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Gene and Protein Information ![]() |
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class B G protein-coupled receptor | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 7 | 466 | 19q13.32 | GIPR | gastric inhibitory polypeptide receptor | 17 |
Mouse | 6 | 460 | 7 A3 | Gipr | gastric inhibitory polypeptide receptor | |
Rat | 7 | 455 | 1q21 | Gipr | gastric inhibitory polypeptide receptor | 16 |
Previous and Unofficial Names ![]() |
Gippr | GIP-R |
Database Links ![]() |
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Specialist databases | |
GPCRDB | gipr_human (Hs), gipr_mouse (Mm), gipr_rat (Rn) |
Other databases | |
Alphafold | P48546 (Hs), Q0P543 (Mm), P43219 (Rn) |
CATH/Gene3D | 4.10.1240.10 |
ChEMBL Target | CHEMBL4383 (Hs), CHEMBL5001 (Rn) |
Ensembl Gene | ENSG00000010310 (Hs), ENSMUSG00000030406 (Mm), ENSRNOG00000015860 (Rn) |
Entrez Gene | 2696 (Hs), 381853 (Mm), 25024 (Rn) |
Human Protein Atlas | ENSG00000010310 (Hs) |
KEGG Gene | hsa:2696 (Hs), mmu:381853 (Mm), rno:25024 (Rn) |
OMIM | 137241 (Hs) |
Pharos | P48546 (Hs) |
RefSeq Nucleotide | NM_000164 (Hs), NM_001080815 (Mm), NM_012714 (Rn) |
RefSeq Protein | NP_000155 (Hs), NP_001074284 (Mm), NP_036846 (Rn) |
UniProtKB | P48546 (Hs), Q0P543 (Mm), P43219 (Rn) |
Wikipedia | GIPR (Hs) |
Selected 3D Structures ![]() |
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Natural/Endogenous Ligands ![]() |
gastric inhibitory polypeptide {Sp: Human} , gastric inhibitory polypeptide {Sp: Mouse} , gastric inhibitory polypeptide {Sp: Rat} |
Download all structure-activity data for this target as a CSV file
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Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific agonist tables |
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific antagonist tables |
Primary Transduction Mechanisms ![]() |
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Transducer | Effector/Response |
Gs family | Adenylyl cyclase stimulation |
References: |
Secondary Transduction Mechanisms ![]() |
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Transducer | Effector/Response |
Phospholipase A2 stimulation | |
References: 4 |
Tissue Distribution ![]() |
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Expression Datasets ![]() |
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Functional Assays ![]() |
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Physiological Functions ![]() |
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Physiological Consequences of Altering Gene Expression ![]() |
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Phenotypes, Alleles and Disease Models ![]() |
Mouse data from MGI | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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1. Bollag RJ, Zhong Q, Phillips P, Min L, Zhong L, Cameron R, Mulloy AL, Rasmussen H, Qin F, Ding KH, Isales CM. (2000) Osteoblast-derived cells express functional glucose-dependent insulinotropic peptide receptors. Endocrinology, 141: 1228-1235. [PMID:10698200]
2. Coskun T, Sloop KW, Loghin C, Alsina-Fernandez J, Urva S, Bokvist KB, Cui X, Briere DA, Cabrera O, Roell WC et al.. (2018) LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept. Mol Metab, 18: 3-14. [PMID:30473097]
3. Deacon CF, Plamboeck A, Rosenkilde MM, de Heer J, Holst JJ. (2006) GIP-(3-42) does not antagonize insulinotropic effects of GIP at physiological concentrations. Am J Physiol Endocrinol Metab, 291 (3): E468-75. [PMID:16608883]
4. Ehses JA, Lee SS, Pederson RA, McIntosh CH. (2001) A new pathway for glucose-dependent insulinotropic polypeptide (GIP) receptor signaling: evidence for the involvement of phospholipase A2 in GIP-stimulated insulin secretion. J Biol Chem, 276 (26): 23667-73. [PMID:11323439]
5. Gallwitz B, Witt M, Morys-Wortmann C, Fölsch UR, Schmidt WE. (1996) GLP-1/GIP chimeric peptides define the structural requirements for specific ligand-receptor interaction of GLP-1. Regul Pept, 63 (1): 17-22. [PMID:8795084]
6. Gault VA, O'Harte FP, Harriott P, Mooney MH, Green BD, Flatt PR. (2003) Effects of the novel (Pro3)GIP antagonist and exendin(9-39)amide on GIP- and GLP-1-induced cyclic AMP generation, insulin secretion and postprandial insulin release in obese diabetic (ob/ob) mice: evidence that GIP is the major physiological incretin. Diabetologia, 46 (2): 222-30. [PMID:12627321]
7. Gelling RW, Coy DH, Pederson RA, Wheeler MB, Hinke S, Kwan T, McIntosh CH. (1997) GIP(6-30amide) contains the high affinity binding region of GIP and is a potent inhibitor of GIP1-42 action in vitro. Regul Pept, 69 (3): 151-4. [PMID:9226399]
8. Hansen LS, Sparre-Ulrich AH, Christensen M, Knop FK, Hartmann B, Holst JJ, Rosenkilde MM. (2016) N-terminally and C-terminally truncated forms of glucose-dependent insulinotropic polypeptide are high-affinity competitive antagonists of the human GIP receptor. Br J Pharmacol, 173 (5): 826-38. [PMID:26572091]
9. McIntosh CH, Bremsak I, Lynn FC, Gill R, Hinke SA, Gelling R, Nian C, McKnight G, Jaspers S, Pederson RA. (1999) Glucose-dependent insulinotropic polypeptide stimulation of lipolysis in differentiated 3T3-L1 cells: wortmannin-sensitive inhibition by insulin. Endocrinology, 140 (1): 398-404. [PMID:9886851]
10. Miyawaki K, Yamada Y, Yano H, Niwa H, Ban N, Ihara Y, Kubota A, Fujimoto S, Kajikawa M, Kuroe A et al.. (1999) Glucose intolerance caused by a defect in the entero-insular axis: a study in gastric inhibitory polypeptide receptor knockout mice. Proc Natl Acad Sci USA, 96 (26): 14843-7. [PMID:10611300]
11. Parthier C, Kleinschmidt M, Neumann P, Rudolph R, Manhart S, Schlenzig D, Fanghänel J, Rahfeld JU, Demuth HU, Stubbs MT. (2007) Crystal structure of the incretin-bound extracellular domain of a G protein-coupled receptor. Proc Natl Acad Sci USA, 104 (35): 13942-7. [PMID:17715056]
12. Preitner F, Ibberson M, Franklin I, Binnert C, Pende M, Gjinovci A, Hansotia T, Drucker DJ, Wollheim C, Burcelin R et al.. (2004) Gluco-incretins control insulin secretion at multiple levels as revealed in mice lacking GLP-1 and GIP receptors. J Clin Invest, 113 (4): 635-45. [PMID:14966573]
13. Trümper A, Trümper K, Trusheim H, Arnold R, Göke B, Hörsch D. (2001) Glucose-dependent insulinotropic polypeptide is a growth factor for beta (INS-1) cells by pleiotropic signaling. Mol Endocrinol, 15 (9): 1559-70. [PMID:11518806]
14. Tseng CC, Kieffer TJ, Jarboe LA, Usdin TB, Wolfe MM. (1996) Postprandial stimulation of insulin release by glucose-dependent insulinotropic polypeptide (GIP). Effect of a specific glucose-dependent insulinotropic polypeptide receptor antagonist in the rat. J Clin Invest, 98 (11): 2440-5. [PMID:8958204]
15. Tseng CC, Zhang XY, Wolfe MM. (1999) Effect of GIP and GLP-1 antagonists on insulin release in the rat. Am J Physiol, 276 (6): E1049-54. [PMID:10362617]
16. Usdin TB, Bonner TI. (1993) Gastric inhibitory polypeptide receptor, a member of the secretin- vasoactive intestinal peptide receptor family, is widely distributed in peripheral organs and the brain. Endocrinology, 133: 2861-2870. [PMID:8243312]
17. Volz A, Göke R, Lankat-Buttgereit B, Fehmann HC, Bode HP, Göke B. (1995) Molecular cloning, functional expression, and signal transduction of the GIP-receptor cloned from a human insulinoma. FEBS Lett, 373 (1): 23-9. [PMID:7589426]
18. Wheeler MB, Gelling RW, McIntosh CH, Georgiou J, Brown JC, Pederson RA. (1995) Functional expression of the rat pancreatic islet glucose-dependent insulinotropic polypeptide receptor: ligand binding and intracellular signaling properties. Endocrinology, 136 (10): 4629-39. [PMID:7664683]
19. Xiong Y, Guo J, Candelore MR, Liang R, Miller C, Dallas-Yang Q, Jiang G, McCann PE, Qureshi SA, Tong X et al.. (2012) Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. J Med Chem, 55 (13): 6137-48. [PMID:22708876]
20. Zhong Q, Bollag RJ, Dransfield DT, Gasalla-Herraiz J, Ding KH, Min L, Isales CM. (2000) Glucose-dependent insulinotropic peptide signaling pathways in endothelial cells. Peptides, 21 (9): 1427-32. [PMID:11072131]