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Chemical Compound Review

Fingolimod     2-amino-2-[2-(4- octylphenyl)ethyl]propane...

Synonyms: SureCN7445, Gilenya (TN), FTY270, CHEMBL314854, CHEBI:63115, ...
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Disease relevance of FTY720

  • After FTY720 treatment, the number of CD4(+) and CD8(+) T cells as well as B cells in peripheral blood is reduced while pertussis toxin-sensitive homing into peripheral lymph nodes, mesenteric lymph node, and Peyer's patches is increased [1].
  • We demonstrate here that FTY720 markedly reduces GvHD in a clinically relevant, haploidentical strain combination, while permitting antitumor effects against a T cell lymphoma of unshared host MHC haplotype to proceed unhindered [2].
  • FTY720, a promising immunosuppressant for use in patients with tissue transplants and autoimmune diseases, is currently in clinical trials [3].
  • Consequently, administration of FTY720 does not induce lymphopenia in SPHK2-deficient mice [4].
  • In nonobese diabetic-severe combined immunodeficient (NOD/SCID) mice, the number of CD34+/CD38- cells that homed to the BM after 18 hours was significantly raised by pretreatment of animals and cells with FTY720, tending to result in improved engraftment [5].

High impact information on FTY720

  • S1P receptor-1 is required for lymphocyte egress from thymus and secondary lymphoid organs and is downregulated by the immunosuppressive drug FTY720 [6].
  • Immunotherapy with CD25-specific and CD154-specific monoclonal antibodies, FTY720 (or tacrolimus), everolimus and leflunomide suppressed indirect activation of T cells, elicitation of non-Gal pig-specific IgG antibody, intragraft expression of proinflammatory cytokines and invasion of infiltrating mononuclear cells into islets [7].
  • Here we report that FTY720, a drug that targets sphingosine 1-phosphate (S1P) receptors, induced marginal zone B cell migration into follicles [8].
  • In this study we demonstrate that FTY720 rescues the homing defect in both CCR7(-/-) mice and plt mice [1].
  • Thus, our data suggest an alternative G-alpha(i)-dependent, CCR7-CCL19/CCL21-independent mechanism for lymphocyte homing through HEVs which is strongly augmented in the presence of FTY720 [1].

Chemical compound and disease context of FTY720


Biological context of FTY720


Anatomical context of FTY720


Associations of FTY720 with other chemical compounds


Gene context of FTY720

  • We conclude that activation of S1PRs by FTY720 increases CXCR4 function in HPCs both in vitro and in vivo, supporting homing and proliferation of HPCs [5].
  • We show here that FTY720 has antiangiogenic activity, potently abrogating VEGF- and S1P-induced angiogenesis in vivo in growth factor implant and corneal models [22].
  • Both FTY720 and FTY-P apparently failed to impede VEGF-produced increases in mitogen-activated protein kinase activity in human umbilical vascular endothelial cells (HUVEC), and unlike its activity in causing S1PR internalization, FTY-P did not result in a decrease of surface VEGFR2 levels in HUVEC cells [22].
  • So far, phosphorylation of FTY720 by murine sphingosine kinase (SPHK) 1a had been documented [21].
  • We have also demonstrated that activation of the ERK signaling pathway completely suppressed the FTY720-induced apoptotic process including activation of caspase 3 and activation of JNK and the 36-kDa MBP kinase [23].

Analytical, diagnostic and therapeutic context of FTY720

  • FTY720 is a novel immunosuppressant that is highly effective in inhibiting rejection of allografts and autoimmunity in various animal models [16].
  • FTY720, a potent immunomodulatory drug in phase 2/3 clinical trials, induces rapid and reversible sequestration of lymphocytes into secondary lymphoid organs, thereby preventing their migration to sites of inflammation [4].
  • To further define the role of S1P1 in lymphocyte trafficking, we performed adoptive transfer experiments and intravital microscopy (IVM) using both S1P1-/- lymphocytes and recipient wild-type (WT) mice treated with FTY720, an immunosuppressant that downmodulates S1P receptors [20].
  • Electron microscopy revealed distinct changes on the cell surface with decreased filopodias and microvilli in cancer cells treated with FTY720 at 2 microM and clear evidence of apoptosis at 10 microM [24].
  • Novel insights into the mechanism of action of FTY720 in a transgenic model of allograft rejection: implications for therapy of chronic rejection [25].


  1. CC chemokine receptor 7-dependent and -independent pathways for lymphocyte homing: modulation by FTY720. Henning, G., Ohl, L., Junt, T., Reiterer, P., Brinkmann, V., Nakano, H., Hohenberger, W., Lipp, M., Förster, R. J. Exp. Med. (2001) [Pubmed]
  2. Graft-versus-host disease can be separated from graft-versus-lymphoma effects by control of lymphocyte trafficking with FTY720. Kim, Y.M., Sachs, T., Asavaroengchai, W., Bronson, R., Sykes, M. J. Clin. Invest. (2003) [Pubmed]
  3. Linking Chinese medicine and G-protein-coupled receptors. Im, D.S. Trends Pharmacol. Sci. (2003) [Pubmed]
  4. Sphingosine kinase type 2 is essential for lymphopenia induced by the immunomodulatory drug FTY720. Zemann, B., Kinzel, B., Müller, M., Reuschel, R., Mechtcheriakova, D., Urtz, N., Bornancin, F., Baumruker, T., Billich, A. Blood (2006) [Pubmed]
  5. 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]
  6. Chemokines, sphingosine-1-phosphate, and cell migration in secondary lymphoid organs. Cyster, J.G. Annu. Rev. Immunol. (2005) [Pubmed]
  7. Prolonged diabetes reversal after intraportal xenotransplantation of wild-type porcine islets in immunosuppressed nonhuman primates. Hering, B.J., Wijkstrom, M., Graham, M.L., Hårdstedt, M., Aasheim, T.C., Jie, T., Ansite, J.D., Nakano, M., Cheng, J., Li, W., Moran, K., Christians, U., Finnegan, C., Mills, C.D., Sutherland, D.E., Bansal-Pakala, P., Murtaugh, M.P., Kirchhof, N., Schuurman, H.J. Nat. Med. (2006) [Pubmed]
  8. Sphingosine 1-phosphate receptor 1 promotes B cell localization in the splenic marginal zone. Cinamon, G., Matloubian, M., Lesneski, M.J., Xu, Y., Low, C., Lu, T., Proia, R.L., Cyster, J.G. Nat. Immunol. (2004) [Pubmed]
  9. Enhanced FTY720-mediated lymphocyte homing requires G alpha i signaling and depends on beta 2 and beta 7 integrin. Pabst, O., Herbrand, H., Willenzon, S., Worbs, T., Schippers, A., Müller, W., Bernhardt, G., Förster, R. J. Immunol. (2006) [Pubmed]
  10. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. Brinkmann, V., Davis, M.D., 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. J. Biol. Chem. (2002) [Pubmed]
  11. FTY720 immunosuppression impairs effector T cell peripheral homing without affecting induction, expansion, and memory. Pinschewer, D.D., Ochsenbein, A.F., Odermatt, B., Brinkmann, V., Hengartner, H., Zinkernagel, R.M. J. Immunol. (2000) [Pubmed]
  12. Transient T cell accumulation in lymph nodes and sustained lymphopenia in mice treated with FTY720. Morris, M.A., Gibb, D.R., Picard, F., Brinkmann, V., Straume, M., Ley, K. Eur. J. Immunol. (2005) [Pubmed]
  13. Early induction of apoptosis in androgen-independent prostate cancer cell line by FTY720 requires caspase-3 activation. Wang, J.D., Takahara, S., Nonomura, N., Ichimaru, N., Toki, K., Azuma, H., Matsumiya, K., Okuyama, A., Suzuki, S. Prostate (1999) [Pubmed]
  14. FTY720 stimulates multidrug transporter- and cysteinyl leukotriene-dependent T cell chemotaxis to lymph nodes. Honig, S.M., Fu, S., Mao, X., Yopp, A., Gunn, M.D., Randolph, G.J., Bromberg, J.S. J. Clin. Invest. (2003) [Pubmed]
  15. FTY720: targeting G-protein-coupled receptors for sphingosine 1-phosphate in transplantation and autoimmunity. Brinkmann, V., Lynch, K.R. Curr. Opin. Immunol. (2002) [Pubmed]
  16. FTY720 suppresses humoral immunity by inhibiting germinal center reaction. Han, S., Zhang, X., Wang, G., Guan, H., Garcia, G., Li, P., Feng, L., Zheng, B. Blood (2004) [Pubmed]
  17. FTY720 induces apoptosis in multiple myeloma cells and overcomes drug resistance. Yasui, H., Hideshima, T., Raje, N., Roccaro, A.M., Shiraishi, N., Kumar, S., Hamasaki, M., Ishitsuka, K., Tai, Y.T., Podar, K., Catley, L., Mitsiades, C.S., Richardson, P.G., Albert, R., Brinkmann, V., Chauhan, D., Anderson, K.C. Cancer Res. (2005) [Pubmed]
  18. The immunosuppressant drug FTY720 inhibits cytosolic phospholipase A2 independently of sphingosine-1-phosphate receptors. Payne, S.G., Oskeritzian, C.A., Griffiths, R., Subramanian, P., Barbour, S.E., Chalfant, C.E., Milstien, S., Spiegel, S. Blood (2007) [Pubmed]
  19. Plasma cell S1P1 expression determines secondary lymphoid organ retention versus bone marrow tropism. Kabashima, K., Haynes, N.M., Xu, Y., Nutt, S.L., Allende, M.L., Proia, R.L., Cyster, J.G. J. Exp. Med. (2006) [Pubmed]
  20. The S1P-analog FTY720 differentially modulates T-cell homing via HEV: T-cell-expressed S1P1 amplifies integrin activation in peripheral lymph nodes but not in Peyer patches. Halin, C., Scimone, M.L., Bonasio, R., Gauguet, J.M., Mempel, T.R., Quackenbush, E., Proia, R.L., Mandala, S., von Andrian, U.H. Blood (2005) [Pubmed]
  21. Phosphorylation of the immunomodulatory drug FTY720 by sphingosine kinases. Billich, A., Bornancin, F., Dévay, P., Mechtcheriakova, D., Urtz, N., Baumruker, T. J. Biol. Chem. (2003) [Pubmed]
  22. Antagonism of sphingosine-1-phosphate receptors by FTY720 inhibits angiogenesis and tumor vascularization. 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. Cancer Res. (2006) [Pubmed]
  23. Differential activation of c-Jun NH2-terminal kinase and p38 pathways during FTY720-induced apoptosis of T lymphocytes that is suppressed by the extracellular signal-regulated kinase pathway. Matsuda, S., Minowa, A., Suzuki, S., Koyasu, S. J. Immunol. (1999) [Pubmed]
  24. Marked prevention of tumor growth and metastasis by a novel immunosuppressive agent, FTY720, in mouse breast cancer models. Azuma, H., Takahara, S., Ichimaru, N., Wang, J.D., Itoh, Y., Otsuki, Y., Morimoto, J., Fukui, R., Hoshiga, M., Ishihara, T., Nonomura, N., Suzuki, S., Okuyama, A., Katsuoka, Y. Cancer Res. (2002) [Pubmed]
  25. Novel insights into the mechanism of action of FTY720 in a transgenic model of allograft rejection: implications for therapy of chronic rejection. Habicht, A., Clarkson, M.R., Yang, J., Henderson, J., Brinkmann, V., Fernandes, S., Jurewicz, M., Yuan, X., Sayegh, M.H. J. Immunol. (2006) [Pubmed]
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