Gastrin-releasing peptide receptor

GRPR
Identifiers
Aliases	GRPR, BB2, gastrin releasing peptide receptor, BB2R, BRS2
External IDs	OMIM: 305670; MGI: 95836; HomoloGene: 21098; GeneCards: GRPR; OMA:GRPR - orthologs
Gene location (Human)
Chr.	X chromosome (human)
End	16,153,518 bp
Gene location (Mouse)
Chr.	X chromosome (mouse)
End	162,332,673 bp
RNA expression pattern
	Top expressed in
	gonad; ; testicle; ; buccal mucosa cell; ; body of pancreas; ; pancreatic ductal cell; ; stromal cell of endometrium; ; deltoid muscle; ; epithelium of colon; ; gastric mucosa; ; smooth muscle tissue;
	Top expressed in
	lumbar spinal ganglion; ; lumbar subsegment of spinal cord; ; supraoptic nucleus; ; embryo; ; dentate gyrus of hippocampal formation granule cell; ; vestibular membrane of cochlear duct; ; ankle joint; ; tibiofemoral joint; ; genital tubercle; ; suprachiasmatic nucleus;
	More reference expression data
	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
	2925
	14829
	ENSG00000126010
	ENSMUSG00000031364
	P30550
	P21729
	NM_005314
	NM_008177
	NP_005305; NP_005305.1
	NP_032203
	Wikidata
View/Edit Human	View/Edit Mouse

The gastrin-releasing peptide receptor (GRPR), now properly known as BB₂ ^[5] is a G protein-coupled receptor whose endogenous ligand is gastrin releasing peptide.^[6] In humans it is highly expressed in the pancreas and is also expressed in the stomach, adrenal cortex and brain.^[7]

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.^[8]

The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.^[9]

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

References

^ ^a ^b ^c GRCh38: Ensembl release 89: ENSG00000126010 – Ensembl, May 2017
^ ^a ^b ^c GRCm38: Ensembl release 89: ENSMUSG00000031364 – Ensembl, May 2017
^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ "Bombesin Receptors: BB₂". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
^ 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.
^ Corjay MH, Dobrzanski DJ, Way JM, Viallet J, Shapira H, Worland P, Sausville EA, Battey JF (1991). "Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells". J. Biol. Chem. 266 (28): 18771–18779. doi:10.1016/S0021-9258(18)55129-2. PMID 1655761.
^ "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. 295 (1): G153–G162. doi:10.1152/ajpgi.00036.2008. PMC 2494719. PMID 18483184.

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)