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Gene Review

S1PR1  -  sphingosine-1-phosphate receptor 1

Homo sapiens

Synonyms: CD363, CHEDG1, D1S3362, ECGF1, EDG-1, ...
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Disease relevance of EDG1


High impact information on EDG1


Chemical compound and disease context of EDG1


Biological context of EDG1


Anatomical context of EDG1

  • Consistent with angiogenesis in general during decidualization, we believe EDG1 and EDG5 to be regulated by the embryo because no microvascular expression for these receptors was observed in oil-induced deciduomas [17].
  • Detailed analysis by in situ hybridization (ISH) and immunohistochemistry (IHC) revealed strong EDG1 expression in cardiomyocytes and in endothelial cells of cardiac vessels [18].
  • Unlike EDG3 and EDG5, which are expressed in the smooth muscle cell layer of the human aorta, no signal corresponding to EDG1 expression could be detected in the aorta [18].
  • This is corroborated with the down-regulation of S1P1 in T cells stimulated with anti-CD3 plus anti-CD28 [19].
  • The agonist-modulated targeting of EDG-1 to caveolae and its dynamic inhibitory interactions with caveolin identify new points for regulation of sphingolipid-dependent signaling in the vascular wall [20].

Associations of EDG1 with chemical compounds


Physical interactions of EDG1

  • Identification of the Hydrophobic Ligand Binding Pocket of the S1P1 Receptor [24].
  • In addition, SPP also has been identified as the ligand for the G-protein-coupled receptors EDG-1, -3, -5, and -6 [25].

Regulatory relationships of EDG1


Other interactions of EDG1


Analytical, diagnostic and therapeutic context of EDG1


  1. The novel sphingosine 1-phosphate receptor AGR16 is coupled via pertussis toxin-sensitive and -insensitive G-proteins to multiple signalling pathways. Gonda, K., Okamoto, H., Takuwa, N., Yatomi, Y., Okazaki, H., Sakurai, T., Kimura, S., Sillard, R., Harii, K., Takuwa, Y. Biochem. J. (1999) [Pubmed]
  2. Activated protein C mediates novel lung endothelial barrier enhancement: role of sphingosine 1-phosphate receptor transactivation. Finigan, J.H., Dudek, S.M., Singleton, P.A., Chiang, E.T., Jacobson, J.R., Camp, S.M., Ye, S.Q., Garcia, J.G. J. Biol. Chem. (2005) [Pubmed]
  3. Sphingosine 1-phosphate receptor expression profile in human gastric cancer cells: differential regulation on the migration and proliferation. Yamashita, H., Kitayama, J., Shida, D., Yamaguchi, H., Mori, K., Osada, M., Aoki, S., Yatomi, Y., Takuwa, Y., Nagawa, H. J. Surg. Res. (2006) [Pubmed]
  4. Sphingosine kinase-1 expression correlates with poor survival of patients with glioblastoma multiforme: roles of sphingosine kinase isoforms in growth of glioblastoma cell lines. Van Brocklyn, J.R., Jackson, C.A., Pearl, D.K., Kotur, M.S., Snyder, P.J., Prior, T.W. J. Neuropathol. Exp. Neurol. (2005) [Pubmed]
  5. EDG1 receptor stimulation leads to cardiac hypertrophy in rat neonatal myocytes. Robert, P., Tsui, P., Laville, M.P., Livi, G.P., Sarau, H.M., Bril, A., Berrebi-Bertrand, I. J. Mol. Cell. Cardiol. (2001) [Pubmed]
  6. Vascular endothelial cell adherens junction assembly and morphogenesis induced by sphingosine-1-phosphate. Lee, M.J., Thangada, S., Claffey, K.P., Ancellin, N., Liu, C.H., Kluk, M., Volpi, M., Sha'afi, R.I., Hla, T. Cell (1999) [Pubmed]
  7. A sphingosine-1-phosphate receptor regulates cell migration during vertebrate heart development. Kupperman, E., An, S., Osborne, N., Waldron, S., Stainier, D.Y. Nature (2000) [Pubmed]
  8. Sphingosine-1-phosphate as a ligand for the G protein-coupled receptor EDG-1. Lee, M.J., Van Brocklyn, J.R., Thangada, S., Liu, C.H., Hand, A.R., Menzeleev, R., Spiegel, S., Hla, T. Science (1998) [Pubmed]
  9. Akt-mediated phosphorylation of the G protein-coupled receptor EDG-1 is required for endothelial cell chemotaxis. Lee, M.J., Thangada, S., Paik, J.H., Sapkota, G.P., Ancellin, N., Chae, S.S., Wu, M., Morales-Ruiz, M., Sessa, W.C., Alessi, D.R., Hla, T. Mol. Cell (2001) [Pubmed]
  10. Lysophosphatidic acid stimulates the G-protein-coupled receptor EDG-1 as a low affinity agonist. Lee, M.J., Thangada, S., Liu, C.H., Thompson, B.D., Hla, T. J. Biol. Chem. (1998) [Pubmed]
  11. VP1 of foot-and-mouth disease virus induces apoptosis via the Akt signaling pathway. Peng, J.M., Liang, S.M., Liang, C.M. J. Biol. Chem. (2004) [Pubmed]
  12. Physiologically based pharmacokinetic modeling of FTY720 (2-amino-2[2-(-4-octylphenyl)ethyl]propane-1,3-diol hydrochloride) in rats after oral and intravenous doses. Meno-Tetang, G.M., Li, H., Mis, S., Pyszczynski, N., Heining, P., Lowe, P., Jusko, W.J. Drug Metab. Dispos. (2006) [Pubmed]
  13. Stimulation of intracellular sphingosine-1-phosphate production by G-protein-coupled sphingosine-1-phosphate receptors. Meyer zu Heringdorf, D., Lass, H., Kuchar, I., Lipinski, M., Alemany, R., Rümenapp, U., Jakobs, K.H. Eur. J. Pharmacol. (2001) [Pubmed]
  14. Dual regulation of EDG1/S1P(1) receptor phosphorylation and internalization by protein kinase C and G-protein-coupled receptor kinase 2. Watterson, K.R., Johnston, E., Chalmers, C., Pronin, A., Cook, S.J., Benovic, J.L., Palmer, T.M. J. Biol. Chem. (2002) [Pubmed]
  15. Sphingosine-1-phosphate signaling via the EDG-1 family of G-protein-coupled receptors. Hla, T., Lee, M.J., Ancellin, N., Thangada, S., Liu, C.H., Kluk, M., Chae, S.S., Wu, M.T. Ann. N. Y. Acad. Sci. (2000) [Pubmed]
  16. High-density lipoprotein stimulates endothelial cell migration and survival through sphingosine 1-phosphate and its receptors. Kimura, T., Sato, K., Malchinkhuu, E., Tomura, H., Tamama, K., Kuwabara, A., Murakami, M., Okajima, F. Arterioscler. Thromb. Vasc. Biol. (2003) [Pubmed]
  17. Sphingosine-1-phosphate receptor expression and signaling correlate with uterine prostaglandin-endoperoxide synthase 2 expression and angiogenesis during early pregnancy. Skaznik-Wikiel, M.E., Kaneko-Tarui, T., Kashiwagi, A., Pru, J.K. Biol. Reprod. (2006) [Pubmed]
  18. Cell type-specific localization of human cardiac S1P receptors. Mazurais, D., Robert, P., Gout, B., Berrebi-Bertrand, I., Laville, M.P., Calmels, T. J. Histochem. Cytochem. (2002) [Pubmed]
  19. Sphingosine 1-phosphate is a novel inhibitor of T-cell proliferation. Jin, Y., Knudsen, E., Wang, L., Bryceson, Y., Damaj, B., Gessani, S., Maghazachi, A.A. Blood (2003) [Pubmed]
  20. Agonist-modulated targeting of the EDG-1 receptor to plasmalemmal caveolae. eNOS activation by sphingosine 1-phosphate and the role of caveolin-1 in sphingolipid signal transduction. Igarashi, J., Michel, T. J. Biol. Chem. (2000) [Pubmed]
  21. EDG3 is a functional receptor specific for sphingosine 1-phosphate and sphingosylphosphorylcholine with signaling characteristics distinct from EDG1 and AGR16. Okamoto, H., Takuwa, N., Yatomi, Y., Gonda, K., Shigematsu, H., Takuwa, Y. Biochem. Biophys. Res. Commun. (1999) [Pubmed]
  22. Sphingosine-1-phosphate inhibits motility of human breast cancer cells independently of cell surface receptors. Wang, F., Van Brocklyn, J.R., Edsall, L., Nava, V.E., Spiegel, S. Cancer Res. (1999) [Pubmed]
  23. The sphingosine 1-phosphate receptor agonist FTY720 supports CXCR4-dependent migration and bone marrow homing of human CD34+ progenitor cells. Kimura, T., Boehmler, A.M., Seitz, G., Kuçi, S., Wiesner, T., Brinkmann, V., Kanz, L., Möhle, R. Blood (2004) [Pubmed]
  24. Identification of the Hydrophobic Ligand Binding Pocket of the S1P1 Receptor. Fujiwara, Y., Osborne, D.A., Walker, M.D., Wang, D.A., Bautista, D.A., Liliom, K., Van Brocklyn, J.R., Parrill, A.L., Tigyi, G. J. Biol. Chem. (2007) [Pubmed]
  25. Sphingosine 1-phosphate: a ligand for the EDG-1 family of G-protein-coupled receptors. Spiegel, S. Ann. N. Y. Acad. Sci. (2000) [Pubmed]
  26. Analysis of gene expression profiles in pancreatic carcinoma by using cDNA microarray. Yu, X.J., Long, J., Fu, D.L., Zhang, Q.H., Ni, Q.X. HBPD INT (2003) [Pubmed]
  27. Regulation of sphingosine 1-phosphate-induced endothelial cytoskeletal rearrangement and barrier enhancement by S1P1 receptor, PI3 kinase, Tiam1/Rac1, and alpha-actinin. Singleton, P.A., Dudek, S.M., Chiang, E.T., Garcia, J.G. FASEB J. (2005) [Pubmed]
  28. Identification of the angiogenic endothelial-cell growth factor-1/thymidine phosphorylase as a potential target for immunotherapy of cancer. Slager, E.H., Honders, M.W., van der Meijden, E.D., van Luxemburg-Heijs, S.A., Kloosterboer, F.M., Kester, M.G., Jedema, I., Marijt, W.A., Schaafsma, M.R., Willemze, R., Falkenburg, J.H. Blood (2006) [Pubmed]
  29. Sphingosine 1-phosphate/sphingosine 1-phosphate receptor 1 signaling in rheumatoid synovium: regulation of synovial proliferation and inflammatory gene expression. Kitano, M., Hla, T., Sekiguchi, M., Kawahito, Y., Yoshimura, R., Miyazawa, K., Iwasaki, T., Sano, H. Arthritis Rheum. (2006) [Pubmed]
  30. A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Pan, S., Mi, Y., Pally, C., Beerli, C., Chen, A., Guerini, D., Hinterding, K., Nuesslein-Hildesheim, B., Tuntland, T., Lefebvre, S., Liu, Y., Gao, W., Chu, A., Brinkmann, V., Bruns, C., Streiff, M., Cannet, C., Cooke, N., Gray, N. Chem. Biol. (2006) [Pubmed]
  31. Recovery and expression of messenger RNA from postmortem human brain tissue. Cummings, T.J., Strum, J.C., Yoon, L.W., Szymanski, M.H., Hulette, C.M. Mod. Pathol. (2001) [Pubmed]
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