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Gastrin-releasing peptide receptor: Wikis


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Gastrin-releasing peptide receptor
Symbols GRPR;
External IDs OMIM305670 MGI95836 HomoloGene21098 IUPHAR: BB2 GeneCards: GRPR Gene
RNA expression pattern
PBB GE GRPR 207929 at tn.png
More reference expression data
Species Human Mouse
Entrez 2925 14829
Ensembl ENSG00000126010 ENSMUSG00000031364
UniProt P30550 Q53WV4
RefSeq (mRNA) NM_005314 NM_008177
RefSeq (protein) NP_005305 NP_032203
Location (UCSC) Chr X:
16.05 - 16.08 Mb
Chr X:
158.86 - 158.89 Mb
PubMed search [1] [2]

The gastrin-releasing peptide receptor (GRPR), now properly known as BB2 [1] is a G protein-coupled receptor whose endogenous ligand is gastrin releasing peptide [2]. In humans it is highly expressed in the pancreas and is also expressed in the stomach, adrenal cortex and brain [3].

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.[4]

The transcription factor CREB is a regulator of human GRP-R expression in colon cancer.[5]



  1. ^ "Bombesin Receptors: BB2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.  
  2. ^ 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.  
  3. ^ Corjay MH, Dobrzanski DJ, Way JM, Viallet J, Shapira H, Worland P, Sausville EA and Battey JF (1991). "Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells.". J. Biol. Chem. 266: 18771–18779. PMID 1655761.  
  4. ^ "Entrez Gene: GRPR gastrin-releasing peptide receptor".  
  5. ^ 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: G153. doi:10.1152/ajpgi.00036.2008. PMID 18483184.  

External links

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. 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. 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. 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

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



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