Gene Symbol: Grpr
Description: gastrin releasing peptide receptor
Alias: GRP-R, gastrin-releasing peptide receptor, GRP-preferring bombesin receptor
Species: mouse
Products:     Grpr

Top Publications

  1. Maslen G, Boyd Y. Comparative mapping of the Grpr locus on the X chromosomes of man and mouse. Genomics. 1993;17:106-9 pubmed
    ..We have mapped the mouse gastrin-releasing peptide receptor (Grpr) locus using a polymorphic CAn repeat located in the 5' untranslated region of the gene and a Mus spretus/Mus ..
  2. Persson K, Pacini G, Sundler F, Ahren B. Islet function phenotype in gastrin-releasing peptide receptor gene-deficient mice. Endocrinology. 2002;143:3717-26 pubmed
    ..To explore whether islet GRP contributes to neurally mediated insulin secretion, we studied GRP receptor (GRPR)-deleted mice...
  3. Maekawa F, Quah H, Tanaka K, Ohki Hamazaki H. Leptin resistance and enhancement of feeding facilitation by melanin-concentrating hormone in mice lacking bombesin receptor subtype-3. Diabetes. 2004;53:570-6 pubmed
  4. Qiao J, Kang J, Ishola T, Rychahou P, Evers B, Chung D. Gastrin-releasing peptide receptor silencing suppresses the tumorigenesis and metastatic potential of neuroblastoma. Proc Natl Acad Sci U S A. 2008;105:12891-6 pubmed publisher
    ..Our findings demonstrate that GRP and GRP-R have important oncogenic properties beyond their established mitogenic functions. Therefore, GRP-R may be an ideal therapeutic target for the treatment of aggressive neuroblastomas. ..
  5. Martel G, Hevi C, Wong A, Zushida K, Uchida S, Shumyatsky G. Murine GRPR and stathmin control in opposite directions both cued fear extinction and neural activities of the amygdala and prefrontal cortex. PLoS ONE. 2012;7:e30942 pubmed publisher
    ..These mutant mice are based on fear memory-related genes, stathmin and gastrin-releasing peptide receptor (GRPR). Remarkably, both mutant lines showed changes in fear extinction to the cue but not to the context...
  6. Kamichi S, Wada E, Aoki S, Sekiguchi M, Kimura I, Wada K. Immunohistochemical localization of gastrin-releasing peptide receptor in the mouse brain. Brain Res. 2005;1032:162-70 pubmed
    ..These anatomical results provide support for the idea that the GRP/GRP-R system mediates memory performance by modulating neurotransmitter release in the local GABAergic network. ..
  7. Sun Y, Chen Z. A gastrin-releasing peptide receptor mediates the itch sensation in the spinal cord. Nature. 2007;448:700-3 pubmed
    ..Here we describe that the gastrin-releasing peptide receptor (GRPR) plays an important part in mediating itch sensation in the dorsal spinal cord...
  8. Xu Y, Lopes C, Wende H, Guo Z, Cheng L, Birchmeier C, et al. Ontogeny of excitatory spinal neurons processing distinct somatic sensory modalities. J Neurosci. 2013;33:14738-48 pubmed publisher
    ..development of a subset of excitatory neurons located in laminae I and II was impaired, including itch-related GRPR-expressing neurons, PKC?-expressing neurons, and neurons expressing three neuropeptide genes: somatostatin, ..
  9. Lagerström M, Rogoz K, Abrahamsen B, Persson E, Reinius B, Nordenankar K, et al. VGLUT2-dependent sensory neurons in the TRPV1 population regulate pain and itch. Neuron. 2010;68:529-42 pubmed publisher
    ..This study establishes that VGLUT2 is a major player in TRPV1 thermal nociception and also serves to regulate a normal itch response. ..

More Information


  1. Liu X, Liu Z, Sun Y, Ross M, Kim S, Tsai F, et al. Unidirectional cross-activation of GRPR by MOR1D uncouples itch and analgesia induced by opioids. Cell. 2011;147:447-58 pubmed publisher
    ..MOR1D heterodimerizes with gastrin-releasing peptide receptor (GRPR) in the spinal cord, relaying itch information...
  2. Sun Y, Zhao Z, Meng X, Yin J, Liu X, Chen Z. Cellular basis of itch sensation. Science. 2009;325:1531-4 pubmed publisher
    ..Although our previous study suggested that gastrin-releasing peptide receptor (GRPR) is an itch-specific gene in the spinal cord, a long-standing question of whether there are separate neuronal ..
  3. Yamada K, Wada E, Wada K. Male mice lacking the gastrin-releasing peptide receptor (GRP-R) display elevated preference for conspecific odors and increased social investigatory behaviors. Brain Res. 2000;870:20-6 pubmed
    ..Rather, these latter behaviors may be a consequence of altered cognition of conspecific odors in the mutant mice. ..
  4. Hampton L, Ladenheim E, Akeson M, Way J, Weber H, Sutliff V, et al. Loss of bombesin-induced feeding suppression in gastrin-releasing peptide receptor-deficient mice. Proc Natl Acad Sci U S A. 1998;95:3188-92 pubmed
    ..These data suggest that selective agonists for the GRP-R may be useful in inducing satiety. ..
  5. Shumyatsky G, Tsvetkov E, Malleret G, Vronskaya S, Hatton M, Hampton L, et al. Identification of a signaling network in lateral nucleus of amygdala important for inhibiting memory specifically related to learned fear. Cell. 2002;111:905-18 pubmed
    ..Moreover, we found that GRP receptor (GRPR) is expressed in GABAergic interneurons of the lateral nucleus...
  6. Ladenheim E, Hampton L, Whitney A, White W, Battey J, Moran T. Disruptions in feeding and body weight control in gastrin-releasing peptide receptor deficient mice. J Endocrinol. 2002;174:273-81 pubmed
    ..These data suggest that the GRP-R mediates the feeding effects of BN-like peptides and participates in the termination of meals in mice. ..
  7. Yu Y, Barry D, Hao Y, Liu X, Chen Z. Molecular and neural basis of contagious itch behavior in mice. Science. 2017;355:1072-1076 pubmed publisher
    ..Ablation of gastrin-releasing peptide receptor (GRPR) or GRPR neurons in the SCN abolished contagious scratching behavior, which was recapitulated by chemogenetic ..
  8. Weber H, Jensen R, Battey J. Molecular organization of the mouse gastrin-releasing peptide receptor gene and its promoter. Gene. 2000;244:137-49 pubmed
  9. Giladi E, Nagalla S, Spindel E. Molecular cloning and characterization of receptors for the mammalian bombesin-like peptides. J Mol Neurosci. 1993;4:41-54 pubmed
    ..The same sequence of normal genes and cDNAs of GRP and NMB receptors, together with the gene characterization, demonstrated that SCLC cell lines do not require a structural change in receptor protein or genomic rearrangement. ..
  10. Sasaki A, Adhikari S, Andoh T, Kuraishi Y. BB2 bombesin receptor-expressing spinal neurons transmit herpes-associated itch by BB2 receptor-independent signaling. Neuroreport. 2013;24:652-6 pubmed publisher
    ..The present results suggest that BB2 receptor-expressing spinal neurons transmit herpes-associated itch by BB2 receptor-independent signaling. ..
  11. Sukhtankar D, Ko M. Physiological function of gastrin-releasing peptide and neuromedin B receptors in regulating itch scratching behavior in the spinal cord of mice. PLoS ONE. 2013;8:e67422 pubmed publisher
    ..Previous studies in rodents suggest that bombesin receptor subtypes i.e. receptors for gastrin-releasing peptide (GRPr) and neuromedin B (NMBr) differentially regulate itch scratching...
  12. Wada E, Watase K, Yamada K, Ogura H, Yamano M, Inomata Y, et al. Generation and characterization of mice lacking gastrin-releasing peptide receptor. Biochem Biophys Res Commun. 1997;239:28-33 pubmed
    ..GRP binds to its high affinity receptor (GRPR) to elicit a wide spectrum of biological effects on behavior, digestion, and metabolism...
  13. Zhao Z, Liu X, Jeffry J, Karunarathne W, Li J, Munanairi A, et al. Descending control of itch transmission by the serotonergic system via 5-HT1A-facilitated GRP-GRPR signaling. Neuron. 2014;84:821-34 pubmed publisher
    ..Coactivation of 5-HT1A and GRP receptors (GRPR) greatly potentiates subthreshold, GRP-induced Ca(2+) transients, and action potential firing of GRPR(+) neurons...
  14. Nakagawa T, Hocart S, Schumann M, Tapia J, Mantey S, Coy D, et al. Identification of key amino acids in the gastrin-releasing peptide receptor (GRPR) responsible for high affinity binding of gastrin-releasing peptide (GRP). Biochem Pharmacol. 2005;69:579-93 pubmed
    The bombesin (Bn) receptor family includes the gastrin-releasing peptide (GRPR) and neuromedin B (NMBR) receptors, Bn receptor subtype 3 (BRS-3) and Bn receptor subtype 4 (BB(4))...
  15. Holstege J, de Graaff W, Hossaini M, Cardona Cano S, Jaarsma D, van den Akker E, et al. Loss of Hoxb8 alters spinal dorsal laminae and sensory responses in mice. Proc Natl Acad Sci U S A. 2008;105:6338-43 pubmed publisher
    ..The data therefore suggest that a lower number of neurons in the upper spinal laminae and neuronal disorganization in the dorsal horn underlie the sensory defects including the excessive grooming of the Hoxb8 mutant. ..
  16. Zhao Z, Huo F, Jeffry J, Hampton L, Demehri S, Kim S, et al. Chronic itch development in sensory neurons requires BRAF signaling pathways. J Clin Invest. 2013;123:4769-80 pubmed
    ..These data uncover RAF/MEK/ERK signaling as a key regulator that confers a subset of nociceptors with pruriceptive properties to initiate and maintain long-lasting itch sensation. ..
  17. Du L, Desbarats M, Cornibert S, Malo D, Ecarot B. Fine genetic mapping of the Hyp mutation on mouse chromosome X. Genomics. 1996;32:177-83 pubmed
    ..One microsatellite marker, DXMit8O, was found to be very tightly linked to Hyp, as it was nonrecombinant with Hyp among all the progeny of both backcrosses corresponding to 1101 meioses. ..
  18. Kusano K, Gainer H, Battey J, Fathi Z, Wada E. Receptor-activated currents in mouse fibroblasts expressing transfected bombesin receptor subtype cDNAs. Am J Physiol. 1993;265:C869-76 pubmed
    ..However, at these concentrations, these four antagonists had little effect on NmB Rt responses, thereby showing a specificity of these antagonists for the GRP receptors...
  19. Yamada K, Wada E, Wada K. Female gastrin-releasing peptide receptor (GRP-R)-deficient mice exhibit altered social preference for male conspecifics: implications for GRP/GRP-R modulation of GABAergic function. Brain Res. 2001;894:281-7 pubmed
  20. Carroll R, Matkowskyj K, Saunthararajah Y, Sekosan M, Battey J, Benya R. Contribution of gastrin-releasing peptide and its receptor to villus development in the murine and human gastrointestinal tract. Mech Dev. 2002;113:121-30 pubmed
    ..To determine if this was the case, we compared and contrasted intestinal development in GRPR-/- mice with their wild type littermates...
  21. Balci F, Papachristos E, Gallistel C, Brunner D, Gibson J, Shumyatsky G. Interval timing in genetically modified mice: a simple paradigm. Genes Brain Behav. 2008;7:373-84 pubmed
    ..We suggest including the analysis of interval timing and temporal memory in tests of genetically modified mice for learning and memory and argue that our paradigm allows this to be done simply and efficiently. ..
  22. Yamada K, Santo Yamada Y, Wada E, Wada K. Role of bombesin (BN)-like peptides/receptors in emotional behavior by comparison of three strains of BN-like peptide receptor knockout mice. Mol Psychiatry. 2002;7:113-7, 6 pubmed
    ..g., risk assessment behavior). Further, we found that the type of emotional behavior to which each of the peptide/receptor pathways contributes can be clearly specified. ..
  23. Boyd Y. Non-mendelian inheritance of X chromosome markers in interspecific backcrosses. Nat Genet. 1996;13:393-4 pubmed
  24. Clarimundo V, Farinon M, Pedó R, Teixeira V, Nör C, Gulko P, et al. Gastrin-releasing peptide and its receptor increase arthritis fibroblast-like synoviocytes invasiveness through activating the PI3K/AKT pathway. Peptides. 2017;95:57-61 pubmed publisher
    ..The present study aimed to examine the role of gastrin-releasing peptide (GRP) and its receptor (GRPR) on invasive behavior of mice fibroblast-like synoviocytes (FLS), as well as to evaluate GRP-induced signaling on ..
  25. Battey J, Way J, Corjay M, Shapira H, Kusano K, Harkins R, et al. Molecular cloning of the bombesin/gastrin-releasing peptide receptor from Swiss 3T3 cells. Proc Natl Acad Sci U S A. 1991;88:395-9 pubmed
    ..Expression of the GRP receptor cDNA in model systems potentially provides a powerful assay for the development of subtype-specific receptor antagonists that may prove to be of therapeutic importance in human small cell lung carcinoma. ..
  26. Buchner G, Orfanelli U, Quaderi N, Bassi M, Andolfi G, Ballabio A, et al. Identification of a new EGF-repeat-containing gene from human Xp22: a candidate for developmental disorders. Genomics. 2000;65:16-23 pubmed
    ..Northern analysis indicates that MAEG is expressed early during development. Taken together, these data render MAEG a candidate for human and murine developmental disorders. ..
  27. Ohki Hamazaki H, Sakai Y, Kamata K, Ogura H, Okuyama S, Watase K, et al. Functional properties of two bombesin-like peptide receptors revealed by the analysis of mice lacking neuromedin B receptor. J Neurosci. 1999;19:948-54 pubmed
    ..In addition, the behavioral phenotypes of GRP-R-deficient mice were not observed in NMB-R-deficient mice. These data show that the functions of NMB-R and GRP-R are distinct, with only partial overlap. ..
  28. Monje F, Kim E, Cabatic M, Lubec G, Herkner K, Pollak D. A role for glucocorticoid-signaling in depression-like behavior of gastrin-releasing peptide receptor knock-out mice. Ann Med. 2011;43:389-402 pubmed publisher
    Abstract Background. The gastrin-releasing peptide receptor (GRPR) is highly expressed in the limbic system, where it importantly regulates emotional functions and in the suprachiasmatic nucleus, where it is central for the photic ..
  29. Li P, Janczewski W, Yackle K, Kam K, Pagliardini S, Krasnow M, et al. The peptidergic control circuit for sighing. Nature. 2016;530:293-297 pubmed publisher
    ..We propose that these overlapping peptidergic pathways comprise the core of a sigh control circuit that integrates physiological and perhaps emotional input to transform normal breaths into sighs. ..
  30. Wan L, Jin H, Liu X, Jeffry J, Barry D, Shen K, et al. Distinct roles of NMB and GRP in itch transmission. Sci Rep. 2017;7:15466 pubmed publisher
    ..Furthermore, both Nmb/Grp and Nmbr/Grpr DKO mice responded normally to a wide array of noxious stimuli...
  31. Spindel E, Giladi E, Brehm P, Goodman R, Segerson T. Cloning and functional characterization of a complementary DNA encoding the murine fibroblast bombesin/gastrin-releasing peptide receptor. Mol Endocrinol. 1990;4:1956-63 pubmed
    ..Data base analysis showed that the BR is most homologous to the tachykinin receptors. Although tyrosine kinase activity has been associated with BR function, no tyrosine kinase homologies occur within the BR sequence. ..
  32. King K, Torday J, Sunday M. Bombesin and [Leu8]phyllolitorin promote fetal mouse lung branching morphogenesis via a receptor-mediated mechanism. Proc Natl Acad Sci U S A. 1995;92:4357-61 pubmed
    ..Furthermore, components of branchpoints may induce pulmonary neuroendocrine cell differentiation as part of a positive feedback loop, which could account in part for the high prevalence of these cells at branchpoints. ..
  33. Reid S, Akhmedov N, Piriev N, Kozak C, Danciger M, Farber D. The mouse X-linked juvenile retinoschisis cDNA: expression in photoreceptors. Gene. 1999;227:257-66 pubmed
    ..Therefore, our data suggest that X-linked juvenile retinoschisis originates from abnormalities in a photoreceptor-derived adhesion protein. ..
  34. Stambolian D, Favor J, Silvers W, Avner P, Chapman V, Zhou E. Mapping of the X-linked cataract (Xcat) mutation, the gene implicated in the Nance Horan syndrome, on the mouse X chromosome. Genomics. 1994;22:377-80 pubmed
  35. Fennelly J, Laval S, Wright E, Plumb M. A polymorphic and hypervariable locus in the pseudoautosomal region of the CBA/H mouse sex chromosomes. Genomics. 1996;33:94-8 pubmed
    ..The absence of DXYH1-related sequences in Mus spretus provides DNA sequence evidence to support the observed failure of X-Y pairing during meiosis and consequent hybrid infertility in C57BL/6 x Mus spretus male F1 offspring. ..
  36. Pereira P, Machado G, Danesi G, Canevese F, Reddy V, Pereira T, et al. GRPR/PI3Kγ: Partners in Central Transmission of Itch. J Neurosci. 2015;35:16272-81 pubmed publisher
    The gastrin-releasing peptide (GRP) and its receptor (GRPR) are important components of itch transmission. Upstream, but not downstream, aspects of GRPR signaling have been investigated extensively...
  37. Shiratori Hayashi M, Koga K, Tozaki Saitoh H, Kohro Y, Toyonaga H, Yamaguchi C, et al. STAT3-dependent reactive astrogliosis in the spinal dorsal horn underlies chronic itch. Nat Med. 2015;21:927-31 pubmed publisher
  38. Ohki Hamazaki H, Wada E, Matsui K, Wada K. Cloning and expression of the neuromedin B receptor and the third subtype of bombesin receptor genes in the mouse. Brain Res. 1997;762:165-72 pubmed
    ..Together with the mouse GRP-R gene cloned previously, cloning of the mouse NMB-R and BRS-3 genes permits comparison of function and structure of the three bombesin receptor subtypes in the mouse. ..
  39. de Conciliis L, Marchitiello A, Wapenaar M, Borsani G, Giglio S, Mariani M, et al. Characterization of Cxorf5 (71-7A), a novel human cDNA mapping to Xp22 and encoding a protein containing coiled-coil alpha-helical domains. Genomics. 1998;51:243-50 pubmed
  40. Carroll R, Matkowskyj K, Tretiakova M, Battey J, Benya R. Gastrin-releasing peptide is a mitogen and a morphogen in murine colon cancer. Cell Growth Differ. 2000;11:385-93 pubmed
    ..Rather, the mitogenic properties of GRP are subordinate to it acting as a morphogen, where it and its receptor are critically involved in regulating colon cancer histological progression by promoting a well-differentiated phenotype. ..
  41. John A, Brylka H, Wiegreffe C, Simon R, Liu P, Jüttner R, et al. Bcl11a is required for neuronal morphogenesis and sensory circuit formation in dorsal spinal cord development. Development. 2012;139:1831-41 pubmed publisher
  42. Zhou E, Favor J, Silvers W, Stambolian D. Exclusion of three candidate genes, Grpr, Cxn33, and Pdha1, for the X-linked cataract gene on the distal region of the mouse chromosome X. Mamm Genome. 1995;6:357-9 pubmed
  43. Karatsoreos I, Romeo R, McEwen B, Silver R. Diurnal regulation of the gastrin-releasing peptide receptor in the mouse circadian clock. Eur J Neurosci. 2006;23:1047-53 pubmed
    ..We focus here on gastrin-releasing peptide- (GRP) and on GRP receptor- (GRPr) expressing cells of the SCN...
  44. Burbelo P, Kozak C, Finegold A, Hall A, Pirone D. Cloning, central nervous system expression and chromosomal mapping of the mouse PAK-1 and PAK-3 genes. Gene. 1999;232:209-15 pubmed
    ..The high level of PAK-1 and PAK-3 kinase expression in the mouse brain and spinal cord suggests a potentially important role for these kinases in the control of the cellular architecture and/or signaling in the central nervous system. ..
  45. Zhao Z, Wan L, Liu X, Huo F, Li H, Barry D, et al. Cross-inhibition of NMBR and GRPR signaling maintains normal histaminergic itch transmission. J Neurosci. 2014;34:12402-14 pubmed publisher
    We previously showed that gastrin-releasing peptide receptor (GRPR) in the spinal cord is important for mediating nonhistaminergic itch...
  46. Montini E, Rugarli E, Van de Vosse E, Andolfi G, Mariani M, Puca A, et al. A novel human serine-threonine phosphatase related to the Drosophila retinal degeneration C (rdgC) gene is selectively expressed in sensory neurons of neural crest origin. Hum Mol Genet. 1997;6:1137-45 pubmed
    ..The selective pattern of expression makes PPEF an important marker for sensory neuron differentiation and suggests a role for serine-threonine phosphatases in mammalian development. ..
  47. Ashour K, Shan L, Lee J, Schlicher W, Wada K, Wada E, et al. Bombesin inhibits alveolarization and promotes pulmonary fibrosis in newborn mice. Am J Respir Crit Care Med. 2006;173:1377-85 pubmed
    ..Compared with wild-type littermates, bombesin-treated GRP receptor (GRPR)-null mice had increased interstitial fibrosis but reduced defects in alveolarization...
  48. Grimsholm O, Guo Y, Ny T, Rantapaa Dahlqvist S, Forsgren S. Are neuropeptides important in arthritis? Studies on the importance of bombesin/GRP and substance P in a murine arthritis model. Ann N Y Acad Sci. 2007;1110:525-38 pubmed
    ..With these findings and previous observations of neuropeptide expression patterns and functions we discuss the possibility that interventions with the effects of BN/GRP, SP, and other neuropeptides might be worthwhile in RA. ..
  49. Czepielewski R, Porto B, Rizzo L, Roesler R, Abujamra A, Pinto L, et al. Gastrin-releasing peptide receptor (GRPR) mediates chemotaxis in neutrophils. Proc Natl Acad Sci U S A. 2012;109:547-52 pubmed publisher
    ..Its receptor, gastrin-releasing peptide receptor (GRPR), is expressed by various cell types, and it is overexpressed in cancer cells...
  50. Persson K, Gingerich R, Nayak S, Wada K, Wada E, Ahren B. Reduced GLP-1 and insulin responses and glucose intolerance after gastric glucose in GRP receptor-deleted mice. Am J Physiol Endocrinol Metab. 2000;279:E956-62 pubmed
  51. Liu X, Wan L, Huo F, Barry D, Li H, Zhao Z, et al. B-type natriuretic peptide is neither itch-specific nor functions upstream of the GRP-GRPR signaling pathway. Mol Pain. 2014;10:4 pubmed publisher
    ..receptor-A (NPRA) expressing neurons, which release gastrin releasing peptide (GRP) to activate GRP receptor (GRPR) expressing neurons to relay itch information from the periphery to the brain (Science 340:968-971, 2013)...
  52. Shan L, Emanuel R, Dewald D, Torday J, Asokanathan N, Wada K, et al. Bombesin-like peptide receptor gene expression, regulation, and function in fetal murine lung. Am J Physiol Lung Cell Mol Physiol. 2004;286:L165-73 pubmed
    ..are mediated by known mammalian bombesin receptors [gastrin-releasing peptide (GRP)/bombesin-preferring receptor (GRPR), neuromedin B (NMB) receptor (NMBR), and the orphan bombesin receptor subtype-3 (BRS-3)], we analyzed the ontogeny ..
  53. Chaperon F, Fendt M, Kelly P, Lingenhoehl K, Mosbacher J, Olpe H, et al. Gastrin-releasing peptide signaling plays a limited and subtle role in amygdala physiology and aversive memory. PLoS ONE. 2012;7:e34963 pubmed publisher
    ..GRP increases inhibition in the LA and mice lacking the GRP receptor (GRPR KO) show more pronounced and persistent fear after single-trial associative learning...
  54. Barry D, Li H, Liu X, Shen K, Liu X, Wu Z, et al. Critical evaluation of the expression of gastrin-releasing peptide in dorsal root ganglia and spinal cord. Mol Pain. 2016;12: pubmed publisher
    ..analysis further shows that substantially more GRPergic fibers form synaptic contacts with gastrin releasing peptide receptor-positive (GRPR(+)) neurons than SPergic fibers...