Novel GPCR Screening Approach: Indirect Identification of S1P Receptor Agonists in Antagonist Screening Using a Calcium Assay

REFERENCES

• An S, Bleu T, Huang W, Hallmark O G, Coughlin S R, Goetzl E J. Identification of cDNAs encoding two G protein-coupled receptors for lysosphingolipids. FEBS Lett 1997; 417: 279–282
   PubMed Web of Science ®Google Scholar
• An S, Zheng Y, Bleu T. Sphingosine 1-phosphate-induced cell proliferation, survival, and related signaling events mediated by G protein-coupled receptors Edg3 and Edg5. J Biol Chem 2000; 275: 288–296
   PubMed Web of Science ®Google Scholar
• Chun J, Goetzl E, Hla T, Igarashi Y, Lynch K, Moolenaar W, Pyne S, Tigyi G. International Union of Pharmacology. XXXIV. Lysophospholipid receptor nomenclature. Pharmacol Rev 2002; 54: 265–269
   PubMed Web of Science ®Google Scholar
• Lee M-J, Van Brocklyn J R, Thangada S, Liu C H, Hand A R, Menzeleev R, Spiegel S, Hla T. Sphingosine 1-phosphate as a ligand for the G protein-coupled receptor Edg-1. Science 1998; 279: 1552–1555
   PubMed Web of Science ®Google Scholar
• Lynch K R, Im D S. Life on the edg. Trends Pharmacol Sci 1999; 20: 473–475
   PubMed Web of Science ®Google Scholar
• MacLennan A J, Browe C S, Gaskin A A, Lado D C, Shaw G. Cloning and characterization of a putative G-protein coupled receptor potentially involved in development. Mol Cell Neurosci 1994; 5: 201–209
   PubMed Web of Science ®Google Scholar
• Okazaki H, Ishizaka N, Sakurai T, Kurokawa K, Goto K, Kumada M, Takuwa Y. Molecular cloning of a novel putative G protein-coupled receptor expressed in the cardiovascular system. Biochem Biophys Res Commun 1993; 190: 1104–1109
   PubMed Web of Science ®Google Scholar
• Yamaguchi F, Tokuda M, Hatase O, Brenner S. Molecular cloning of the novel human G protein-coupled receptor (GPCR) gene mapped on chromosome 9. Biochem Biophys Res Commun 1996; 227: 608–614
   PubMed Web of Science ®Google Scholar
• Zhang G, Contos J J, Weiner J A, Fukushima N, Chun J. Comparative analysis of three murine G-protein coupled receptors activated by sphingosine-1-phosphate. Gene 1999; 227: 89–99
   PubMed Web of Science ®Google Scholar
• Lee M-J, Thangada S, Liu C H, Thompson B D, Hla T. Lysophosphatidic acid stimulates the G protein-coupled receptor Edg-1 as a low affinity agonist. J Biol Chem 1998; 273: 22105–22112
   PubMed Web of Science ®Google Scholar
• Parrill A L, Wang D-A, Bautista D L, Van Brocklyn J R, Lorincz Z, Fischer D J, Baker D L, Liliom K, Spiegel S, Tigyi G. Identification of Edg1 receptor residues that recognize sphingosine 1-phosphate. J Biol Chem 2000; 275: 39379–39384
   PubMed Web of Science ®Google Scholar
• Kon J, Sato K, Watanabe T, Tomura H, Kuwabara A, Kimura T, Tamama K, Ishizuka T, Murata N, Kanda T, Kobayashi I, Ohta H, Ui M, Okajima F. Comparison of intrinsic activities of the putative sphingosine 1-phosphate receptor subtypes to regulate several signaling pathways in their cDNA-transfected Chinese hamster ovary cells. J Biol Chem 1999; 274: 23940–23947
   PubMed Web of Science ®Google Scholar
• Van Brocklyn J R, Tu Z, Edsall L C, Schmidt R R, Spiegel S. Sphingosine 1-phosphate-induced cell rounding and neurite retraction are mediated by the G protein-coupled receptor H218. J Biol Chem 1999; 274: 4626–4632
   PubMed Web of Science ®Google Scholar
• Windh R T, Lee M-J, Hla T, An S, Barr A J, Manning D R. Differential coupling of the sphingosine 1-phosphate receptors Edg-1, Edg-3, and H218/Edg-5 to the Gi, Gq, and G12 families of heterotrimeric G proteins. J Biol Chem 1999; 274: 27351–27358
   PubMed Web of Science ®Google Scholar
• Okamoto H, Takuwa N, Gonda K, Okazaki H, Chang K, Yatomi Y, Shigematsu H, Takuwa Y. Edg-1 is a functional sphingosine 1-phosphate receptor that is linked via a Gi/o to multiple signaling pathways, including phospholipase C activation, Ca2 + mobilization, Ras-mitogen-activated protein kinase activation, and adenylate cyclase inhibition. J Biol Chem 1998; 273: 27104–27110
   PubMed Web of Science ®Google Scholar
• Okamoto H, Takuwa N, Yatomi Y, Gonda K, Shigematsu H, Takuwa Y. Edg-3 is a functional receptor specific for sphingosine 1-phosphate and sphingosylphosphorylcholine with signaling characteristics distinct from Edg-1 and AGR16. Biochem Biophys Res Commun 1999; 260: 203–208
   PubMed Web of Science ®Google Scholar
• Siehler S, Manning D R. Pathways of transduction engaged by sphingosine 1-phosphate through G protein-coupled receptors. Biochim Biophys Acta 2002; 1582: 94–99
   PubMed Web of Science ®Google Scholar
• An S, Bleu T, Zheng Y. Transduction of intracellular calcium signals through G protein-mediated activation of phospholipase C by recombinant sphingosine 1-phosphate receptors. Mol Pharmacol 1999; 55: 787–794
   PubMed Web of Science ®Google Scholar
• Ancellin N, Hla T. Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5. J Biol Chem 1999; 274: 18997–19002
   PubMed Web of Science ®Google Scholar
• Gonda K, Okamoto H, Takuwa N, Yatomi Y, Okazaki H, Sakurai T, Kimura S, Sillard R, Harii K, Takuwa Y. The novel sphingosine 1-phosphate receptor AGR16 is coupled via pertussis toxin-sensitive and-insensitive G-proteins to multiple signalling pathways. Biochem J 1999; 337: 67–75
   PubMed Web of Science ®Google Scholar
• Siehler S, Wang Y, Fan X, Windh R T, Manning D R. Sphingosine 1-phosphate activates nuclear factor-kappa B through Edg receptors. Activation through Edg-3 and Edg-5, but not Edg-1, in human embryonic kidney 293 cells. J Biol Chem 2001; 276: 48733–48739
   PubMed Web of Science ®Google Scholar
• Okamoto H, Takuwa N, Yokomizo T, Sugimoto N, Sakurada S, Shigematsu H, Takuwa Y. 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. Mol Cell Biol 2000; 20: 9247–9261
   PubMed Web of Science ®Google Scholar
• Paik J H, Chae S S, Lee M J, Thangada S, Hla T. Sphingosine 1-phosphate-induced endothelial cell migration requires the expression of EDG-1 and EDG-3 receptors and Rho-dependent activation of alpha beta3-and beta1-containing integrins. J Biol Chem 2001; 276: 11830–11837
   PubMedGoogle Scholar
• Lee O H, Kim Y M, Lee Y M, Moon E J, Lee D J, Kim J H, Kim K W, Kwon Y G. Sphingosine 1-phosphate induces angiogenesis: Its angiogenic action and signaling mechanism in human umbilical vein endothelial cells. Biochem Biophys Res Commun 1999; 264: 743–750
   PubMed Web of Science ®Google Scholar
• Ishii I, Friedman B, Ye X, Kawamura S, McGiffert C, Contos J J, Kingsbury M A, Zhang G, Brown J H, Chun J. Selective loss of sphingosine 1-phosphate signaling with no obvious phenotypic abnormality in mice lacking its G protein-coupled receptor, LP(B3)/EDG-3. J Biol Chem 2001; 276: 33697–33704
   PubMed Web of Science ®Google Scholar
• Ishii I, Ye X, Friedman B, Kawamura S, Contos J J, Kingsbury M A, Yang A H, Zhang G, Brown J H, Chun J. Marked perinatal lethality and cellular signaling deficits in mice null for the two sphingosine 1-phosphate (S1P) receptors, S1P(2)/LP(B2)/EDG-5 and S1P(3)/LP(B3)/EDG-3. J Biol Chem 2002; 277: 25152–25159
   PubMed Web of Science ®Google Scholar
• Salomone S, Yoshimura S, Reuter U, Foley M, Thomas S S, Moskowitz M A, Waeber C. S1P3 receptors mediate the potent constriction of cerebral arteries by sphingosine-1-phosphate. Eur J Pharmacol 2003; 469: 125–134
   PubMed Web of Science ®Google Scholar
• Zhou H, Murthy K S. Distinctive G protein-dependent signaling in smooth muscle by sphingosine 1-phosphate receptors S1P1 and S1P2. Am J Cell Physiol 2004; 286: C1130–C1138
   PubMed Web of Science ®Google Scholar
• Koide Y, Hasegawa T, Takahashi A, Endo A, Mochizuki N, Nakagawa M, Nishida A. Development of EDG3 Antagonists using a 3D database search and their structure-activity relationships. J Med Chem 2002; 45: 4629–4638
   PubMed Web of Science ®Google Scholar
• Ohmori T, Yatomi Y, Osada M, Kazama F, Takafuta T, Ikeda H, Ozaki Y. Sphingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2. Cardiovasc Res 2003; 58: 170–177
   PubMed Web of Science ®Google Scholar
• MacLennan A J, Carney P R, Zhu W J, Chaves A H, Garcia J, Grimes J R, Anderson K J, Roper S N, Lee N. An essential role for the H218/AGR16/Edg-5/LP(B2) sphingosine 1-phosphate receptor in neuronal excitability. Eur J Neurosci 2001; 14: 203–209
   PubMed Web of Science ®Google Scholar
• Gon Y, Wood M R, Kiosses W B, Jo E, Sanna M G, Chun J, Rosen H. S1P3 receptor-induced reorganization of epithelial tight junctions compromises lung barrier integrity and is potentiated by TNF. Proc Natl Acad Sci USA 2005; 102: 9270–9275
   PubMed Web of Science ®Google Scholar
• Albert R, Hinterding K, Brinkmann V, Guerini D, Muller-Hartwieg C, Knecht H, Simeon C, Streiff M, Wagner T, Welzenbach K, Zecri F, Zollinger M, Cooke N, Francotte E. Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer. J Med Chem 2005; 48: 5373–5377
   PubMed Web of Science ®Google Scholar
• Brinkmann V, Davis D M, Heise C E, Albert R, Cottens S, Hof R, Bruns C, Prieschl E, Baumruker T, Hiestand P, Foster C A, Zollinger M, Lynch K R. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem 2002; 277: 21453–21457
   PubMed Web of Science ®Google Scholar
• Mandala S, Hajdu R, Bergstrom J, Quackenbush E, Xie J, Milligan J, Thornton R, Shei G J, Card D, Keohane C A, Rosenbach M, Hale J, Lynch C L, Rupprecht K, Parsons W, Rosen H. Alteration of lymphocyte trafficking by sphingosine 1-phosphate receptor agonists. Science 2002; 296: 346–349
   PubMed Web of Science ®Google Scholar
• Brinkmann V, Cyster J G, Hla T. FTY720: Sphingosine 1-phosphate receptor-1 in the control of lymphocyte egress and endothelial barrier function. Am J Transplant 2004; 4: 1019–1025
   PubMed Web of Science ®Google Scholar
• Jo E, Sanna M G, Gonzalez-Cabrera P J, Thangada S, Tigyi G, Osborne D A, Hla T, Parrill A L, Rosen H. S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate. Chem Biol 2005; 12: 703–715
   PubMed Web of Science ®Google Scholar
• Hla T, Maciag T. An abundant transcript induced in differentiating human endothelial cells encodes a polypeptide with structural similarities to G protein-coupled receptors. J Biol Chem 1990; 265: 9308–9313
   PubMed Web of Science ®Google Scholar
• Allende M L, Proia R L. Sphingosine 1-phosphate receptors and the development of the vascular system. Biochim Biophys Acta 2002; 1582: 222–227
   PubMed Web of Science ®Google Scholar
• LaMontagne K, Littlewood-Evans A, Schnell C, O'Reilly T, Wyder L, Sanchez T, Probst B, Butler J, Wood A, Liau G, Billy E, Theuer A, Hla T, Wood J. Antagonism of sphingosine-1-phosphate receptors by FTY720 inhibits angiogenesis and tumor vascularization. Cancer Res 2006; 66: 221–231
   PubMed Web of Science ®Google Scholar
• Offermanns S, Simon M I. Gα 15 and Gα 16 couple a wide variety of receptors to phospolipase C. J Biol Chem 1995; 270: 15175–15180
   PubMed Web of Science ®Google Scholar
• Liu A MF, Ho M K, Wong C SS, Chan J HP, Pau A HM, Wong Y H. Gα 16/z chimeras efficiently link a wide range of G protein-coupled receptors to calcium mobilization. J Biomol Screen 2003; 8: 39–49
   PubMed Web of Science ®Google Scholar
• Holdsworth G, Slocombe P, Hutchinson G, Milligan G. Analysis of endogenous S1P and LPA receptor expression in CHO-K1 cells. Gene 2005; 350: 59–63
   PubMed Web of Science ®Google Scholar
• Sato K, Tomura H, Igarashi Y, Ui M, Okajima F. Possible involvement of cell surface receptors in sphingosine 1-phosphate–induced activation of extracellular signal-regulated kinase in C6 glioma cells. Mol Pharmacol 1999; 55: 126–133
   PubMed Web of Science ®Google Scholar
• Candelore M R, Wright M J, Tota L M, Milligan J, Shei G J, Bergstrom J D, Mandala S M. Phytosphingosine 1-phosphate: A high affinity ligand for the S1P(4)/Edg-6 receptor. Biochem Biophys Res Commun 2002; 297: 600–606
   PubMed Web of Science ®Google Scholar
• Graeler M H, Goetzl E J. The immunosuppressant FTY720 down-regulates sphingosine 1-phosphate G-protein-coupled receptors. FASEB J 2004; 18: 551–553
   PubMed Web of Science ®Google Scholar
• Claing A, Laporte S A, Caron M G, Lefkowitz R J. Endocytosis of G protein-coupled receptors: Roles of G protein-coupled receptor kinases and beta-arrestin proteins. Prog Neurobiol 2002; 66: 61–79
   PubMed Web of Science ®Google Scholar