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 GIPRgene.[1][2] GIP-R is a member of the 7-transmembrane protein family, a class of G protein–coupled receptors.[3] GIP-R is found on beta-cells in the pancreas.[4][5]
Gastric inhibitory polypeptide (GIP), 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]
↑Stoffel M, Fernald AA, Le Beau MM, Bell GI (August 1995). "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. doi:10.1006/geno.1995.1203. PMID7490109.
↑Brubaker PL, Drucker DJ (2002). "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. doi:10.1080/10606820213687. PMID12529935.
Further reading
Yamada Y, Seino Y (2005). "Physiology of GIP--a lesson from GIP receptor knockout mice". Horm. Metab. Res. 36 (11–12): 771–774. doi:10.1055/s-2004-826162. PMID15655707.
Gremlich S, Porret A, Hani EH, et al. (1995). "Cloning, functional expression, and chromosomal localization of the human pancreatic islet glucose-dependent insulinotropic polypeptide receptor". Diabetes. 44 (10): 1202–1208. doi:10.2337/diabetes.44.10.1202. PMID7556958.
Volz A, Göke R, Lankat-Buttgereit B, et al. (1995). "Molecular cloning, functional expression, and signal transduction of the GIP-receptor cloned from a human insulinoma". FEBS Lett. 373 (1): 23–29. doi:10.1016/0014-5793(95)01006-Z. PMID7589426.
Usdin TB, Mezey E, Button DC, et al. (1994). "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. doi:10.1210/en.133.6.2861. PMID8243312.
Yamada Y, Hayami T, Nakamura K, et al. (1996). "Human gastric inhibitory polypeptide receptor: cloning of the gene (GIPR) and cDNA". Genomics. 29 (3): 773–776. doi:10.1006/geno.1995.9937. PMID8575774.
Gallwitz B, Witt M, Morys-Wortmann C, et al. (1997). "GLP-1/GIP chimeric peptides define the structural requirements for specific ligand-receptor interaction of GLP-1". Regul. Pept. 63 (1): 17–22. doi:10.1016/0167-0115(96)00019-5. PMID8795084.
N'Diaye N, Tremblay J, Hamet P, et al. (1998). "Adrenocortical overexpression of gastric inhibitory polypeptide receptor underlies food-dependent Cushing's syndrome". J. Clin. Endocrinol. Metab. 83 (8): 2781–2785. doi:10.1210/jc.83.8.2781. PMID9709947.
Tseng CC, Zhang XY (2000). "Role of G protein-coupled receptor kinases in glucose-dependent insulinotropic polypeptide receptor signaling". Endocrinology. 141 (3): 947–952. doi:10.1210/en.141.3.947. PMID10698169.
Baldacchino V, Oble S, Hamet P, et al. (2003). "Partial characterisation of the 5' flanking region of the human GIP receptor (GIPR) gene". Endocr. Res. 28 (4): 577–577. doi:10.1081/ERC-120016843. PMID12530665.
Antonini SR, N'Diaye N, Hamet P, et al. (2003). "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. doi:10.1081/ERC-120017003. PMID12530694.
Manhart S, Hinke SA, McIntosh CH, et al. (2003). "Structure-function analysis of a series of novel GIP analogues containing different helical length linkers". Biochemistry. 42 (10): 3081–3088. doi:10.1021/bi026868e. PMID12627975.
Ding KH, Zhong Q, Isales CM (2003). "Glucose-dependent insulinotropic peptide stimulates thymidine incorporation in endothelial cells: role of endothelin-1". Am. J. Physiol. Endocrinol. Metab. 285 (2): E390–6. doi:10.1152/ajpendo.00509.2002. PMID12721154.
Grimwood J, Gordon LA, Olsen A, et al. (2004). "The DNA sequence and biology of human chromosome 19". Nature. 428 (6982): 529–535. doi:10.1038/nature02399. PMID15057824.
Hansotia T, Baggio LL, Delmeire D, et al. (2004). "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. doi:10.2337/diabetes.53.5.1326. PMID15111503.
Baldacchino V, Oble S, Hamet P, et al. (2005). "The Sp transcription factor family is involved in the cellular expression of the human GIP-R gene promoter". Endocr. Res. 30 (4): 805–806. doi:10.1081/ERC-200044046. PMID15666829.
External links
"Glucagon Receptor Family: GIP". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.