Biology:Gastrin-releasing peptide receptor

Short description: Protein-coding gene in the species Homo sapiens

Generic protein structure example

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.

Activation MOR1D‐GRPR heteromers in the spinal cord mediate the common troublesome opioid-induced itch.

Further reading

• "Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells". J. Biol. Chem. 266 (28): 18771–9. 1991. doi:10.1016/S0021-9258(18)55129-2. PMID 1655761. 
• "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. 1995. doi:10.1016/0888-7543(95)80012-B. PMID 7759104. 
• "Expression and characterization of cloned human bombesin receptors". Mol. Pharmacol. 47 (1): 10–20. 1995. PMID 7838118. 
• "Molecular cloning and characterization of receptors for the mammalian bombesin-like peptides". J. Mol. Neurosci. 4 (1): 41–54. 1993. doi:10.1007/BF02736689. PMID 8391296. 
• "Comparative mapping of the Grpr locus on the X chromosomes of man and mouse". Genomics 17 (1): 106–9. 1993. doi:10.1006/geno.1993.1290. PMID 8406441. 
• "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. 1997. doi:10.1093/hmg/6.8.1241. PMID 9259269. 
• "Exclusion of the gastrin-releasing peptide receptor (GRPR) locus as a candidate gene for Rett syndrome". Am. J. Med. Genet. 78 (2): 173–5. 1998. doi:10.1002/(SICI)1096-8628(19980630)78:2<173::AID-AJMG15>3.0.CO;2-K. PMID 9674911. 
• "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. 2000. doi:10.1093/jnci/92.1.24. PMID 10620630. 
• "The human gastrin-releasing peptide receptor gene structure, its tissue expression and promoter". Gene 264 (1): 95–103. 2001. doi:10.1016/S0378-1119(00)00596-5. PMID 11245983. 
• "Contribution of gastrin-releasing peptide and its receptor to villus development in the murine and human gastrointestinal tract". Mech. Dev. 113 (2): 121–30. 2002. doi:10.1016/S0925-4773(02)00032-1. PMID 11960700. 
• "Human gastrin-releasing peptide receptor mediates sustained CREB phosphorylation and transactivation in HuTu 80 duodenal cancer cells". FEBS Lett. 527 (1–3): 109–13. 2002. doi:10.1016/S0014-5793(02)03177-0. PMID 12220644. 
• "GRP receptor-mediated immediate early gene expression and transcription factor Elk-1 activation in prostate cancer cells". Regul. Pept. 109 (1–3): 141–8. 2003. doi:10.1016/S0167-0115(02)00197-0. PMID 12409226. 
• "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. 2003. doi:10.1007/s00432-002-0392-8. PMID 12474049. 
• "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. 2003. doi:10.1073/pnas.242603899. PMID 12477932. Bibcode: 2002PNAS...9916899M. 
• "Identification of a signaling network in lateral nucleus of amygdala important for inhibiting memory specifically related to learned fear". Cell 111 (6): 905–18. 2003. doi:10.1016/S0092-8674(02)01116-9. PMID 12526815. 
• "Increased frequency of gastrin-releasing peptide receptor gene mutations during colon-adenocarcinoma progression". Mol. Carcinog. 37 (1): 5–15. 2003. doi:10.1002/mc.10117. PMID 12720295. 
• "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. 2003. doi:10.1038/sj.bjc.6600957. PMID 12771999. 
• "Gastrin releasing peptide and gastrin releasing peptide receptor expression in gastrointestinal carcinoid tumours". J. Clin. Pathol. 57 (2): 189–92. 2004. doi:10.1136/jcp.2003.10660. PMID 14747448. 
• "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. 2005. doi:10.1124/mol.104.001206. PMID 15361544. 
• "The Status, Quality, and Expansion of the NIH Full-Length cDNA Project: The Mammalian Gene Collection (MGC)". Genome Res. 14 (10B): 2121–7. 2004. doi:10.1101/gr.2596504. PMID 15489334. 

External links

• "Bombesin Receptors: BB₂". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2957. 
• 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.