rat intestinal mucosa. Endocrinology144: 4385-4392. [PMID:12960094]

13. Yusta B, Drucker DJ. (1999) Identification of glucagon-like peptide-2 (GLP-2)-activated signalling pathways in baby hamster kidney fibroblasts expressing the rat GLP-2 receptor. J. Biol. Chem.274: 30459-30467. [PMID:10521425]

Contributors

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How to cite this page

Dominique Bataille, Philippe Delagrange, Daniel J. Drucker, Burkhard Göke, Rebecca Hills, Kelly E. Mayo, Laurence J. Miller, Bernard Thorens.
Glucagon receptor family: GLP-2 receptor. Last modified on 10/07/2015. Accessed on 23/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=250.