Gastrin-releasing peptide receptor

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Species	Human	Mouse
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The gastrin-releasing peptide receptor (GRPR), now properly known as BB₂ is a G protein-coupled receptor whose endogenous ligand is gastrin releasing peptide. In humans it is highly expressed in the pancreas and is also expressed in the stomach, adrenal cortex and brain.

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.

The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.

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. doi:10.1016/0888-7543(95)80012-B. 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. doi:10.1007/BF02736689. 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. doi:10.1093/hmg/6.8.1241. 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. doi:10.1002/(SICI)1096-8628(19980630)78:2<173::AID-AJMG15>3.0.CO;2-K. 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. doi:10.1093/jnci/92.1.24. 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. doi:10.1016/S0378-1119(00)00596-5. 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. doi:10.1016/S0925-4773(02)00032-1. 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. doi:10.1016/S0014-5793(02)03177-0. 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. doi:10.1016/S0167-0115(02)00197-0. 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. PMC 139241. 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. doi:10.1016/S0092-8674(02)01116-9. 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. PMC 2377129. 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. doi:10.1136/jcp.2003.10660. PMC 1770197. 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. PMC 528928. PMID 15489334.

External links

• "Bombesin Receptors: BB₂". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
• IUPHAR GPCR Database - BB₂ receptor
• Receptors,+Bombesin at the US National Library of Medicine Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.