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Gene Review

GRP  -  gastrin-releasing peptide

Homo sapiens

Synonyms: BN, GRP-10, Gastrin-releasing peptide, preproGRP, proGRP
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Disease relevance of GRP


Psychiatry related information on GRP

  • We conclude that BN-related peptides play an important role in the control of food intake, and may contribute to ingestive disruptions associated with anorexia (anorexia nervosa, AIDS and cancer anorexia), bulimia, obesity and depression [5].
  • Total body images were acquired in patients and normal volunteers 1 and 3 h after 99mTc BN acquisition [6].
  • METHODS: To explore further the role of GRP in humans, its effects on satiety and eating behavior were investigated by infusion of GRP into healthy men at three dosages (10, 40, and 160 pmol/kg per hour) and compared with saline infusions [7].
  • When bulls were in GRP and tested first on test days, more (P <0.05) copulations were distributed to the first three females encountered compared with either the fourth female (P <0.05) or to each of the other females in SEQ (P <0.05) [8].
  • Gastrin-releasing peptide: an identity crisis at 30 [9]?

High impact information on GRP


Chemical compound and disease context of GRP


Biological context of GRP


Anatomical context of GRP

  • Therapy with RC-3095 decreased the concentration of BN/GRP receptors on H-128 SCLC tumor membranes [22].
  • Conversely, GRP receptors were identified in only a few hyperplastic prostates and were localized in very low density in glandular tissue and, focally, in some stromal tissue [1].
  • GRP treatment resulted in intracellular calcium [Ca2+]i mobilization in two cell lines (SK-N-SH, LAN-1) [3].
  • RESULTS: Normal uterine tissues expressed GRP receptors (GRP-Rs) in the myometrium, in subsets of secretory endometrial glands, and in subsets of endometrial blood vessels of the late proliferative and the secretory phase [23].
  • Furthermore, expression of GRP receptors, neurokinin (NK)1 receptors, VIP type2-receptors and sst2 receptors was found in the mucosa-directed margin of the circular smooth muscle where the interstitial cells of Cajal are located [24].

Associations of GRP with chemical compounds

  • 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 [1].
  • In addition to TGF-alpha release, GRP induced amphiregulin, but not EGF, secretion into HNSCC cell culture medium, an effect that was blocked by the MMP inhibitor marimastat [25].
  • The affinities of various agonists for binding to the huGRP-R were Bn (Ki = 1.4 +/- 0.2 nM) = 4 x GRP = 300 x NMB [26].
  • GRP also induced the labeling of a large percentage (53%) of the cells with bromodeoxyuridine [27].
  • Both agents markedly inhibited the degradation of GRP, indicating that this process involves a lysosomal pathway and a phosphoramidon-sensitive pathway, possibly involving the EC enzyme [28].

Physical interactions of GRP


Co-localisations of GRP


Regulatory relationships of GRP

  • NMB induced a larger percent change in alkaline phosphatase secretion than GRP with a half maximal response at less than 1 nM NMB [31].
  • All actions of bombesin were blocked by BME (D-Phe(6)-bombesin-(6-13)-methylester), a selective GRP receptor antagonist, but not by the NMB receptor antagonist BIM-23127 (D-Nal-cyclo[Cys-Tyr-D-Trp-Orn-Val-Cys]-Nal-NH(2)).We conclude that HPAF cells express mRNA for GRP receptors and that functional receptors are present in the cell membrane [32].
  • Thus this study demonstrates that GRP receptors are expressed on airway epithelial cells in developing fetal lung and that the interaction of GRP with the GRP receptor stimulates airway development [13].
  • Gastrin-releasing peptide mediates its morphogenic properties in human colon cancer by upregulating intracellular adhesion protein-1 (ICAM-1) via focal adhesion kinase [33].
  • Although we have shown that these processes are mediated by focal adhesion kinase (FAK), the downstream target(s) of GRP-induced FAK activation are not known [33].

Other interactions of GRP

  • To further elucidate the mechanism of activation of EGFR by GRP in HNSCC, we investigated the role of Src family kinases [25].
  • Invasion and growth assays showed that c-Src was required for GRP-induced proliferation or invasion of HNSCC cells [25].
  • Lung tissue GRP, CGRP, and PYY levels appeared to decrease gradually with time, perhaps as a result of the positive pressure ventilation procedure [34].
  • GRP concentrations increased during hypoglycaemia (p < 0.01) while a reduction in AVP occurred at the start of hypoglycaemia (p < 0.001) [35].
  • Levels of gastrin-releasing peptide and substance P in synovial fluid and serum correlate with levels of cytokines in rheumatoid arthritis [36].

Analytical, diagnostic and therapeutic context of GRP

  • In the present study, we have evaluated the expression of GRP receptors in human nonneoplastic and neoplastic prostate tissues using in vitro receptor autoradiography on tissue sections with 125I-Tyr4-bombesin as radio-ligand [1].
  • Apart from suggesting a role of GRP in breast physiology, these data represent the molecular basis for potential clinical applications of GRP analogs such as GRP receptor scintigraphy, radiotherapy, or chemotherapy [2].
  • METHODS: Sections of paraffin-embedded neuroblastomas from 33 patients were analyzed for GRP and GRP-R protein expression by immunohistochemistry [3].
  • Sequence-specific radioimmunoassay demonstrated the presence of substantial amounts of fully processed amidated GRP in the ovine renal cortex and medulla [37].
  • GRP mRNA was detected in rat kidney from embryonic day 19 to postnatal day 30 by RT-PCR [37].


  1. Gastrin-releasing peptide receptors in the human prostate: relation to neoplastic transformation. Markwalder, R., Reubi, J.C. Cancer Res. (1999) [Pubmed]
  2. Gastrin-releasing peptide receptors in non-neoplastic and neoplastic human breast. Gugger, M., Reubi, J.C. Am. J. Pathol. (1999) [Pubmed]
  3. Gastrin-releasing peptide is a growth factor for human neuroblastomas. Kim, S., Hu, W., Kelly, D.R., Hellmich, M.R., Evers, B.M., Chung, D.H. Ann. Surg. (2002) [Pubmed]
  4. Expression of mRNA for gastrin-releasing peptide receptor by human bronchial epithelial cells. Association with prolonged tobacco exposure and responsiveness to bombesin-like peptides. Siegfried, J.M., DeMichele, M.A., Hunt, J.D., Davis, A.G., Vohra, K.P., Pilewski, J.M. Am. J. Respir. Crit. Care Med. (1997) [Pubmed]
  5. Role of bombesin-related peptides in the control of food intake. Merali, Z., McIntosh, J., Anisman, H. Neuropeptides (1999) [Pubmed]
  6. Phase I trial of technetium [Leu13] bombesin as cancer seeking agent: possible scintigraphic guide for surgery? De Vincentis, G., Scopinaro, F., Varvarigou, A., Ussof, W., Schillaci, O., Archimandritis, S., Corleto, V., Longo, F., Delle Fave, G. Tumori. (2002) [Pubmed]
  7. Effect of intravenous human gastrin-releasing peptide on food intake in humans. Gutzwiller, J.P., Drewe, J., Hildebrand, P., Rossi, L., Lauper, J.Z., Beglinger, C. Gastroenterology (1994) [Pubmed]
  8. Effects of sequential or group exposure to unrestrained estrual females on expression of sexual behavior in sexually experienced beef bulls. Bailey, J.D., Anderson, L.H., Schillo, K.K. J. Anim. Sci. (2005) [Pubmed]
  9. Gastrin-releasing peptide: an identity crisis at 30? Dockray, G.J. Lancet (2001) [Pubmed]
  10. Bombesin-like peptides can function as autocrine growth factors in human small-cell lung cancer. Cuttitta, F., Carney, D.N., Mulshine, J., Moody, T.W., Fedorko, J., Fischler, A., Minna, J.D. Nature (1985) [Pubmed]
  11. 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]
  12. 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]
  13. A rhesus monkey model to characterize the role of gastrin-releasing peptide (GRP) in lung development. Evidence for stimulation of airway growth. Li, K., Nagalla, S.R., Spindel, E.R. J. Clin. Invest. (1994) [Pubmed]
  14. Bombesin specifically induces intracellular calcium mobilization via gastrin-releasing peptide receptors in human prostate cancer cells. Aprikian, A.G., Han, K., Chevalier, S., Bazinet, M., Viallet, J. J. Mol. Endocrinol. (1996) [Pubmed]
  15. Gastrin releasing peptide receptor expression is decreased in patients with Crohn's disease but not in ulcerative colitis. ter Beek, W.P., Muller, E.S., Van Hogezand, R.A., Biemond, I., Lamers, C.B. J. Clin. Pathol. (2004) [Pubmed]
  16. Effect of somatostatin analog RC-160 and bombesin/gastrin releasing peptide antagonist RC-3095 on growth of PC-3 human prostate-cancer xenografts in nude mice. Pinski, J., Schally, A.V., Halmos, G., Szepeshazi, K. Int. J. Cancer (1993) [Pubmed]
  17. Effect of sepsis or cytokine administration on release of gut peptides. Zamir, O., Hasselgren, P.O., Higashiguchi, T., Frederick, J.A., Fischer, J.E. Am. J. Surg. (1992) [Pubmed]
  18. Bombesin/gastrin-releasing peptide receptor antagonists increase the ability of histone deacetylase inhibitors to reduce lung cancer proliferation. Moody, T.W., Nakagawa, T., Kang, Y., Jakowlew, S., Chan, D., Jensen, R.T. J. Mol. Neurosci. (2006) [Pubmed]
  19. 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]
  20. 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]
  21. Neuromedin B binds with high affinity, elevates cytosolic calcium and stimulates the growth of small-cell lung cancer cell lines. Moody, T.W., Staley, J., Zia, F., Coy, D.H., Jensen, R.T. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  22. Reduction in receptors for bombesin and epidermal growth factor in xenografts of human small-cell lung cancer after treatment with bombesin antagonist RC-3095. Halmos, G., Schally, A.V. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  23. Gastrin-releasing peptide receptors in normal and neoplastic human uterus: involvement of multiple tissue compartments. Fleischmann, A., Waser, B., Gebbers, J.O., Reubi, J.C. J. Clin. Endocrinol. Metab. (2005) [Pubmed]
  24. Localization and characterization of neuropeptide receptors in human colon. Rettenbacher, M., Reubi, J.C. Naunyn Schmiedebergs Arch. Pharmacol. (2001) [Pubmed]
  25. SRC family kinases mediate epidermal growth factor receptor ligand cleavage, proliferation, and invasion of head and neck cancer cells. Zhang, Q., Thomas, S.M., Xi, S., Smithgall, T.E., Siegfried, J.M., Kamens, J., Gooding, W.E., Grandis, J.R. Cancer Res. (2004) [Pubmed]
  26. Expression and characterization of cloned human bombesin receptors. Benya, R.V., Kusui, T., Pradhan, T.K., Battey, J.F., Jensen, R.T. Mol. Pharmacol. (1995) [Pubmed]
  27. Bombesin-like peptide receptor subtypes promote mitogenesis, which requires persistent receptor signaling. Feldman, R.I., Bartholdi, M.F., Wu, J.M. Mol. Pharmacol. (1996) [Pubmed]
  28. Characterization of ligand binding and processing by gastrin-releasing peptide receptors in a small-cell lung cancer cell line. Cardona, C., Bleehen, N.M., Reeve, J.G. Biochem. J. (1992) [Pubmed]
  29. Analysis of the phase shifting effects of gastrin releasing peptide when microinjected into the suprachiasmatic region. Albers, H.E., Gillespie, C.F., Babagbemi, T.O., Huhman, K.L. Neurosci. Lett. (1995) [Pubmed]
  30. Colocalization of neuropeptides with calbindin D28k and NADPH diaphorase in the enteric nerve plexuses of normal human ileum. Dhatt, N., Buchan, A.M. Gastroenterology (1994) [Pubmed]
  31. Effects of bombesin family peptides and antagonists on guinea pig nasal mucosal secretion. Ali, M., Gawin, A.Z., Baraniuk, J.N. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  32. GRP-receptor-mediated signal transduction, gene expression and DNA synthesis in the human pancreatic adenocarcinoma cell line HPAF. Burghardt, B., Wenger, C., Barabás, K., Rácz, G., Oláh, A., Flautner, L., Coy, D.H., Gress, T.M., Varga, G. Peptides (2001) [Pubmed]
  33. 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]
  34. Oxygen toxicity in the infant rhesus monkey: effects on regulatory peptides in lung and blood. Keith, I.M., Ekman, R., Farrell, P.M. Pediatr. Pulmonol. (1988) [Pubmed]
  35. The response of regulatory peptides to moderate hypoglycaemia of short duration in type 1 (insulin-dependent) diabetes mellitus and in normal man. Tallroth, G., Ryding, E., Ekman, R., Agardh, C.D. Diabetes Res. (1992) [Pubmed]
  36. Levels of gastrin-releasing peptide and substance P in synovial fluid and serum correlate with levels of cytokines in rheumatoid arthritis. Grimsholm, O., Rantapää-Dahlqvist, S., Forsgren, S. Arthritis Res. Ther. (2005) [Pubmed]
  37. Developmental expression and biological activity of gastrin-releasing peptide and its receptors in the kidney. Dumesny, C., Whitley, J.C., Baldwin, G.S., Giraud, A.S., Shulkes, A. Am. J. Physiol. Renal Physiol. (2004) [Pubmed]
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