Gastric inhibitory polypeptide receptor explained

The gastric inhibitory polypeptide receptor (GIP-R), also known as the glucose-dependent insulinotropic polypeptide receptor, is a protein that in humans is encoded by the GIPR gene.^{[1] [2]}

GIP-R is a member of the class B family of G protein coupled receptors. GIP-R is found on beta-cells in the pancreas^{[3] [4]} where it serves as the receptor for the hormone Gastric inhibitory polypeptide (GIP).

Function

Gastric inhibitory polypeptide, also called glucose-dependent insulinotropic polypeptide, is a 42-amino acid polypeptide synthesized by K cells of the duodenum and small intestine. It was originally identified as an activity in gut extracts that inhibited gastric acid secretion and gastrin release, but subsequently was demonstrated to stimulate insulin release potently in the presence of elevated glucose. The insulinotropic effect on pancreatic islet beta-cells was then recognized to be the principal physiologic action of GIP. Together with glucagon-like peptide-1, GIP is largely responsible for the secretion of insulin after eating. It is involved in several other facets of the anabolic response.^[1]

Further reading

• Yamada Y, Seino Y . Physiology of GIP--a lesson from GIP receptor knockout mice . Horm. Metab. Res. . 36 . 11–12 . 771–774 . 2005 . 15655707 . 10.1055/s-2004-826162 . 262453421 .
• Gremlich S . Cloning, functional expression, and chromosomal localization of the human pancreatic islet glucose-dependent insulinotropic polypeptide receptor . Diabetes . 44 . 10 . 1202–1208 . 1995 . 7556958 . 10.2337/diabetes.44.10.1202 . Porret A . Hani EH . Cherif . D. . Vionnet . N. . Froguel . P. . Thorens . B. .
• Volz A . Molecular cloning, functional expression, and signal transduction of the GIP-receptor cloned from a human insulinoma . FEBS Lett. . 373 . 1 . 23–29 . 1995 . 7589426 . 10.1016/0014-5793(95)01006-Z . Göke R . Lankat-Buttgereit B . Fehmann . HC . Bode . HP . Göke . B . 25033358 . free.
• Usdin TB . 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 . 6 . 2861–2870 . 1994 . 8243312 . 10.1210/endo.133.6.8243312 . Mezey E . Button DC . Brownstein . MJ . Bonner . TI .
• Yamada Y . Human gastric inhibitory polypeptide receptor: cloning of the gene (GIPR) and cDNA . Genomics . 29 . 3 . 773–776 . 1996 . 8575774 . 10.1006/geno.1995.9937 . Hayami T . Nakamura K . Kaisaki . PJ . Someya . Y . Wang . CZ . Seino . S . Seino . Y .
• Gallwitz B . GLP-1/GIP chimeric peptides define the structural requirements for specific ligand-receptor interaction of GLP-1 . Regul. Pept. . 63 . 1 . 17–22 . 1997 . 8795084 . 10.1016/0167-0115(96)00019-5 . Witt M . Morys-Wortmann C . Fölsch . UR . Schmidt . WE . 42462407 .
• N'Diaye N . Adrenocortical overexpression of gastric inhibitory polypeptide receptor underlies food-dependent Cushing's syndrome . J. Clin. Endocrinol. Metab. . 83 . 8 . 2781–2785 . 1998 . 9709947 . Tremblay J . Hamet P . De Herder . WW . Lacroix . A . 10.1210/jcem.83.8.5038 . free .
• Tseng CC, Zhang XY . Role of G protein-coupled receptor kinases in glucose-dependent insulinotropic polypeptide receptor signaling . Endocrinology . 141 . 3 . 947–952 . 2000 . 10698169 . 10.1210/endo.141.3.7365 . free .
• Bollag RJ . Osteoblast-derived cells express functional glucose-dependent insulinotropic peptide receptors . Endocrinology . 141 . 3 . 1228–1235 . 2000 . 10698200 . 10.1210/endo.141.3.7366 . Zhong Q . Phillips P . Min . L . Zhong . L . Cameron . R . Mulloy . AL . Rasmussen . H . Qin . F . free .
• Strausberg RL . 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 . 16899–16903 . 2003 . 12477932 . 10.1073/pnas.242603899 . 139241 . Feingold EA . Grouse LH . Derge . JG . Klausner . RD . Collins . FS . Wagner . L . Shenmen . CM . Schuler . GD . 2002PNAS...9916899M . free .
• Baldacchino V . Partial characterisation of the 5' flanking region of the human GIP receptor (GIPR) gene . Endocr. Res. . 28 . 4 . 577 . 2003 . 12530665 . 10.1081/ERC-120016843 . Oble S . Hamet P . Tremblay . J. . Lacroix . A. . 32639335 .
• Antonini SR . Analysis of the putative promoter region of the GIP receptor gene (GIPR) in GIP-dependent Cushing's syndrome (CS) . Endocr. Res. . 28 . 4 . 755–756 . 2003 . 12530694 . 10.1081/ERC-120017003 . N'Diaye N . Hamet P . Tremblay . J. . Lacroix . A. . 21467413 .
• Manhart S . Structure-function analysis of a series of novel GIP analogues containing different helical length linkers . Biochemistry . 42 . 10 . 3081–3088 . 2003 . 12627975 . 10.1021/bi026868e . Hinke SA . McIntosh CH . Pederson . Raymond A. . Demuth . Hans-Ulrich .
• Ding KH, Zhong Q, Isales CM . Glucose-dependent insulinotropic peptide stimulates thymidine incorporation in endothelial cells: role of endothelin-1 . Am. J. Physiol. Endocrinol. Metab. . 285 . 2 . E390–6 . 2003 . 12721154 . 10.1152/ajpendo.00509.2002 .
• Grimwood J . The DNA sequence and biology of human chromosome 19 . Nature . 428 . 6982 . 529–535 . 2004 . 15057824 . 10.1038/nature02399 . Gordon LA . Olsen A . Terry . Astrid . Schmutz . Jeremy . Lamerdin . Jane . Hellsten . Uffe . Goodstein . David . Couronne . Olivier . 2004Natur.428..529G . free .
• Hansotia T . Double incretin receptor knockout (DIRKO) mice reveal an essential role for the enteroinsular axis in transducing the glucoregulatory actions of DPP-IV inhibitors . Diabetes . 53 . 5 . 1326–1335 . 2004 . 15111503 . 10.2337/diabetes.53.5.1326 . Baggio LL . Delmeire D . Hinke . S. A. . Yamada . Y. . Tsukiyama . K. . Seino . Y. . Holst . J. J. . Schuit . F. . free .
• Gerhard DS . The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC) . Genome Res. . 14 . 10B . 2121–2127 . 2004 . 15489334 . 10.1101/gr.2596504 . 528928 . Wagner L . Feingold EA . Shenmen . CM . Grouse . LH . Schuler . G . Klein . SL . Old . S . Rasooly . R .
• Baldacchino V . The Sp transcription factor family is involved in the cellular expression of the human GIP-R gene promoter . Endocr. Res. . 30 . 4 . 805–806 . 2005 . 15666829 . 10.1081/ERC-200044046 . Oble S . Hamet P . Tremblay . J. . Bourdeau . I. . Lacroix . A. . 40407171 .

External links

• Web site: Glucagon Receptor Family: GIP . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology . 2007-10-25 . 2016-03-03 . https://web.archive.org/web/20160303191301/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2294 . dead .

Notes and References

1. Web site: Entrez Gene: gastric inhibitory polypeptide receptor.
2. Stoffel M, Fernald AA, Le Beau MM, Bell GI . Assignment of the gastric inhibitory polypeptide receptor gene (GIPR) to chromosome bands 19q13.2-q13.3 by fluorescence in situ hybridization . Genomics . 28 . 3 . 607–609 . August 1995 . 7490109 . 10.1006/geno.1995.1203 .
3. Web site: Gastrointestinal Hormones and Peptides . 2007-08-24 . 2007-12-06 . https://web.archive.org/web/20071206035951/http://web.indstate.edu/thcme/mwking/peptide-hormones.html#gastrin . dead .
4. Brubaker PL, Drucker DJ . Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors . Recept. Channels . 8 . 3–4 . 179–188 . 2002 . 12529935 . 10.1080/10606820213687 .