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Gene Review

Grp  -  gastrin releasing peptide

Rattus norvegicus

Synonyms: GRP, Gastrin-releasing peptide
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Disease relevance of Grp


Psychiatry related information on Grp

  • The observations suggest that GRP may be one of several neural messengers involved in the control of uterine motor activity [5].
  • Exogenous GRP and NMB, in particular, appear to interact with processes stimulated by the postingestive actions of food, supporting a role for peripheral, endogenous GRP and NMB in the development of satiation and the maintenance of postprandial satiety, respectively [6].

High impact information on Grp


Chemical compound and disease context of Grp


Biological context of Grp


Anatomical context of Grp

  • GRP binds specifically to a high affinity site in rat brain membranes, with a Kd equal to 2 nM and Bmax equal to 5 pmol/g wet weight of tissue [18].
  • MEASUREMENTS AND MAIN RESULTS: The GRP antagonist attenuated LPS- or CLP-induced TNF-alpha, IL-1beta, and nitric oxide release in cultured macrophages and decreased the mRNA levels of inducible nitric oxide synthase [1].
  • The biochemical and pharmacological characteristics of specific binding sites for gastrin-releasing peptide (GRP) were investigated in normal exocrine pancreas and in an azaserine-induced pancreatic carcinoma in the rat, under similar experimental conditions [14].
  • Scatchard analysis of equilibrium data obtained with normal and tumor plasma membranes indicated a single class of high-affinity sites (KD = 0.42 +/- 0.06 and 0.35 +/- 0.05 nM, respectively), but the number of GRP receptors was significantly different (Bmax = 31 +/- 4.5 and 189 +/- 20 fmol/mg protein, respectively) [14].
  • In comparison with epithelial cells expressing wild-type GRPR, the GRPR-GFP expressing cells showed similar ligand binding affinity, GRP-stimulated Ca2+ signaling, and GRP-initiated internalization [19].

Associations of Grp with chemical compounds

  • KNRK cells expressing the GRP receptor rapidly internalized bound 125I-GRP at 37 degree C. Internalization was inhibited at 4 degrees C and by 0.45 m sucrose [20].
  • Therefore, the highly conserved tyrosine 324 does not have a role in GRP binding, receptor-G-protein interaction, or initial events of ligand induced receptor internalization [20].
  • The bombesin-related peptides gastrin-releasing peptide (GRP) and neuromedin B (NMB) have been demonstrated in the anterior pituitary (AP) on an immunological basis [21].
  • NMB mRNA is more prominent than GRP mRNA in all AP-like tissues examined (fresh AP, estradiol-treated reaggregate AP cell cultures and GH3 cells) [21].
  • Specific 125I-GRP binding was 500, 700 and 1400 fmol/mg protein, respectively, in the 0-25%, 25-50% and 50-80% saturated ammonium sulfate fractions (125I-GRP concentration = 1 nM) [22].

Regulatory relationships of Grp


Other interactions of Grp

  • The internalization of bound 125I-GRP by the mutant GRP receptor was identical to the wild type receptor [20].
  • This stress-induced activation of both the serotonergic neurons and the hypothalamus-pituitary-adrenal axis was blocked by CRF and GRP antagonists [27].
  • In turn, it appears that endogenous GRP and CRF receptor ligands are both simultaneously involved in the regulation of the increase in 5-HT neuronal activity, ACTH and corticosterone secretion, under stress conditions [27].
  • The CCKB/gastrin receptor antagonist CI-988 (1 microM) had no effect on either GRP- or NMC-mediated excitation [28].
  • Early adaptation of pancreas to a protein-enriched diet: role of cholecystokinin and gastrin-releasing peptide [29].

Analytical, diagnostic and therapeutic context of Grp


  1. Gastrin-releasing peptide receptor antagonist effects on an animal model of sepsis. Dal-Pizzol, F., Di Leone, L.P., Ritter, C., Martins, M.R., Reinke, A., Pens Gelain, D., Zanotto-Filho, A., de Souza, L.F., Andrades, M., Barbeiro, D.F., Bernard, E.A., Cammarota, M., Bevilaqua, L.R., Soriano, F.G., Cláudio, J., Moreira, F., Roesler, R., Schwartsmann, G. Am. J. Respir. Crit. Care Med. (2006) [Pubmed]
  2. Gastrin-releasing peptide: in vivo and in vitro growth effects on an acinar pancreatic carcinoma. Hajri, A., Balboni, G., Koenig, M., Garaud, J.C., Damgé, C. Cancer Res. (1992) [Pubmed]
  3. Pharmacological characteristics of bombesin receptor mediating hypothermia in the central nervous system of rats. Tsushima, H., Mori, M., Fujiwara, N., Moriyama, A. Brain Res. (2003) [Pubmed]
  4. Inhibitory effects of somatostatin analogue RC-160 and bombesin/gastrin-releasing peptide antagonist RC-3095 on the growth of the androgen-independent Dunning R-3327-AT-1 rat prostate cancer. Pinski, J., Reile, H., Halmos, G., Groot, K., Schally, A.V. Cancer Res. (1994) [Pubmed]
  5. Neuronal localization and motor effects of gastrin-releasing peptide (GRP) in rat uterus. Stjernquist, M., Ekblad, E., Owman, C., Sundler, F. Regul. Pept. (1986) [Pubmed]
  6. Prefeeding potentiates anorectic actions of neuromedin B and gastrin releasing peptide. Kirkham, T.C., Perez, S., Gibbs, J. Physiol. Behav. (1995) [Pubmed]
  7. Selective ligand-induced intracellular calcium changes in a population of rat isolated gastric endocrine cells. Zeng, N., Walsh, J.H., Kang, T., Helander, K.G., Helander, H.F., Sachs, G. Gastroenterology (1996) [Pubmed]
  8. Pancreatic polypeptide secretion from the isolated perfused ventral and dorsal areas of the rat pancreas. Miyazaki, K., Funakoshi, A. Gastroenterology (1988) [Pubmed]
  9. Autoradiographic demonstration of gastrin-releasing peptide-binding sites in the rat gastric mucosa. Nakamura, M., Oda, M., Kaneko, K., Akaiwa, Y., Tsukada, N., Komatsu, H., Tsuchiya, M. Gastroenterology (1988) [Pubmed]
  10. Effects of a transplantable insulinoma upon regulatory peptide concentrations in the gastrointestinal tract of the rat. Conlon, J.M., Deacon, C.F., Bailey, C.J., Flatt, P.R. Diabetologia (1986) [Pubmed]
  11. Somatostatin, gastrin-releasing peptide and gastrin in the stomach of rats with streptozotocin-induced diabetes and insulinoma. Flatt, P.R., Bailey, C.J., Conlon, J.M. J. Nutr. (1991) [Pubmed]
  12. Capsaicin-sensitive vagal fibres and 5-HT3-, gastrin releasing peptide- and cholecystokinin A-receptors are involved in distension-induced inhibition of gastric emptying in the rat. Bozkurt, A., Oktar, B.K., Kurtel, H., Alican, I., Coşkun, T., Yeğen, B.C. Regul. Pept. (1999) [Pubmed]
  13. Mechanisms underlying anorexia after microinjection of bombesin into the lateral cerebroventricle. Tsushima, H., Mori, M. Pharmacol. Biochem. Behav. (2005) [Pubmed]
  14. Expression and characterization of gastrin-releasing peptide receptor in normal and cancerous pancreas. Hajri, A., Koenig, M., Balboni, G., Damgé, C. Pancreas (1996) [Pubmed]
  15. The rat prepro gastrin releasing peptide gene is transcribed from two initiation sites in the brain. Lebacq-Verheyden, A.M., Krystal, G., Sartor, O., Way, J., Battey, J.F. Mol. Endocrinol. (1988) [Pubmed]
  16. Effect of the gastrin-releasing peptide antagonist BIM 26226 and lanreotide on an acinar pancreatic carcinoma. Damgé, C., Hajri, A. Eur. J. Pharmacol. (1998) [Pubmed]
  17. Sustained bombesin exposure results in receptor down-regulation and tolerance to the chronic but not acute effects of bombesin on ingestion. Plamondon, H., Lambert, C., Merali, Z. Brain Res. (1998) [Pubmed]
  18. Gastrin-releasing peptide receptor in rat brain membranes: specific binding and stimulation of phosphoinositide breakdown. Hollingsworth, E.B. Mol. Pharmacol. (1989) [Pubmed]
  19. Visualization of internalization and recycling of the gastrin releasing peptide receptor-green fluorescent protein chimera expressed in epithelial cells. Slice, L.W., Yee, H.F., Walsh, J.H. Recept. Channels (1998) [Pubmed]
  20. The conserved NPXnY motif present in the gastrin-releasing peptide receptor is not a general sequestration sequence. Slice, L.W., Wong, H.C., Sternini, C., Grady, E.F., Bunnett, N.W., Walsh, J.H. J. Biol. Chem. (1994) [Pubmed]
  21. Expression of the genes encoding bombesin-related peptides and their receptors in anterior pituitary tissue. Houben, H., Vandenbroucke, A.T., Verheyden, A.M., Denef, C. Mol. Cell. Endocrinol. (1993) [Pubmed]
  22. Isolation of a gastrin releasing peptide receptor from normal rat pancreas. Kane, M.A., Kelley, K., Ross, S.E., Portanova, L.B. Peptides (1991) [Pubmed]
  23. Increased sensitivity of gastrin cells to gastric distension following antral denervation in the rat. Higham, A., Noble, P., Thompson, D.G., Dockray, G.J. J. Physiol. (Lond.) (1997) [Pubmed]
  24. Evidence for a physiological role of hypothalamic gastrin-releasing peptide to suppress growth hormone and prolactin release in the rat. Kentroti, S., Dees, W.L., McCann, S.M. Proc. Natl. Acad. Sci. U.S.A. (1988) [Pubmed]
  25. Gastrin-releasing peptide stimulates cholecystokinin secretion in perfused rat duodenum. Nakano, I., Miyazaki, K., Funakoshi, A., Tateishi, K., Hamaoka, T., Yajima, H. Regul. Pept. (1988) [Pubmed]
  26. Regulation of cholecystokinin secretion by food, hormones, and neural pathways in the rat. Lewis, L.D., Williams, J.A. Am. J. Physiol. (1990) [Pubmed]
  27. Gastrin-releasing peptide mediated regulation of 5-HT neuronal activity in the hypothalamic paraventricular nucleus under basal and restraint stress conditions. Garrido, M.M., Fuentes, J.A., Manzanares, J. Life Sci. (2002) [Pubmed]
  28. Different types of bombesin receptors on neurons in the dorsal raphe nucleus and the rostral hypothalamus in rat brain slices in vitro. Pinnock, R.D., Reynolds, T., Woodruff, G.N. Brain Res. (1994) [Pubmed]
  29. Early adaptation of pancreas to a protein-enriched diet: role of cholecystokinin and gastrin-releasing peptide. Lhoste, E.F., Fiszlewicz, M., Gueugneau, A.M., Tranchant, T., Corring, T. Pancreas (1994) [Pubmed]
  30. Gastrin-releasing peptide microinjected into the amygdala inhibits feeding. Fekete, E., Vígh, J., Bagi, E.E., Lénárd, L. Brain Res. (2002) [Pubmed]
  31. Development of a radioimmunoassay for a pseudononapeptide bombesin/GRP antagonist with antitumor activity. Groot, K., Horvàth, J.E., Cai, R.Z., Schally, A.V. Int. J. Pept. Protein Res. (1995) [Pubmed]
  32. Central nervous system inhibition of gastric secretion in the rat by gastrin-releasing peptide, a mammalian bombesin. Taché, Y., Marki, W., Rivier, J., Vale, W., Brown, M. Gastroenterology (1981) [Pubmed]
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