Gastrin-releasing peptide receptor

For other uses, see BB2 (disambiguation).

GRPR
Identifiers
Aliases	GRPR, BB2, gastrin releasing peptide receptor, BB2R, BRS2
External IDs	OMIM: 305670 MGI: 95836 HomoloGene: 21098 GeneCards: GRPR
Gene location (Human) Chr. X chromosome (human) Band Xp22.2 Start 16,123,565 bp End 16,153,518 bp
Gene location (Mouse) Chr. X chromosome (mouse) Band X F5|X 75.63 cM Start 162,296,900 bp End 162,332,673 bp
RNA expression pattern Bgee Human Mouse (ortholog) Top expressed in body of pancreas pancreatic ductal cell stromal cell of endometrium deltoid muscle gastric mucosa smooth muscle tissue monocyte islet of Langerhans sigmoid colon prefrontal cortex Top expressed in supraoptic nucleus ankle joint suprachiasmatic nucleus right ventricle vastus lateralis muscle adrenal gland large intestine colon hippocampus proper superior frontal gyrus More reference expression data BioGPS More reference expression data
Gene ontology Molecular function signal transducer activity G protein-coupled receptor activity G protein-coupled peptide receptor activity neuropeptide receptor activity neuropeptide binding Cellular component membrane integral component of membrane plasma membrane integral component of plasma membrane Biological process regulation of cell population proliferation signal transduction cell population proliferation G protein-coupled receptor signaling pathway psychomotor behavior response to external biotic stimulus phospholipase C-activating G protein-coupled receptor signaling pathway neuropeptide signaling pathway social behavior motor behavior learning or memory Sources:Amigo / QuickGO
Orthologs Species Human Mouse Entrez 2925 14829 Ensembl ENSG00000126010 ENSMUSG00000031364 UniProt P30550 P21729 RefSeq (mRNA) NM_005314 NM_008177 RefSeq (protein) NP_005305 NP_005305.1 NP_032203 Location (UCSC) Chr X: 16.12 – 16.15 Mb Chr X: 162.3 – 162.33 Mb PubMed search
Wikidata
View/Edit Human View/Edit Mouse

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

• 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. doi:10.1016/S0021-9258(18)55129-2. 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. S2CID 20854144.
• 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. S2CID 15515339.
• 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. S2CID 26497603.
• 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. S2CID 20563506.
• 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. S2CID 23764903.
• 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. Bibcode:2002PNAS...9916899M. 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. S2CID 16950847.
• 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. S2CID 35607051.
• 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. S2CID 31811739.
• 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. Archived from the original on 2016-03-03. Retrieved 2007-10-25.
• IUPHAR GPCR Database - BB₂ receptor Archived 2016-03-03 at the Wayback Machine
• Receptors,+Bombesin at the U.S. 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.