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Gene Review

Gpr1  -  G protein-coupled receptor 1

Mus musculus

Synonyms: G-protein coupled receptor 1
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Disease relevance of Gpr1

  • We have recently engineered an in vivo endothelial cell-specific retroviral gene transfer system and found that a single Kaposi's sarcoma (KS)-associated herpesvirus/human herpesvirus 8 gene encoding a G protein-coupled receptor (vGPCR), is sufficient to induce KS-like tumors in mice [1].
  • Akt plays a central role in sarcomagenesis induced by Kaposi's sarcoma herpesvirus-encoded G protein-coupled receptor [1].
  • Broad-spectrum G protein-coupled receptor antagonist, [D-Arg1,D-Trp5,7,9,Leu11]SP: a dual inhibitor of growth and angiogenesis in pancreatic cancer [2].
  • Here we show that the KSHV GPCR enhances the expression of VEGF by stimulating the activity of the transcription factor hypoxia-inducible factor (HIF)-1alpha, which activates transcription from a hypoxia response element within the 5'-flanking region of the VEGF promoter [3].
  • G Protein-coupled Receptor (GPCR) Kinase 2 Regulates Agonist-independent Gq/11 Signaling from the Mouse Cytomegalovirus GPCR M33 [4].

High impact information on Gpr1


Chemical compound and disease context of Gpr1

  • Lysophosphatidic acid (LPA) is a lipid-derived G-protein-coupled receptor (GPCR) agonist that is involved in a variety of physiological and pathological processes, including cell survival, proliferation and differentiation, cytoskeletal rearrangement, cell-cell interactions, tumorigenesis and cell invasion [10].
  • Involvement of metabotropic glutamate receptor 1, a G protein coupled receptor, in melanoma development [11].

Biological context of Gpr1

  • Open reading frame 74 encodes KSHV G protein-coupled receptor (GPCR), a constitutively active chemokine receptor that directly transforms NIH 3T3 cells in vitro and induces multifocal KS-like lesions in KSHV-GPCR-transgenic mice [12].
  • We have reported the cloning from mouse genomic DNA of a fragment encoding a G-protein-coupled receptor related to the receptor for the blood clotting enzyme thrombin [13].
  • Protein folding as posttranslational regulation: evolution of a mechanism for controlled plasma membrane expression of a g protein-coupled receptor [14].
  • DNA sequence analysis of RRV indicates that it shares numerous open reading frames (ORFs) with HHV-8, including one (ORF74) encoding a seven-transmembrane-spanning G protein-coupled receptor (GPCR) with similarity to cellular chemokine receptors [15].
  • CONCLUSION: These results deny the coexistence of an additional AT(2) subtype in rabbit proximal tubule cells and demonstrate for the first time the presence of functional diversity for closely related Eutherian orthologues of a G protein-coupled receptor (GPCR) that are more than 90% homologous in the amino acid sequence [16].

Anatomical context of Gpr1

  • Our data reveal Edg-1 to be the first G protein-coupled receptor required for blood vessel formation and show that sphingolipid signaling is essential during mammalian development [6].
  • G2A is an orphan G protein-coupled receptor (GPCR), expressed predominantly in T and B cells and homologous to a small group of GPCRs of unknown function expressed in lymphoid tissues [17].
  • RDC1 is an orphan G protein-coupled receptor, whereas Neuritin is a growth-promoting protein known to mediate neurite outgrowth [18].
  • In this study, we have identified the G protein-coupled receptor (GPR)83 to be selectively up-regulated by CD4+CD25+ Treg cells of both murine and human origin in contrast to naive CD4+CD25- or recently activated T cells [19].
  • Specialized membrane microdomains known as lipid rafts are thought to contribute to G-protein coupled receptor (GPCR) signaling by organizing receptors and their cognate signaling molecules into discrete membrane domains [20].

Associations of Gpr1 with chemical compounds

  • Substance P analogues, including [D-Arg(1),D-Trp(5,7,9),Leu(11)]SP (SPA) are broad-spectrum G protein-coupled receptor (GPCR) antagonists that have potential antitumorigenic activities, although the mechanism(s) are not completely understood [2].
  • Stimulation of RBL-2H3 m1 mast cells through the IgE receptor with antigen, or through a G protein-coupled receptor with carbachol, leads to the rapid appearance of phosphothreonine in nonmuscle myosin heavy chain II-A (NMHC-IIA) [21].
  • GPCR-dependent ROS formation is absent in lipopolysaccharide (LPS)-primed P-Rex1(-/-) neutrophils, but less affected in unprimed or TNFalpha-primed cells [22].
  • Protein kinase D (PKD)/protein kinase C (PKC) mu is a serine/threonine protein kinase that can be activated by physiological stimuli like growth factors, antigen-receptor engagement and G protein-coupled receptor (GPCR) agonists via a phosphorylation-dependent mechanism that requires PKC activity [23].
  • Estrogen may bind membrane proteins comparable to classical nuclear estrogen receptors (ERs), but some studies identify nonclassical receptors, such as G protein-coupled receptor (GPR)30 [24].

Other interactions of Gpr1


Analytical, diagnostic and therapeutic context of Gpr1

  • In order to better understand signalling adaptations at the molecular level, we used high-density oligonucleotide microarrays (Codelink Mouse 20K) to define alterations in the expression of transcripts encoding regulator of G-protein coupled receptor signalling in dopamine D1 receptor knockout mice (Drd1a-KO) [26].
  • We have used reverse transcription-polymerase chain reaction (PCR) to isolate a cDNA from human brain mRNA, GPCR/CNS, that encodes a putative G protein-coupled receptor (GPCR) based upon the presence of the paradigmatic seven heptahelical transmembrane domains in its predicted amino acid sequence [27].
  • Interestingly, these two G-protein-coupled receptor systems are targeted by modern heart failure treatment including beta-adrenergic blockers, angiotensin-converting enzyme inhibitors, and angiotensin receptor blockers [28].
  • Mass spectrometry and immunoblotting were used to identify this antigen as the avian ortholog of the very large G-protein-coupled receptor VLGR1, the product of the Usher syndrome USH2C (Mass1) locus [29].


  1. Akt plays a central role in sarcomagenesis induced by Kaposi's sarcoma herpesvirus-encoded G protein-coupled receptor. Sodhi, A., Montaner, S., Patel, V., Gómez-Román, J.J., Li, Y., Sausville, E.A., Sawai, E.T., Gutkind, J.S. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  2. Broad-spectrum G protein-coupled receptor antagonist, [D-Arg1,D-Trp5,7,9,Leu11]SP: a dual inhibitor of growth and angiogenesis in pancreatic cancer. Guha, S., Eibl, G., Kisfalvi, K., Fan, R.S., Burdick, M., Reber, H., Hines, O.J., Strieter, R., Rozengurt, E. Cancer Res. (2005) [Pubmed]
  3. The Kaposi's sarcoma-associated herpes virus G protein-coupled receptor up-regulates vascular endothelial growth factor expression and secretion through mitogen-activated protein kinase and p38 pathways acting on hypoxia-inducible factor 1alpha. Sodhi, A., Montaner, S., Patel, V., Zohar, M., Bais, C., Mesri, E.A., Gutkind, J.S. Cancer Res. (2000) [Pubmed]
  4. G Protein-coupled Receptor (GPCR) Kinase 2 Regulates Agonist-independent Gq/11 Signaling from the Mouse Cytomegalovirus GPCR M33. Sherrill, J.D., Miller, W.E. J. Biol. Chem. (2006) [Pubmed]
  5. Neutrophil direction sensing and superoxide production linked by the GTPase-activating protein GIT2. Mazaki, Y., Hashimoto, S., Tsujimura, T., Morishige, M., Hashimoto, A., Aritake, K., Yamada, A., Nam, J.M., Kiyonari, H., Nakao, K., Sabe, H. Nat. Immunol. (2006) [Pubmed]
  6. Edg-1, the G protein-coupled receptor for sphingosine-1-phosphate, is essential for vascular maturation. Liu, Y., Wada, R., Yamashita, T., Mi, Y., Deng, C.X., Hobson, J.P., Rosenfeldt, H.M., Nava, V.E., Chae, S.S., Lee, M.J., Liu, C.H., Hla, T., Spiegel, S., Proia, R.L. J. Clin. Invest. (2000) [Pubmed]
  7. A novel angiotensin II type 2 receptor signaling pathway: possible role in cardiac hypertrophy. Senbonmatsu, T., Saito, T., Landon, E.J., Watanabe, O., Price, E., Roberts, R.L., Imboden, H., Fitzgerald, T.G., Gaffney, F.A., Inagami, T. EMBO J. (2003) [Pubmed]
  8. CARMA3/Bcl10/MALT1-dependent NF-{kappa}B activation mediates angiotensin II-responsive inflammatory signaling in nonimmune cells. McAllister-Lucas, L.M., Ruland, J., Siu, K., Jin, X., Gu, S., Kim, D.S., Kuffa, P., Kohrt, D., Mak, T.W., Nu??ez, G., Lucas, P.C. Proc. Natl. Acad. Sci. U.S.A. (2007) [Pubmed]
  9. Kelch-repeat proteins interacting with the Galpha protein Gpa2 bypass adenylate cyclase for direct regulation of protein kinase A in yeast. Peeters, T., Louwet, W., Geladé, R., Nauwelaers, D., Thevelein, J.M., Versele, M. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
  10. Roles of LPA3 and COX-2 in implantation. Shah, B.H., Catt, K.J. Trends Endocrinol. Metab. (2005) [Pubmed]
  11. Involvement of metabotropic glutamate receptor 1, a G protein coupled receptor, in melanoma development. Marín, Y.E., Chen, S. J. Mol. Med. (2004) [Pubmed]
  12. Kaposi's sarcoma-associated herpesvirus G protein-coupled receptor constitutively activates NF-kappa B and induces proinflammatory cytokine and chemokine production via a C-terminal signaling determinant. Schwarz, M., Murphy, P.M. J. Immunol. (2001) [Pubmed]
  13. The mouse proteinase-activated receptor-2 cDNA and gene. Molecular cloning and functional expression. Nystedt, S., Larsson, A.K., Aberg, H., Sundelin, J. J. Biol. Chem. (1995) [Pubmed]
  14. Protein folding as posttranslational regulation: evolution of a mechanism for controlled plasma membrane expression of a g protein-coupled receptor. Conn, P.M., Knollman, P.E., Brothers, S.P., Janovick, J.A. Mol. Endocrinol. (2006) [Pubmed]
  15. A G protein-coupled receptor encoded by rhesus rhadinovirus is similar to ORF74 of Kaposi's sarcoma-associated herpesvirus. Estep, R.D., Axthelm, M.K., Wong, S.W. J. Virol. (2003) [Pubmed]
  16. Functional diversity of AT2 receptor orthologues in closely related species. Feng, Y.H., Zhou, L., Sun, Y., Douglas, J.G. Kidney Int. (2005) [Pubmed]
  17. Direct genetic demonstration of G alpha 13 coupling to the orphan G protein-coupled receptor G2A leading to RhoA-dependent actin rearrangement. Kabarowski, J.H., Feramisco, J.D., Le, L.Q., Gu, J.L., Luoh, S.W., Simon, M.I., Witte, O.N. Proc. Natl. Acad. Sci. U.S.A. (2000) [Pubmed]
  18. Novel cellular genes essential for transformation of endothelial cells by Kaposi's sarcoma-associated herpesvirus. Raggo, C., Ruhl, R., McAllister, S., Koon, H., Dezube, B.J., Früh, K., Moses, A.V. Cancer Res. (2005) [Pubmed]
  19. G protein-coupled receptor 83 overexpression in naive CD4+CD25- T cells leads to the induction of Foxp3+ regulatory T cells in vivo. Hansen, W., Loser, K., Westendorf, A.M., Bruder, D., Pfoertner, S., Siewert, C., Huehn, J., Beissert, S., Buer, J. J. Immunol. (2006) [Pubmed]
  20. Constitutive localization of the gonadotropin-releasing hormone (GnRH) receptor to low density membrane microdomains is necessary for GnRH signaling to ERK. Navratil, A.M., Bliss, S.P., Berghorn, K.A., Haughian, J.M., Farmerie, T.A., Graham, J.K., Clay, C.M., Roberson, M.S. J. Biol. Chem. (2003) [Pubmed]
  21. Calcium-dependent threonine phosphorylation of nonmuscle myosin in stimulated RBL-2H3 mast cells. Buxton, D.B., Adelstein, R.S. J. Biol. Chem. (2000) [Pubmed]
  22. P-Rex1 regulates neutrophil function. Welch, H.C., Condliffe, A.M., Milne, L.J., Ferguson, G.J., Hill, K., Webb, L.M., Okkenhaug, K., Coadwell, W.J., Andrews, S.R., Thelen, M., Jones, G.E., Hawkins, P.T., Stephens, L.R. Curr. Biol. (2005) [Pubmed]
  23. Rapid protein kinase D translocation in response to G protein-coupled receptor activation. Dependence on protein kinase C. Rey, O., Young, S.H., Cantrell, D., Rozengurt, E. J. Biol. Chem. (2001) [Pubmed]
  24. Nature of functional estrogen receptors at the plasma membrane. Pedram, A., Razandi, M., Levin, E.R. Mol. Endocrinol. (2006) [Pubmed]
  25. Loss of the transmembrane and cytoplasmic domains of the very large G-protein-coupled receptor-1 (VLGR1 or Mass1) causes audiogenic seizures in mice. McMillan, D.R., White, P.C. Mol. Cell. Neurosci. (2004) [Pubmed]
  26. Genetic or pharmacological inactivation of the dopamine D1 receptor differentially alters the expression of regulator of G-protein signalling (Rgs) transcripts. Stanwood, G.D., Parlaman, J.P., Levitt, P. Eur. J. Neurosci. (2006) [Pubmed]
  27. A human gene encodes a putative G protein-coupled receptor highly expressed in the central nervous system. Donohue, P.J., Shapira, H., Mantey, S.A., Hampton, L.L., Jensen, R.T., Battey, J.F. Brain Res. Mol. Brain Res. (1998) [Pubmed]
  28. Role of G-protein-coupled receptor kinase 2 in the heart--do regulatory mechanisms open novel therapeutic perspectives? Hansen, J.L., Theilade, J., Aplin, M., Sheikh, S.P. Trends Cardiovasc. Med. (2006) [Pubmed]
  29. The very large G-protein-coupled receptor VLGR1: a component of the ankle link complex required for the normal development of auditory hair bundles. McGee, J., Goodyear, R.J., McMillan, D.R., Stauffer, E.A., Holt, J.R., Locke, K.G., Birch, D.G., Legan, P.K., White, P.C., Walsh, E.J., Richardson, G.P. J. Neurosci. (2006) [Pubmed]
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