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Gene Review

S1PR3  -  sphingosine-1-phosphate receptor 3

Homo sapiens

Synonyms: EDG-3, EDG3, Endothelial differentiation G-protein coupled receptor 3, LPB3, S1P receptor 3, ...
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Disease relevance of EDG3


High impact information on EDG3


Chemical compound and disease context of EDG3

  • The inhibitory effects of HDL, SPC, and LSF on TNF-alpha-induced E-selectin expression were partially reverted in the presence of suramin, an antagonist of lysosphingolipid receptor EDG-3, or pertussis toxin, an inhibitor of trimeric G proteins [9].
  • High-density lipoproteins and their constituent, sphingosine-1-phosphate, directly protect the heart against ischemia/reperfusion injury in vivo via the S1P3 lysophospholipid receptor [10].

Biological context of EDG3


Anatomical context of EDG3


Associations of EDG3 with chemical compounds

  • Overexpression of EDG3 conferred a specific [32P]S1P binding, which was displaced by S1P and sphingosylphosphorylcholine (SPC), but not by LPA or other related lipids [18].
  • Additionally, EDG3 mediated a decrease in cellular cyclic AMP content, like EDG1, but contrasting with AGR16 which mediated an increase in cyclic AMP [18].
  • Furthermore, because only EDG-3 was antagonized by suramin, variations in receptor structure may determine differences in antagonist selectivity [11].
  • Moreover, an antisense ODN designed to inhibit Edg5 expression also decreased the SPP-induced rise in Ca(2+), although to a lesser extent than that observed by inhibiting Edg3 [17].
  • Vascular sphingosine-1-phosphate S1P1 and S1P3 receptors [19].

Other interactions of EDG3


Analytical, diagnostic and therapeutic context of EDG3


  1. Sphingosine-1-phosphate stimulates human glioma cell proliferation through Gi-coupled receptors: role of ERK MAP kinase and phosphatidylinositol 3-kinase beta. Van Brocklyn, J., Letterle, C., Snyder, P., Prior, T. Cancer Lett. (2002) [Pubmed]
  2. Sphingosine 1-phosphate-induced cell proliferation, survival, and related signaling events mediated by G protein-coupled receptors Edg3 and Edg5. An, S., Zheng, Y., Bleu, T. J. Biol. Chem. (2000) [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. Biochemical regulation of breast cancer cell expression of S1P2 (Edg-5) and S1P3 (Edg-3) G protein-coupled receptors for sphingosine 1-phosphate. Dolezalova, H., Shankar, G., Huang, M.C., Bikle, D.D., Goetzl, E.J. J. Cell. Biochem. (2003) [Pubmed]
  5. 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]
  6. Estrogen transactivates EGFR via the sphingosine 1-phosphate receptor Edg-3: the role of sphingosine kinase-1. Sukocheva, O., Wadham, C., Holmes, A., Albanese, N., Verrier, E., Feng, F., Bernal, A., Derian, C.K., Ullrich, A., Vadas, M.A., Xia, P. J. Cell Biol. (2006) [Pubmed]
  7. Inhibitory regulation of Rac activation, membrane ruffling, and cell migration by the G protein-coupled sphingosine-1-phosphate receptor EDG5 but not EDG1 or EDG3. Okamoto, H., Takuwa, N., Yokomizo, T., Sugimoto, N., Sakurada, S., Shigematsu, H., Takuwa, Y. Mol. Cell. Biol. (2000) [Pubmed]
  8. Immunomodulator FTY720 Induces Myofibroblast Differentiation via the Lysophospholipid Receptor S1P3 and Smad3 Signaling. Keller, C.D., Rivera Gil, P., T??lle, M., van der Giet, M., Chun, J., Radeke, H.H., Sch??fer-Korting, M., Kleuser, B. Am. J. Pathol. (2007) [Pubmed]
  9. High density lipoprotein-associated lysosphingolipids reduce E-selectin expression in human endothelial cells. Nofer, J.R., Geigenmüller, S., Göpfert, C., Assmann, G., Buddecke, E., Schmidt, A. Biochem. Biophys. Res. Commun. (2003) [Pubmed]
  10. High-density lipoproteins and their constituent, sphingosine-1-phosphate, directly protect the heart against ischemia/reperfusion injury in vivo via the S1P3 lysophospholipid receptor. Theilmeier, G., Schmidt, C., Herrmann, J., Keul, P., Sch??fers, M., Herrgott, I., Mersmann, J., Larmann, J., Hermann, S., Stypmann, J., Schober, O., Hildebrand, R., Schulz, R., Heusch, G., Haude, M., von Wnuck Lipinski, K., Herzog, C., Schmitz, M., Erbel, R., Chun, J., Levkau, B. Circulation (2006) [Pubmed]
  11. Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5. Ancellin, N., Hla, T. J. Biol. Chem. (1999) [Pubmed]
  12. Molecular cloning of the novel human G protein-coupled receptor (GPCR) gene mapped on chromosome 9. Yamaguchi, F., Tokuda, M., Hatase, O., Brenner, S. Biochem. Biophys. Res. Commun. (1996) [Pubmed]
  13. 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]
  14. 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]
  15. 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]
  16. Sphingosine 1-phosphate stimulates cell migration through a G(i)-coupled cell surface receptor. Potential involvement in angiogenesis. Wang, F., Van Brocklyn, J.R., Hobson, J.P., Movafagh, S., Zukowska-Grojec, Z., Milstien, S., Spiegel, S. J. Biol. Chem. (1999) [Pubmed]
  17. Sphingosine 1-phosphate evokes calcium signals in C2C12 myoblasts via Edg3 and Edg5 receptors. Meacci, E., Cencetti, F., Formigli, L., Squecco, R., Donati, C., Tiribilli, B., Quercioli, F., Zecchi Orlandini, S., Francini, F., Bruni, P. Biochem. J. (2002) [Pubmed]
  18. 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]
  19. Vascular sphingosine-1-phosphate S1P1 and S1P3 receptors. Waeber, C., Blondeau, N., Salomone, S. Drug News Perspect. (2004) [Pubmed]
  20. Molecular cloning of EDG-3 and N-Shc genes from the puffer fish, Fugu rubripes, and conservation of synteny with the human genome. Yamaguchi, F., Yamaguchi, K., Tokuda, M., Brenner, S. FEBS Lett. (1999) [Pubmed]
  21. S1P3 receptors mediate the potent constriction of cerebral arteries by sphingosine-1-phosphate. Salomone, S., Yoshimura, S., Reuter, U., Foley, M., Thomas, S.S., Moskowitz, M.A., Waeber, C. Eur. J. Pharmacol. (2003) [Pubmed]
  22. High-density lipoprotein stimulates myocardial perfusion in vivo. Levkau, B., Hermann, S., Theilmeier, G., van der Giet, M., Chun, J., Schober, O., Schäfers, M. Circulation (2004) [Pubmed]
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