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14-September-2008 18:02:43 - Gastrin-releasing peptide receptor Gastrin-releasing peptide receptor Identifiers Symbols GRPR; External IDs OMIM: 305670 MGI: 95836 HomoloGene: 21098 Gene ontology Molecular function: receptor activity bombesin receptor activity peptide receptor activity, G-protein coupled Cellular component: plasma membrane integral to plasma membrane integral to membrane Biological process: signal transduction G-protein coupled receptor protein signaling pathway regulation of cell proliferation RNA expression pattern More reference expression data Orthologs Human Mouse Entrez 2925 14829 Ensembl ENSG00000126010 ENSMUSG00000031364 Uniprot P30550 Q53WV4 Refseq NM_005314 mRNA NP_005305 protein NM_008177 mRNA NP_032203 protein Location Chr X: 16.05 - 16.08 Mb Chr X: 158.86 - 158.89 Mb Pubmed search 1 2 The gastrin-releasing peptide receptor GRPR is a G protein-coupled receptor whose endogenous ligand is gastrin releasing peptide.1 Gastrin-releasing peptide GRP regulates numerous functions of the gastrointestinal and central nervous systems, including release of gastrointestinal hormones, smooth muscle cell contraction, and epithelial cell proliferation and is a potent mitogen for neoplastic tissues. The effects of GRP are mediated through the gastrin-releasing peptide receptor. This receptor is a glycosylated, 7-transmembrane G-protein coupled receptor that activates the phospholipase C signaling pathway. The receptor is aberrantly expressed in numerous cancers such as those of the lung, colon, and prostate. An individual with autism and multiple exostoses was found to have a balanced translocation between chromosome 8 and a chromosome X breakpoint located within the gastrin-releasing peptide receptor gene.2 The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.3 References ^ Benya RV, Kusui T, Pradhan TK, Battey JF, Jensen RT 1995. Expression and characterization of cloned human bombesin receptors. Mol. Pharmacol. 47 1: 10-20. PMID 7838118. ^ Entrez Gene: GRPR gastrin-releasing peptide receptor. ^ Chinnappan D, Qu X, Xiao D, Ratnasari A, Weber HC May 2008. Human gastrin releasing peptide receptor gene regulation requires transcription factor binding at two distinct cre sites. Am. J. Physiol. Gastrointest. Liver Physiol.. doi:10.1152/ajpgi.00036.2008. PMID 18483184. Further reading Corjay MH, Dobrzanski DJ, Way JM, et al. 1991. Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells.. J. Biol. Chem. 266 28: 18771-9. PMID 1655761. Alitalo T, Francis F, Kere J, et al. 1995. A 6-Mb YAC contig in Xp22.1-p22.2 spanning the DXS69E, XE59, GLRA2, PIGA, GRPR, CALB3, and PHKA2 genes.. Genomics 25 3: 691-700. PMID 7759104. Benya RV, Kusui T, Pradhan TK, et al. 1995. Expression and characterization of cloned human bombesin receptors.. Mol. Pharmacol. 47 1: 10-20. PMID 7838118. Giladi E, Nagalla SR, Spindel ER 1993. Molecular cloning and characterization of receptors for the mammalian bombesin-like peptides.. J. Mol. Neurosci. 4 1: 41-54. PMID 8391296. Maslen GL, Boyd Y 1993. Comparative mapping of the Grpr locus on the X chromosomes of man and mouse.. Genomics 17 1: 106-9. doi:10.1006/geno.1993.1290. PMID 8406441. Ishikawa-Brush Y, Powell JF, Bolton P, et al. 1997. Autism and multiple exostoses associated with an X;8 translocation occurring within the GRPR gene and 3' to the SDC2 gene.. Hum. Mol. Genet. 6 8: 1241-50. PMID 9259269. Heidary G, Hampton LL, Schanen NC, et al. 1998. Exclusion of the gastrin-releasing peptide receptor GRPR locus as a candidate gene for Rett syndrome.. Am. J. Med. Genet. 78 2: 173-5. PMID 9674911. Shriver SP, Bourdeau HA, Gubish CT, et al. 2000. Sex-specific expression of gastrin-releasing peptide receptor: relationship to smoking history and risk of lung cancer.. J. Natl. Cancer Inst. 92 1: 24-33. PMID 10620630. Xiao D, Wang J, Hampton LL, Weber HC 2001. The human gastrin-releasing peptide receptor gene structure, its tissue expression and promoter.. Gene 264 1: 95-103. PMID 11245983. Carroll RE, Matkowskyj K, Saunthararajah Y, et al. 2002. Contribution of gastrin-releasing peptide and its receptor to villus development in the murine and human gastrointestinal tract.. Mech. Dev. 113 2: 121-30. PMID 11960700. Qu X, Xiao D, Weber HC 2002. Human gastrin-releasing peptide receptor mediates sustained CREB phosphorylation and transactivation in HuTu 80 duodenal cancer cells.. FEBS Lett. 527 1-3: 109-13. PMID 12220644. Xiao D, Qu X, Weber HC 2003. GRP receptor-mediated immediate early gene expression and transcription factor Elk-1 activation in prostate cancer cells.. Regul. Pept. 109 1-3: 141-8. PMID 12409226. Uchida K, Kojima A, Morokawa N, et al. 2003. Expression of progastrin-releasing peptide and gastrin-releasing peptide receptor mRNA transcripts in tumor cells of patients with small cell lung cancer.. J. Cancer Res. Clin. Oncol. 128 12: 633-40. doi:10.1007/s00432-002-0392-8. PMID 12474049. Strausberg RL, Feingold EA, Grouse LH, et al. 2003. 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: 16899-903. doi:10.1073/pnas.242603899. PMID 12477932. Shumyatsky GP, Tsvetkov E, Malleret G, et al. 2003. Identification of a signaling network in lateral nucleus of amygdala important for inhibiting memory specifically related to learned fear.. Cell 111 6: 905-18. PMID 12526815. Glover SC, Tretiakova MS, Carroll RE, Benya RV 2003. Increased frequency of gastrin-releasing peptide receptor gene mutations during colon-adenocarcinoma progression.. Mol. Carcinog. 37 1: 5-15. doi:10.1002/mc.10117. PMID 12720295. Waters CM, MacKinnon AC, Cummings J, et al. 2003. Increased gastrin-releasing peptide GRP receptor expression in tumour cells confers sensitivity to Arg6,D-Trp7,9,NmePhe8-substance P 6-11-induced growth inhibition.. Br. J. Cancer 88 11: 1808-16. doi:10.1038/sj.bjc.6600957. PMID 12771999. Scott N, Millward E, Cartwright EJ, et al. 2004. Gastrin releasing peptide and gastrin releasing peptide receptor expression in gastrointestinal carcinoid tumours.. J. Clin. Pathol. 57 2: 189-92. PMID 14747448. Chen PW, Kroog GS 2005. Alterations in receptor expression or agonist concentration change the pathways gastrin-releasing peptide receptor uses to regulate extracellular signal-regulated kinase.. Mol. Pharmacol. 66 6: 1625-34. doi:10.1124/mol.104.001206. PMID 15361544. Gerhard DS, Wagner L, Feingold EA, et al. 2004. The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection MGC.. Genome Res. 14 10B: 2121-7. doi:10.1101/gr.2596504. PMID 15489334. External links IUPHAR GPCR Database - BB2 receptor MeSH Receptors,+Bombesin This transmembrane receptor-related article is a stub. This article incorporates text from the United States National Library of Medicine, which is in the public domain. v d e Transmembrane receptor: G protein-coupled receptors Class A: Rhodopsin like Adrenergic α1 A, B, D, α2 A, B, C, β1, β2, β3 Eicosanoid CysLT 1, 2, LTB4 1, 2, FPRL1, OXE, Prostaglandin DP, EP 1, 2, 3, 4, PGF, Prostacyclin, Thromboxane Neuropeptide B/W 1, 2, FF 1, 2, S, Y 1, 2, 4, 5 Orphan GPR 1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182 Purinergics Adenosine A1, A2a, A2b, A3, P2Y, 1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14 Serotonin all but 5-HT3 5-HT1 A, B, D, E, F, 5-HT2 A, B, C, 5-HT 4, 5A, 6, 7 Other Acetylcholine M1, M2, M3, M4, M5 - Adrenomedullin - Anaphylatoxin C3a, C5a - Angiotensin 1, 2 - Apelin - Bile acid - Bombesin BRS3, GRPR, NMBR - Bradykinin B1, B2 - Cannabinoid CB1, CB2 - Chemokine - Cholecystokinin A, B - Dopamine D1, D2, D3, D4, D5 - EBI2 - Endothelin A, B - Estrogen - Formyl peptide 1, L1, L2 - Free fatty acid 1, 2, 3, 4 - FSH - Galanin 1, 2, 3 - Gonadotropin-releasing hormone 1, 2 - Ghrelin - Histamine H1, H2, H3, H4 - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid 1, 2, 3, 4, 5, 6, 7, 8 - MAS 1, 1L, D, E, F, G, X1, X2, X3, X4 - Melanocortin 1, 2, 3, 4, 5 - MCHR 1, 2 - Melatonin 1A, 1B- Motilin - neuromedin B, U 1, 2 - Neurotensin 1, 2 - Opioid Delta, Kappa, Mu, Nociceptin, but not Sigma - Olfactory - Opsin 3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH - Orexin 1, 2 - Oxytocin - Oxoglutarate - PAF - Prokineticin 1, 2 - Prolactin-releasing peptide - Protease-activated 1, 2, 3, 4 - Relaxin 1, 2, 3, 4 - Somatostatin 1, 2, 3, 4, 5 - SREB - Succinate - TAAR 1, 2, 3, 5, 6, 8, 9 - Tachykinin 1, 2, 3 - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin 1A, 1B, 2 Class B: Secretin like Brain-specific angiogenesis inhibitor 1, 2, 3 - Cadherin 1, 2, 3 - Calcitonin - CD97 - Corticotropin-releasing hormone 1, 2 - EMR 1, 2, 3 - Glucagon GR, GIPR, GLP1R, GLP2R - Growth hormone releasing hormone - PACAPR1- GPR 56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 157 - Latrophilin 1, 2, 3, ELTD1 - Parathyroid hormone 1, 2 - Secretin - Vasoactive intestinal peptide 1, 2 Class C: Metabotropic glutamate / pheromone Calcium-sensing receptor - GABA B 1, 2 - Glutamate receptor Metabotropic glutamate 1, 2, 3, 4, 5, 6, 7, 8 - GPRC6A - GPR 156, 158, 179 - RAIG 1, 2, 3, 4 - Taste receptors TAS1R 1, 2, 3 TAS2R 1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50 Frizzled / Smoothened Frizzled 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 - Smoothened Retrieved from http://en..org/wiki/Gastrin-releasing_peptide_receptor Categories: Genes on chromosome X | Human proteins | Transmembrane receptor stubs | G protein coupled receptorsHidden category: Protein pages needing a picture Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page This page was last modified on 8 July 2008, at 05:34
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