Sphingosine 1-phosphate receptor 1 as a useful target for treatment of multiple sclerosis

Pharmaceuticals

Volumn 5, Issue 5, 2012, Pages 514-528

  Chiba, Kenji ^a   Adachi, Kunitomo ^a  

^a MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

Author keywords

Experimental autoimmune encephalomyelitis (EAE); Fingolimod (FTY720); Immunomodulator; Lymphocyte egress; Multiple sclerosis (MS); Sphingosine 1 phasphate (S1P); Therapy

Indexed keywords

BETA INTERFERON; BETA1A INTERFERON; CYCLOPHOSPHAMIDE; CYCLOSPORIN A; FINGOLIMOD; GLATIRAMER; IMUSERA; PLACEBO; RECOMBINANT BETA INTERFERON; SPHINGOSINE 1 PHOSPHATE RECEPTOR; SPHINGOSINE 1 PHOSPHATE RECEPTOR 1; TACROLIMUS; UNCLASSIFIED DRUG;

ALLERGIC ENCEPHALOMYELITIS; ARTHRITIS; AUTOIMMUNE DISEASE; CLINICAL EFFECTIVENESS; CONCENTRATION RESPONSE; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG POTENCY; DRUG POTENTIATION; DRUG PROTEIN BINDING; DRUG TARGETING; HUMAN; IMMUNOMODULATION; LUPUS ERYTHEMATOSUS NEPHRITIS; LYMPHOCYTE ACTIVATION; LYMPHOCYTE COUNT; LYMPHOID ORGAN; MULTIPLE SCLEROSIS; NEUROPROTECTION; NONHUMAN; OUTCOME ASSESSMENT; PROTEIN EXPRESSION; PROTEIN FUNCTION; REVIEW; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; TREATMENT DURATION;

EID: 84861599724     PISSN: None     EISSN: 14248247     Source Type: Journal    
DOI: 10.3390/ph5050514     Document Type: Review

References (52)

1. Fujita, T.; Inoue, K.; Yamamoto, S.; Ikumoto, T.; Sasaki, S.; Toyama, R.; Chiba, K.; Hoshino, Y.; Okumoto, T. Fungal metabolites. Part 11. A potent immunosuppressive activity found in Isaria sinclairii metabolite. J. Antibiot. 1994, 47, 208-215.
2. Adachi, K.; Kohara, T.; Nakao, N.; Arita, M.; Chiba, K.; Mishina, T.; Sasaki, S.; Fujita, T. Design, synthesis, and structure-activity relationships of 2-infstituted-2-amino-1,3-propanediols: Discovery of a novel immunosuppressant, FTY720. Bioorg. Med. Chem. Lett. 1995, 5, 853-856.
3. Fujita, T.; Yoneta, M.; Hirose, R.; Sasaki, S.; Inoue, K.; Kiuchi, M.; Hirase, S.; Adachi, K.; Arita, M.; Chiba, K. Simple compounds, 2-alkyl-2-amino-1,3-propane-diols have potent immunosuppressive activity. Bioorg. Med. Chem. Lett. 1995, 5, 847-852.
4. Fujita, T.; Hirose, R.; Yoneta, M.; Sasaki, S.; Inoue, K.; Kiuchi, M.; Hirase, S.; Chiba, K.; Sakamoto, H.; Arita, M. Potent immunosuppressants, 2-alkyl-2-aminopropane-1,3-diols. J. Med. Chem. 1996, 39, 4451-4459.
5. Chiba, K.; Hoshino, Y.; Suzuki, C.; Mainfuchi, Y.; Yanagawa, Y.; Ohtsuki, M.; Sasaki, S.; Fujita, T. FTY720, a novel immunosuppressant possessing unique mechanisms. I. Prolongation of skin allograft survival and synergistic effect in combination with cyclosporine in rats. Transplant. Proc. 1996, 28, 1056-1059.
6. Hoshino, Y.; Suzuki, C.; Ohtsuki, M.; Mainfuchi, Y.; Amano, Y.; Chiba, K. FTY720, a novel immunosuppressant possessing unique mechanisms. II. Long-term graft survival induction in rat heterotopic cardiac allografts and synergistic effect in combination with cyclosporine A. Transplant. Proc. 1996, 28, 1060-1061.
7. Kawaguchi, T.; Hoshino, Y.; Rahman, F.; Amano, Y.; Higashi, H.; Kataoka, H.; Ohtsuki, M.; Teshima, K.; Chiba, K.; Kakefuda, T. et al. FTY720, a novel immunosuppressant possessing unique mechanisms. III. Synergistic prolongation of canine renal allograft survival in combination with cyclosporine A. Transplant. Proc. 1996, 28, 1062-1063.
8. Chiba, K. FTY720, a new class of immunomodulator, inhibits lymphocyte egress from secondary lymphoid tissues and thymus by agonistic activity at sphingosine 1-phosphate receptors. Pharmacol. Ther. 2005, 108, 308-319.
9. Matsuura, M.; Imayoshi, T.; Chiba, K.; Okumoto, T. Effect of FTY720, a novel immunosuppressant, on adjuvant-induced arthritis in rats. Inflamm. Res. 2000, 49, 404-410.
10. Chiba, K.; Yanagawa, Y.; Mainfuchi, Y.; Kataoka, H.; Kawaguchi, T.; Ohtsuki, M.; Hoshino, Y. FTY720, a novel immunosuppressant, induces sequestration of circulating mature lymphocytes by acceleration of lymphocyte homing in rats. I. FTY720 selectively decreases the number of circulating mature lymphocytes by acceleration of lymphocyte homing. J. Immunol. 1998, 160, 5037-5044.
11. Brinkmann, V.; Pinschewer, D.; Chiba, K.; Feng, L. FTY720: A novel transplantation drug that modulates lymphocyte traffic rather than activation. Trends Pharmacol. Sci. 2000, 21, 49-52.
12. Yanagawa, Y.; Sugahara, K.; Kataoka, H.; Kawaguchi, T.; Mainfuchi, Y.; Chiba, K. FTY720, a novel immunosuppressant, induces sequestration of circulating mature lymphocytes by acceleration of lymphocyte homing in rats. II. FTY720 prolongs skin allograft survival by decreasing T cell infiltration into grafts but not cytokine production in vivo. J. Immunol. 1998, 160, 5493-5499.
13. Cyster, J.G. Chemokines, sphingosine-1-phosphate, and cell migration in secondary lymphoid organs. Annu. Rev. Immunol. 2005, 23, 127-159.
14. Matloubian, M.; Lo, C.G.; Cinamon, G.; Lesneski, M.J.; Xu, Y.; Brinkmann, V.; Allende, M.L.; Proia, R.L.; Cyster, J.G. Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature 2004, 427, 355-360.
15. Brinkmann, V.; Davis, M.D.; Heise, C.E.; Albert, R.; Cottens, S.; Hof, R.; Bruns, C.; Prieschl, E.; Baumruker, T.; Hiestand, P. et al. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J. Biol. Chem. 2002, 277, 21453-21457.
16. Paugh, S.W.; Payne, S.G.; Barbour, S.E.; Milstien, S.; Spiegel, S. The immunosuppressant FTY720 is phosphorylated by sphingosine kinase type 2. FEBS Lett. 2003, 554,189-193.
17. Chiba, K.; Matsuyuki, H.; Maeda, Y.; Sugahara, K. Role of sphingosine 1-phosphate receptor type 1 in lymphocyte egress from secondary lymphoid tissues and thymus. Cell. Mol. Immunol. 2006, 3, 11-19.
18. Maeda, Y.; Matsuyuki, H.; Shimano, K.; Kataoka, H.; Sugahara, K.; Chiba, K. Migration of CD4 T cells and dendritic cells toward sphingosine 1-phosphate (S1P) is mediated by different receptor inftypes: S1P regulates the functions of murine mature dendritic cells via S1P receptor type 3. J. Immunol. 2007, 178, 3437-3446.
19. Pham, T.H.; Okada, T.; Matloubian, M.; Lo, C.G.; Cyster, J.G. S1P1 receptor signaling overrides retention mediated by G alpha i-coupled receptors to promote T cell egress. Immunity 2008, 28, 122-133.
20. Fujita, T.; Inoue, K.; Yamamoto, S.; Ikumoto, T.; Sasaki, S.; Toyama, R.; Chiba, K.; Hoshino, Y.; Okumoto, T. Fungal metabolites. Part 12. Potent immunosuppressant, 14-deoxomyruiocin, (2S,3R,4R)-(E)-2-amino-3,4-dihydroxy-2-hydroxymethyleicos-6-enoic acid and structure-activity relationships of myriocin derivatives. J. Antibiot. 1994, 47, 216-224.
21. Chiba, K. Immunoregulation by sphinfosine 1-phosphate receptor modulator, FTY720. Kagaku To Seibutsu 2008, 46, 259-264.
22. Kiuchi, M.; Adachi, K.; Kohara, T.; Minoguchi, M.; Hanano, T.; Aoki, Y.; Mishina, T.; Arita, M.; Nakao, N.; Ohtsuki, M. et al. Synthesis and immunosuppressive activity of 2-infstituted 2-aminopropane-1,3-diols and 2-aminoethanols. J. Med. Chem. 2000, 43, 2946-2961.
23. Adachi, K.; Chiba, K. FTY720 story. Its discovery and the following accelerated development of sphingosine 1-phosphate receptor agonists as immunomodulators based on reverse pharmacology. Perspect. Medicin. Chem. 2008, 1, 11-23.
24. Suzuki, S.; Kakefuda, T.; Amemiya, H.; Chiba, K.; Hoshino, Y.; Kawaguchi, T.; Kataoka, H.; Rahman, F. An immunosuppressive regimen using FTY720 combined with cyclosporin in canine kidney transplantation. Transpl. Int. 1998, 11, 95-101.
25. Yanagawa, Y.; Mainfuchi, Y.; Chiba, K. FTY720, a novel immunosuppressant, induces sequestration of circulating mature lymphocytes by acceleration of lymphocyte homing in rats, III. Increase in frequency of CD62L-positive T cells in Peyer's patches by FTY720-induced lymphocyte homing. Immunology 1998, 95, 591-594.
26. Kataoka, H.; Sugahara, K.; Shimano, K.; Teshima, K.; Koyama, M.; Fukunari, A.; Chiba, K. FTY720, sphingosine 1-phosphate receptor modulator, ameliorates experimental autoimmune encephalomyelitis by inhibition of T cell infiltration. Cell. Mol. Immunol. 2005, 2, 439-448.
27. Lo, C.G.; Xu, Y.; Proia, R.L.; Cyster, J.G. Cyclical modulation of sphingosine-1-phosphate receptor 1 surface expression during lymphocyte recirculation and relationship to lymphoid organ transit. J. Exp. Med. 2005, 201, 291-301.
28. Pappu, R.; Schwab, S.R.; Cornelissen, I.; Pereira, J.P.; Regard, J.B.; Xu, Y.; Camerer, E.; Zheng, Y.W.; Huang, Y.; Cyster, J.G. et al. Promotion of lymphocyte egress into blood and lymph by distinct sources of sphingosine-1-phosphate. Science 2007, 316, 295-298.
29. Pyne, S.; Pyne, N. Sphingosine 1-phosphate signalling via the endothelial differentiation gene family of G-protein-coupled receptors. Pharmacol. Ther. 2000, 88, 115-131.
30. Spiegel, S. Sphingosine 1-phosphate: A ligand for the EDG-1 family of G-protein-coupled receptors. Ann. NY Acad. Sci. 2000, 905, 54-60.
31. Mandala, S.; Hajdu, R.; Bergstrom, J.; Quackenbush, E.; Xie, J.; Milligan, J.; Thornton, R.; Shei, G.J.; Card, D.; Keohane, C. et al. Alteration of lymphocyte trafficking by sphingosine-1-phosphate receptor agonists. Science 2002, 296, 346-349.
32. Kiuchi, M.; Adachi, K.; Tomatsu, A.; Chino, M.; Takeda, S.; Tanaka, Y.; Maeda, Y.; Sato, N.; Mitsutomi, N.; Sugahara, K. et al. Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate. Bioorg. Med. Chem. 2005, 13, 425-432.
33. Matsuyuki, H.; Maeda, Y.; Yano, K.; Sugahara, K.; Chiba, K.; Kohno, T.; Igarashi, Y. Involvement of sphingosine 1-phosphate (S1P) receptor type 1 and type 4 in migratory response of mouse T cells toward S1P. Cell. Mol. Immunol. 2006, 3, 429-437.
34. Webb, M.; Tham, C.S.; Lin, F.F.; Lariosa-Willingham, K.; Yu, N.; Hale, J.; Mandala, S.; Chun, J.; Rao, T.S. Sphingosine 1-phosphate receptor agonists attenuate relapsing-remitting experimental autoimmune encephalitis in SJL mice. J. Neuroimmunol. 2004, 153, 108-121.
35. Balatoni, B.; Storch, M.K.; Swoboda, E.M.; Schonborn, V.; Koziel, A.; Lambrou, G.N.; Hiestand, P.C.; Weissert, R.; Foster, C.A. FTY720 sustains and restores neuronal function in the DA rat model of MOG-induced experimental autoimmune encephalomyelitis. Brain Res. Bull. 2007, 74, 307-316.
36. Brinkmann, V. Sphingosine 1-phosphate receptors in health and disease: Mechanistic insights from gene deletion studies and reverse pharmacology. Pharmacol. Ther. 2007, 115, 84-105.
37. Foster, C.A.; Howard, L.M.; Schweitzer, A.; Persohn, E.; Hiestand, P.C.; Balatoni, B.; Reuschel, R.; Beerli, C.; Schwartz, M.; Billich, A. Brain penetration of the oral immunomodulatory drug FTY720 and its phosphorylation in the central nervous system during experimental autoimmune encephalomyelitis: Consequences for mode of action in multiple sclerosis. J. Pharmacol. Exp. Ther. 2007, 323, 469-475.
38. Chiba, K.; Kataoka, H.; Seki, N.; Shimano, K.; Koyama, M.; Fukunari, A.; Sugahara, K.; Sugita, T. Fingolimod (FTY720), sphingosine 1-phosphate receptor modulator, shows superior efficacy as compared with interferon-β in mouse experimental autoimmune encephalomyelitis. Int. Immunopharmacol. 2011, 11, 366-372.
39. Langrish, C.L.; Chen, Y.; Blumenschein, W.M.; Mattson, J.; Basham, B.; Sedgwick, J.D.; McClanahan, T.; Kastelein, R.A.; Cua, D.J. IL-23 drives a pathogenic T cell population that induces autoimmune inflammation. J. Exp. Med. 2005, 201, 233-240.
40. Komiyama, Y.; Nakae, S.; Matsuki, T.; Nambu, A.; Ishigame, H.; Kakuta, S.; Sudo, K.; Iwakura, Y. IL-17 plays an important role in the development of experimental autoimmune encephalomyelitis. J. Immunol. 2006, 177, 566-573.
41. Stromnes, I.M.; Cerretti, L.M.; Liggitt, D.; Harris, R.A.; Goverman, J.M. Differential regulation of central nervous system autoimmunity by TH1 and TH17 cells. Nat. Med. 2008, 14, 337-342.
42. Seki, N.; Maeda, Y.; Kataoka, H.; Sugahara, K.; Sugita, T.; Chiba, K. Fingolimod (FTY720) ameliorates Experimental Autoimmune Encephalomyelitis (EAE) II. FTY720 decreases infiltration of Th17 and Th1 cells into the central nervous system in EAE. Inflamm. Regen. 2010, 30, 545-551.
43. Brinkmann, V. FTY720 (fingolimod) in Multiple Sclerosis: Therapeutic effects in the immune and the central nervous system. Br. J. Pharmacol. 2009, 158, 1173-1182.
44. Choi, J.W.; Gardell, S.E.; Herr, D.R.; Rivera, R.; Lee, C.W.; Noguchi, K.; Teo, S.T.; Yung, Y.C.; Lu, M.; Kennedy, G. et al. FTY720 (fingolimod) efficacy in an animal model of multiple sclerosis requires astrocyte sphingosine 1-phosphate receptor 1 (S1P1) modulation. Proc. Natl. Acad. Sci. USA 2011, 108, 751-756.
45. Martin, R.; McFarland, H.F.; McFarlin, D.E. Immunological aspects of demyelinating diseases. Annu. Rev. Immunol. 1992, 10, 153-187.
46. Kornek, B.; Storch, M.K.; Weissert, R.; Wallstroem, E.; Stefferl, A.; Olsson, T.; Linington, C.; Schmidbauer, M.; Lassmann, H. Multiple sclerosis and chronic autoimmune encephalomyelitis: A comparative quantitative study of axonal injury in active, inactive, and remyelinated lesions. Am. J. Pathol. 2000, 157, 267-276.
47. Lublin, F.D.; Reingold, S.C. Defining the clinical course of multiple sclerosis: Results of an international survey. National Multiple Sclerosis Society (USA) Advisory Committee on Clinical Trials of New Agents in Multiple Sclerosis. Neurology 1996, 46, 907-911.
48. Goodkin, D.E.; Reingold, S.; Sibley, W.; Wolinsky, J.; McFarland, H.; Cookfair, D.; Lublin, F.D. Guidelines for clinical trials of new therapeutic agents in multiple sclerosis: Reporting extended results from phase III clinical trials. National Multiple Sclerosis Society Advisory Committee on Clinical Trials of New Agents in Multiple Sclerosis. Ann. Neurol. 1999, 46, 132-134.
49. Kappos, L.; Antel, J.; Comi, G.; Montalban, X.; O'Connor, P.; Polman, C.H.; Haas, T.; Korn, A.A.; Karlsson, G.; Radue, E.W. Oral fingolimod (FTY720) for relapsing multiple sclerosis. N. Engl. J. Med. 2006, 355, 1124-1140.
50. Mehling, M.; Lindberg, R.; Raulf, F.; Kuhle, J.; Hess, C.; Kappos, L.; Brinkmann, V. Th17 central memory T cells are reduced by FTY720 in patients with multiple sclerosis. Neurology 2010, 75, 403-410.
51. Kappos, L.; Radue, E.W.; O'Connor, P.; Polman, C.; Hohlfeld, R.; Calabresi, P.; Selmaj, K.; Agoropoulou, C.; Leyk, M.; Zhang-Auberson, L. et al. A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis. N. Engl. J. Med. 2010, 362, 387-401.
52. Cohen, J.A.; Barkhof, F.; Comi, G.; Hartung, H.P.; Khatri, B.O.; Montalban, X.; Pelletier, J.; Capra, R.; Gallo, P.; Izquierdo, G. et al. Oral fingolimod or intramuscular interferon for relapsing multiple sclerosis. N. Engl. J. Med. 2010, 362, 402-415.