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Gene Review

GRPR  -  gastrin-releasing peptide receptor

Homo sapiens

Synonyms: BB2, GRP-R, GRP-preferring bombesin receptor, Gastrin-releasing peptide receptor
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Disease relevance of GRPR

  • The presence of two expressed copies of the GRPR gene in females may be a factor in the increased susceptibility of women to tobacco-induced lung cancer [1].
  • Thus, these findings suggest that expression of GRP/GRPR in cancer inhibits metastasis by enhancing cell attachment to the matrix, regulating motility in the context of remodeling, and decreasing deformability [2].
  • Additionally, we have detected transcripts for GRPR and NMBR in four of seven and seven of seven cases, respectively, of cultured non-small cell lung carcinomas (NSCLC) [3].
  • Importantly, GRPR mRNA is ubiquitously mutated in human colon cancer cell lines, with inactivating mutations detected in all cell lines not expressing functional receptor [4].
  • Of the 22 prostate cancer specimens analyzed by RT-PCR, 20 (91%) expressed GRPR mRNA, 3 (14%) showed NMBR mRNA, and 2 ( approximately 9%) revealed BRS-3 mRNA [5].

Psychiatry related information on GRPR


High impact information on GRPR

  • We used neutralizing GRP monoclonal antibody 2A11 to block the GRP-GRPR interaction in SCCHN cell lines and xenografts and assessed the antibody's effect on proliferation by counting cultured cells or measuring xenograft tumor volume in vivo [10].
  • METHODS: We assessed GRPR messenger RNA (mRNA) expression in specimens from 25 patients with SCCHN, six control noncancer patients, and 14 SCCHN cell lines by use of quantitative reverse transcriptase-polymerase chain reaction [10].
  • SCCHN cells expressed fivefold higher levels of GRPR mRNA than did cultured normal mucosal epithelial cells (P =.005) [10].
  • The levels of GRPR expression in the tumor and adjacent normal epithelium of individual patients with SCCHN were correlated (r =.652; P =.001), suggesting that increased GRPR expression is an early event in SCCHN formation [10].
  • Because expression of GRPR, however, has not been reported in squamous cell carcinoma of the head and neck (SCCHN), we investigated its expression and that of its ligand GRP in normal mucosa and SCCHN tissues and the involvement of these proteins in the proliferation of SCCHN cells [10].

Chemical compound and disease context of GRPR


Biological context of GRPR


Anatomical context of GRPR


Associations of GRPR with chemical compounds

  • Combining a GRPR antagonist with the EGFR tyrosine kinase inhibitor, gefitinib, resulted in additive cytotoxic effects [18].
  • In all of the cases, the receptors corresponded to the GRP receptor subtype of bombesin receptors, having high affinity for GRP and bombesin and lower affinity for neuromedin B [11].
  • Androgen-dependent expression of the gastrin-releasing Peptide receptor in human prostate tumor xenografts [19].
  • GRP receptor mRNA was expressed predominantly in the luminal and basal epithelial cells in both histologically normal and cancerous glands within sections of normal (3 cases) and diseased (37 cases) tissue [20].
  • Bombesin (BN) is a tetradecapeptide that binds with high affinity to GRPR and can be radiolabeled with the positron-emitter, copper-64 ((64)Cu) for imaging with positron-emission tomography (PET) [21].

Physical interactions of GRPR

  • An increase in GRP binding capacity was confirmed in GRP-R overexpressing cells, which demonstrated an accelerated constitutive cell growth rate [22].

Regulatory relationships of GRPR

  • We demonstrated that the activity of MEK is important for maintaining elevated [Ca(2+)](i) levels induced by GRP-R activation, suggesting that MEK may affect receptor-regulated secretion by modulating the activity of Ca(2+)-sensitive PKC [23].
  • Yet GRP has not been shown to be expressed by colon cancers in humans nor has the effect of GRP and/or GRPR coexpression on tumor behavior been investigated [24].
  • This novel signaling mechanism might be of importance for regulation of CREB-dependent gene expression in human cancer expressing functional hGRP-R [25].
  • Further evaluation revealed that GRP-R in these cells tonically stimulated G alpha q/11, resulting in increased phospholipase C activation [26].
  • Previously, we demonstrated that the human gastric cancer SIIA possesses GRP-R and that BBS stimulates activator protein-1 (AP-1) gene expression [27].

Other interactions of GRPR


Analytical, diagnostic and therapeutic context of GRPR


  1. Sex-specific expression of gastrin-releasing peptide receptor: relationship to smoking history and risk of lung cancer. Shriver, S.P., Bourdeau, H.A., Gubish, C.T., Tirpak, D.L., Davis, A.L., Luketich, J.D., Siegfried, J.M. J. Natl. Cancer Inst. (2000) [Pubmed]
  2. Phosphorylation of focal adhesion kinase tyrosine 397 critically mediates gastrin-releasing peptide's morphogenic properties. Glover, S., Delaney, M., Dematte, C., Kornberg, L., Frasco, M., Tran-Son-Tay, R., Benya, R.V. J. Cell. Physiol. (2004) [Pubmed]
  3. Expression of mRNA for three bombesin receptor subtypes in human bronchial epithelial cells. DeMichele, M.A., Davis, A.L., Hunt, J.D., Landreneau, R.J., Siegfried, J.M. Am. J. Respir. Cell Mol. Biol. (1994) [Pubmed]
  4. Increased frequency of gastrin-releasing peptide receptor gene mutations during colon-adenocarcinoma progression. Glover, S.C., Tretiakova, M.S., Carroll, R.E., Benya, R.V. Mol. Carcinog. (2003) [Pubmed]
  5. Presence of receptors for bombesin/gastrin-releasing peptide and mRNA for three receptor subtypes in human prostate cancers. Sun, B., Halmos, G., Schally, A.V., Wang, X., Martinez, M. Prostate (2000) [Pubmed]
  6. Molecular mechanisms mediating gastrin-releasing peptide receptor modulation of memory consolidation in the hippocampus. Roesler, R., Luft, T., Oliveira, S.H., Farias, C.B., Almeida, V.R., Quevedo, J., Dal Pizzol, F., Schröder, N., Izquierdo, I., Schwartsmann, G. Neuropharmacology (2006) [Pubmed]
  7. Gastrin-releasing Peptide receptor as a molecular target for psychiatric and neurological disorders. Roesler, R., Henriques, J.A., Schwartsmann, G. CNS & neurological disorders drug targets. (2006) [Pubmed]
  8. Exclusion of the gastrin-releasing peptide receptor (GRPR) locus as a candidate gene for Rett syndrome. Heidary, G., Hampton, L.L., Schanen, N.C., Rivkin, M.J., Darras, B.T., Battey, J., Francke, U. Am. J. Med. Genet. (1998) [Pubmed]
  9. Gastrin-releasing peptide receptor (GRPR) locus in Japanese subjects with autism. Marui, T., Hashimoto, O., Nanba, E., Kato, C., Tochigi, M., Umekage, T., Kato, N., Sasaki, T. Brain Dev. (2004) [Pubmed]
  10. Gastrin-releasing peptide receptor-mediated autocrine growth in squamous cell carcinoma of the head and neck. Lango, M.N., Dyer, K.F., Lui, V.W., Gooding, W.E., Gubish, C., Siegfried, J.M., Grandis, J.R. J. Natl. Cancer Inst. (2002) [Pubmed]
  11. Gastrin-releasing peptide receptors in the human prostate: relation to neoplastic transformation. Markwalder, R., Reubi, J.C. Cancer Res. (1999) [Pubmed]
  12. Selective targeting and inducible destruction of human cancer cells by retroviruses with envelope proteins bearing short peptide ligands. Gollan, T.J., Green, M.R. J. Virol. (2002) [Pubmed]
  13. Effect of bombesin, gastrin-releasing peptide (GRP)(14-27) and bombesin/GRP receptor antagonist RC-3095 on growth of nitrosamine-induced pancreatic cancers in hamsters. Szepeshazi, K., Schally, A.V., Groot, K., Halmos, G. Int. J. Cancer (1993) [Pubmed]
  14. Stimulation of proliferation and migration of a colorectal cancer cell line by amidated and glycine-extended gastrin-releasing peptide via the same receptor. Patel, O., Dumesny, C., Giraud, A.S., Baldwin, G.S., Shulkes, A. Biochem. Pharmacol. (2004) [Pubmed]
  15. Autism and multiple exostoses associated with an X;8 translocation occurring within the GRPR gene and 3' to the SDC2 gene. Ishikawa-Brush, Y., Powell, J.F., Bolton, P., Miller, A.P., Francis, F., Willard, H.F., Lehrach, H., Monaco, A.P. Hum. Mol. Genet. (1997) [Pubmed]
  16. Gastrin-releasing peptide mediates its morphogenic properties in human colon cancer by upregulating intracellular adhesion protein-1 (ICAM-1) via focal adhesion kinase. Taglia, L., Matusiak, D., Matkowskyj, K.A., Benya, R.V. Am. J. Physiol. Gastrointest. Liver Physiol. (2007) [Pubmed]
  17. Gastrin releasing peptide and gastrin releasing peptide receptor expression in gastrointestinal carcinoid tumours. Scott, N., Millward, E., Cartwright, E.J., Preston, S.R., Coletta, P.L. J. Clin. Pathol. (2004) [Pubmed]
  18. Gastrin-releasing peptide receptor mediates activation of the epidermal growth factor receptor in lung cancer cells. Thomas, S.M., Grandis, J.R., Wentzel, A.L., Gooding, W.E., Lui, V.W., Siegfried, J.M. Neoplasia (2005) [Pubmed]
  19. Androgen-dependent expression of the gastrin-releasing Peptide receptor in human prostate tumor xenografts. de Visser, M., van Weerden, W.M., de Ridder, C.M., Reneman, S., Melis, M., Krenning, E.P., de Jong, M. J. Nucl. Med. (2007) [Pubmed]
  20. In situ hybridization for gastrin-releasing peptide receptor (GRP receptor) expression in prostatic carcinoma. Bartholdi, M.F., Wu, J.M., Pu, H., Troncoso, P., Eden, P.A., Feldman, R.I. Int. J. Cancer (1998) [Pubmed]
  21. MicroPET Imaging of Breast Cancer Using Radiolabeled Bombesin Analogs Targeting the Gastrin-releasing Peptide Receptor. Parry, J.J., Andrews, R., Rogers, B.E. Breast Cancer Res. Treat. (2007) [Pubmed]
  22. Gastrin-releasing peptide-induced down-regulation of tumor suppressor protein PTEN (phosphatase and tensin homolog deleted on chromosome ten) in neuroblastomas. Qiao, J., Kang, J., Cree, J., Evers, B.M., Chung, D.H. Ann. Surg. (2005) [Pubmed]
  23. Multiple protein kinase pathways are involved in gastrin-releasing peptide receptor-regulated secretion. Hellmich, M.R., Ives, K.L., Udupi, V., Soloff, M.S., Greeley, G.H., Christensen, B.N., Townsend, C.M. J. Biol. Chem. (1999) [Pubmed]
  24. Aberrant expression of gastrin-releasing peptide and its receptor by well-differentiated colon cancers in humans. Carroll, R.E., Matkowskyj, K.A., Chakrabarti, S., McDonald, T.J., Benya, R.V. Am. J. Physiol. (1999) [Pubmed]
  25. Human gastrin-releasing peptide receptor mediates sustained CREB phosphorylation and transactivation in HuTu 80 duodenal cancer cells. Qu, X., Xiao, D., Weber, H.C. FEBS Lett. (2002) [Pubmed]
  26. Constitutive activation of the gastrin-releasing peptide receptor expressed by the nonmalignant human colon epithelial cell line NCM460. Ferris, H.A., Carroll, R.E., Rasenick, M.M., Benya, R.V. J. Clin. Invest. (1997) [Pubmed]
  27. Signaling mechanisms regulating bombesin-mediated AP-1 gene induction in the human gastric cancer SIIA. Kim, H.J., Evers, B.M., Litvak, D.A., Hellmich, M.R., Townsend, C.M. Am. J. Physiol., Cell Physiol. (2000) [Pubmed]
  28. Activation of extracellular signal-regulated kinase mediates bombesin-induced mitogenic responses in prostate cancer cells. Xiao, D., Qu, X., Weber, H.C. Cell. Signal. (2003) [Pubmed]
  29. Expression of progastrin-releasing peptide and gastrin-releasing peptide receptor mRNA transcripts in tumor cells of patients with small cell lung cancer. Uchida, K., Kojima, A., Morokawa, N., Tanabe, O., Anzai, C., Kawakami, M., Eto, Y., Yoshimura, K. J. Cancer Res. Clin. Oncol. (2002) [Pubmed]
  30. Characterization of a bombesin/gastrin-releasing peptide receptor on a human gastric-cancer cell line. Preston, S.R., Woodhouse, L.F., Gokhale, J., Miller, G.V., Primrose, J.N. Int. J. Cancer (1994) [Pubmed]
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