S1P receptor agonists, a novel generation of immunosuppressants

G Protein-Coupled Receptors: Structure, Signaling, and Physiology

Volumn , Issue , 2010, Pages 380-397

  Almagro, Rosa López ^a   Tarrasón, Gema ^a   Godessart, Nuria ^a  

^a Research and Development Center Almirall ^*  (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 84928859917     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1017/CBO9780511760334.018     Document Type: Chapter

References (96)

1. Pyne S et al. (2000) Sphingosine 1-phosphate signalling in mammalian cells. Biochem J, 349 (2), 385-402.
2. Pitson SM et al. (2000) Human sphingosine kinase: Purification, molecular cloning and characterization of the native and recombinant enzymes. Biochemistry Journal, 350 (2), 429-441.
3. Zhou J et al. (1998) Identification of the first mammalian sphingosine phosphate lyase gene and its functional expression in yeast. Biophys. Res. Commun. 242, 502-507
4. Cuvillier O. et al. (1996) Supression of ceramide-mediated programmed cell death by sphingosine-1-phosphate. Nature, 381, 800-803.
5. Alvarez SE et al. (2007) Autocrine and paracrine roles of sphingosine-1-phosphate. Trends Endocrinol. Metab., 18,300-307.
6. Maceyka M et al. (2005) Sphk1 and Sphk2: Sphingosine kinase isoenzymes with opposing functions in sphingolipid metabolism. J. Biol. Chem, 280, 37118-37129
7. Le Stunff H. et al. (2007) Recycling of sphingosine is regulated by the concerted actions of sphingosine-1-phosphate phosphohydrolase 1 and sphingosine kinase 2. J Biol. Chem. 282, 3472-3480.
8. Mizugishi K et al. (2005) Essential role for sphingosine kinases in neural and vascular development. Mol. Cell Biol., 25, 11113-11121.
9. Xia P et al. (2000) An oncogenic role of sphingosine kinase. Curr. Biol. 10, 1527-1530.
10. Pappu R. et al (2007) Promotion of lymphocyte egress into blood and lymph by distinct sources of sphingosine-1-phosphate. Science, 316, 295-298.
11. Okajima F (2002) Plasma lipoproteins behave as carriers of extracellular sphingosine 1-phosphate: is this an atherogenic mediator or an anti-atherogenic mediator? Biochim. Biophys. Acta, 1582, 132-137.
12. Yatomi Y et al. (1997) Sphingosine 1-phosphate, a bioactive sphingolipid abundantly stored in platelets, is a normal constituent of human plasma and serum. J. Biochem. 121, 969-973.
13. Hanel P et al. (2007) Erythrocytes store and release sphingosine 1-phosphate in blood. FASEB J., 21, 1202-1209.
14. Kihara A et al. (2008) Production and release of sphingosine-1-phosphate and the phosphorylated form of the immunomodulator FTY720. Biochim. Biophys. Acta, 1781, 496-502.
15. Ventakaraman K et al. (2008) Vascular endothelium as a contributor of plasma sphingosine 1-phosphate. Circ. Res., 102, 669-676.
16. Olivera A et al. (2006) IgE-dependent activation of sphingosine kinases 1 and 2 and secretion of sphingosine 1-phosphate requires Fyn kinase and contributes to mast cell responses. J. Biol. Chem, 281, 2515-2525.
17. Mitra P et al. (2006) Role of ABCC1 in export of sphingosine-1-phosphate from mast cells. Proc. Natl. Acad. Sci. U.S.A., 103, 16394-16399.
18. Kobayashi N, et al. (2006) Sphingosine 1-phosphate is released from the cytosol of rat platelets in a carrier-mediated manner. J. Lipid Res., 47, 614-621
19. Lee YM et al. (2007) A novel method to quantify sphingosine 1-phosphate by immobilized metal affinity chromatography (IMAC). Prostaglandins Other Lipid Mediat., 84, 154-162.
20. Romiti E et al (2000) Neutral/alkaline and acid ceramidase activities are activily released by murine endothelial cells. Biochem. Biophys. Res. Commun., 275, 476-751
21. Tabas I. (1999) Secretory sphingomyelinase. Chem. Phys. Lipids, 102, 123-130
22. Ancellin N, Colmont C, Su J, Li Q Mittereder N, Chae SS, Stefansson S, Liau G, Hla T (2002) Extracellular export of sphingosine kinase-1 enzyme. Sphingosine 1-phosphate generation and the induction of angiogenic vascular maturation. J. Biol. Chem., 277, 6667-6675
23. Van Brocklyn JR. et al. (1998) Dual actions of sphingosine-1-phosphate: extracellular through the G- coupled receptor Edg-1 and intracellular to regulate proliferation and survival. J. Cell Biol., 142(1), 229-240.
24. Kariya Y et al. (2005) Products by the sphingosine kinase/sphingosine-1-phos-phate (S1P) lyase pathway but not S1P stimulate mitogenesis. Genes Cells, 10 (6), 605-615.
25. Hla T et al. (1990) An abundant transcript induced in differentiating human endothe-lial cells encodes a polypeptide with structural similarities to G-protein-coupled receptors. J. Biol. Chem. 265, 9308-9313.
26. Okamoto H et al. (1998) EDG1 is a functional sphingosine-1-phosphate receptor that is linged via a Gi/o to multiple signalling pathways, including phospholipase C activation, Ca2+ mobilization, Ras-mitogen-activated protein kinase activation, and adenylate cyclase inhibition. J. Biol. Chem. 273, 27104-27110.
27. Alderton F et al. (2001) Tethering of the platelet-derived growth factor beta receptor to G-protein coupled receptors: a novel platform for integrative signalling by these receptor classes in mammalian cells. J. Biol. Chem. 276, 28578-28585.
28. Liu Y et al.(2000) Edg-1, the G protein-coupled receptor for sphingosine-1-phosphate, is essential for vascular maturation. J. Clin. Invest. 106, 951-961.
29. Allende ML et al. (2003) G-protein-coupled receptor S1P1 acts within endothelial cells to regulate vascular maturation. Blood 102, 3665-3667.
30. Allende ML et al. (2004) Expression of the sphingosine-1-phosphate receptor, S1P1, on T cells controls thymic emigration. J. Biol. Chem. 279 (15), 15396-15401
31. Matloubian M. et al. (2004) Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature 427 (6972), 355-360
32. Chi H. et al. (2005) Cutting edge: Regulation of T cell trafficking and primary immune responses by sphingosine 1-phosphate receptor 1. J. Immunol. 174 (5), 2485-2488
33. Kabashima K et al. (2006) Plasma cell S1P1 expression determines secondary lymphoid organ retention versus bone marrow tropism. J. Exp. Med. 203(12), 2683-2690
34. Singleton PA et al. (2005), Regulation of sphingosine 1-phosphate-induced endothelial cytoskeletal rearrangement and barrier enhancement by S1P1 receptor, PI3 kinase, Tiam1/Rac1, and alpha-actinin.FASEB J. Oct; 19 (12):1646-56.
35. Kimura A et al (2007) Essential roles of sphingosine 1-phosphate/S1P1 receptor axis in the migration of neural stem cells toward a site of spinal cord injury. Stem Cells 25, 115-124.
36. Ishii I et al. (2001) Selective loss of sphingosine 1-phosphate signalling with no obvious phenotypic abnormality in mice lacking its G protein-coupled receptor, LP (B3)/EDG-3. J. Biol. Chem. 276, 33697-33704.
37. Ancellin N et al.(1999) Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5. Biol. Chem. 274, 18997-19002.
38. Okamoto H et al. (2000) 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. 20, 9247-9261.
39. Paik J H e t al. (2001) Sphingosine 1-phosphate-induced endothelial cell migration requires the expression of EDG-1 and EDG-3 receptors and Rho-dependent activation of alpha vbeta3- and beta1-containing integrins. J. Biol. Chem. 276, 11830-11837
40. Goparaju SK et al. (2005) The S1P2 receptor negatively regulates platelet-derived growth factor-induced motility and proliferation. Mol. Cell. Biol. 25(10), 4237-4249
41. Baudhuin LM et al. (2004) S1P3-mediated Akt-activation and cross-talk with platelet-derived growth factor receptor (PDGFR). FASEB J. 18(2), 341-343
42. Ishii I et al. (2002) Marked perinatal lethality and cellular signalling 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. 277, 25152-25159.
43. Kono M et al.(2004) The sphingosine-1-phosphate receptors S1P1, S1P2, and S1P3 function co-ordinately during embryonic angiogenesis. J. Biol. Chem. 279, 29367-29373
44. MacLennan AJ et al. (2001) An essential role for the H218/AGR16/Edg-5/LP(B2) sphin-gosine 1-phosphate receptor in neuronal excitability. Eur. J. Neurosci. 14, 203-209
45. Serriere-Lanneau V et al. (2007) The sphingosine 1-phosphate receptor S1P2 triggers hepatic wound healing. FASEB J. 21, 2005-2013.
46. Hu W et al. (2006) Lentiviral siRNA silencing of sphingosine-1-phosphate receptors S1P1 and S1P2 in smooth muscle. Biochem. Biophys. Res. Commun. 343, 1038-1044
47. Sanna MG. et al. (2004) Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J. Biol. Chem. 279, 13839-13848.
48. Theilmeier G et al. (2006) High-density lipoproteins and their constituent, sphin-gosine-1-phosphate, directly protect the heart against ischemia/reperfusion injury in vivo via the S1P3 lysophospholipid receptor. Circulation 114, 1403-1409
49. Gon Y et al. (2005) S1P3 receptor-induced reorganization of epithelial tight junctions compromises lung barrier integrity and is potentiated by TNF. Proc. Natl. Acad. Sci. U.S.A. 102, 9270-9275.
50. Niessen F et al. (2008) Dendritic cell PAR1-S1P3 signalling couples coagulation and inflammation. Nature 452, 654-658.
51. Graler MH et al. (2003) The sphingosine 1-phosphate receptor S1P4 regulates cell shape and motility via coupling to Gi and G12/13. J. Cell. Biochem. 89, 507-519
52. Malek RL et al. (2001) Nrg-1 belongs to the endothelial differentiation gene family of G protein-coupled sphingosine-1-phosphate receptors. J. Biol. Chem. 276: 5692-5699.
53. Deltagen Inc. 2005: http://www.informatics.jax.org/external/ko/deltagen/302
54. Jaillard C et al. (2005) Edg8/S1P5: an oligodendroglial receptor with dual function on process retraction and cell survival. J. Neurosci. 25, 1459-1469.
55. Novgorodov AS et al. (2007) Activation of sphingosine-1-phosphate receptor S1P5 inhibits oligodendrocyte progenitor migration. FASEB J. 21, 1503-1514
56. Walzer T et al. (2007) Natural killer cell trafficking in vivo requires a dedicated sphingosine 1-phosphate receptor. Nat. Immunol. 8, 1337-1344.
57. Rivera J et al. (2008) The alliance of sphingosine 1-phospahte and its receptors in immunity. Nat. Rev. Immunol. 8, 753-763.
58. Cyster JG. (2007) Specifying the patterns of immune cell migration Novartis Found. Symp. 281; 54-61
59. Grigorova IL et al. (2009) Cortical sinus probing, S1P1-dependent entry and flow-based capture of egressing T cells. Nat Immunol.; 10 (1):58-65.
60. Chaffin KE, and Perlmutter RM (1991) A pertussis toxin-sensitive process controls thymocyte emigration. Eur J Immunol.; 21(10):2565-73.
61. Chiba K, et al. (2006) Role of sphingosine 1-phosphate receptor type 1 in lymphocyte egress from secondary lymphoid tissues and thymus. Cell Mol. Immunol. 3 (1):11-9
62. Mandala S. et al (2002) Alteration of lymphocyte trafficking by sphingosine-1-phos-phate receptor agonists. Science; 296 (5566):346-9.
63. Hla T et al. (2008) The vascular S1P gradient: cellular sources and biological significance. Biochim Biophys Acta; 1781(9):477-82.
64. Vachal P et al. (2006) Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor. Bioorg Med Chem Lett.;16(14):3684-7.
65. Schwab SR and Cyster JG.(2007) Finding a way out: lymphocyte egress from lymphoid organs. Nat Immunol. 8 (12):1295-301
66. Rosen H, et al. (2009) Sphingosine 1-phosphate receptor signaling. Annu Rev Biochem; 78:743-68.
67. Wei SH, et al. (2005) Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses. Nat Immunol. 6 (12):1228-35.
68. Sanna G et al. (2006) Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nat Chem Biol. 2 (8):434-41
69. Oo ML et al. (2007) Immunosuppressive and anti-angiogenic sphingosine 1-phosphate receptor-1 agonists induce ubiquitinylation and proteasomal degradation of the receptor. J Biol Chem.; 282 (12):9082-9.
70. Harrington, LE. et al. (2005) Interleukin 17-producing CD4+ effector T cells develop via a lineage distinct from the T helper type 1 and 2 lineages. Nat. Immunol. 6:1123-1132.
71. Liao JJ et al. (2007) Cutting edge: alternative signalling of Th17 cell development by sphingosine 21-phosphate. J.Immunol. 178, 5425-5428.
72. Huang MC et al. (2007) Th17 augmentation in OTII TCR plus T cell-selective type 1 sphingosine 1-phosphate receptor double transgenic mice. J. Immunol. 178, 6806-6813.
73. Piccirillo CA et al. (2008) CD4+ Foxp3+ regulatory T cells in the control of autoimmu-nity: in vivo veritas. Curr. Opin. Immunol. 20, 655-662.
74. Liu G et al. (2009) The receptor SP1 overrides regulatory T cell mediated immune suppression through Akt-mTOR. Nat. Immunol. Jul;10 (7):769-77
75. Huwiler A et al. (2008) New players on the center stage: Sphingosine 1-phosphate and its receptors as drug targets. Biochem.Pharmacol. 75: 1893-1900.
76. Baumruker T. et al. (2007) FTY720, an immunomodulatory sphingolipd mimetic: translation of a novel mechanism into clinical benefit in multiple sclerosis. Expert Opin. Investig.Drugs 16; 283-289
77. Martini S et al. (2007) Current perspectives on FTY720. Expert Opin. Invest. Drugs 16, 505-518.
78. O' Connor P et al. (2009) Oral fingolimod (FTY720) in multiple sclerosis, Two year results of a phase II extension study. Neurology 72, 73-79.
79. Sawicka E et al. (2005) The sphingosine 1-phosphate receptor agonist FTY720 differentially affects the sequestration of CD4+/CD25+ T-regulatory cells and enhances their functional activity. J Immunol; 175 (12):7973-80.
80. Gergely P. et al. (2009) Phase I study with the selective S1P1/S1P5 receptor modulator BAF312 indicates that S1P1 rather than S1P3 mediates transient heart rate reduction in humans. Abstract P437. 25th Congress of the European Committee for Treatment and Research in Multiple Sclerosis. Sep 9-12
81. Düsseldorf, Germany. Shida D et al. (2008) Targeting SphK1 as a new strategy against cancer. Curr Drug Targets. 9(8):662-73.
82. Pappas, C. et al. (2008) LX2931: A Potential Small Molecule Treatment for Autoimmune Disorders. Presentation # 351, American College of Rheumatology meeting
83. O' Brien N et al. (2009) Production and characterization of monoclonal anti-sphingosine-1-phosphate antibodies. J. Lipid Res. 50, 2245-2257
84. Keul P et al. (2007) The sphingosine-1-phosphate analogue FTY720 reduces atherosclerosis in apolipoprotein E-deficient mice. Arterioscler. Thromb. Vasc. Biol. 27, 607-613.
85. Idzko M et al. (2006) Local application of FTY720 to the lung abrogates experimental asthma by altering dendritic cell function. J. Clin. Invest. 116, 2935-2944
86. Liu HB et al. (2008) Sphingosine-1-phosphate and its analogue FTY720 diminish acute pulmonary injury in rats with acute necrotizing pancreatitis. Pancreas 36, e10-5
87. Fujishiro J, et al. (2006). Use of sphingosine-1-phosphate 1 receptor agonist, KRP-203, in combination with a subtherapeutic dose of cyclosporine A for rat renal transplantation. Transplantation 82, 804-812.
88. Wenderfer SE et al. (2008) I ncreased survival and reduced renal injury in MRL/lpr mice treated with a novel sphingosine-1-phosphate receptor agonist. Kidney Int. 74, 1319-1326.
89. Ogawa R et al. (2007) A novel sphingosine-1-phosphate receptor agonist KRP-203 attenuates rat autoimmune myocarditis. Biochem. Biophys. Res. Commun. 361, 621-628
90. Kawanabe T, et al. (2007) Sphingosine 1-phosphate accelerates wound healing in diabetic mice. J. Dermatol. Sci. 48,53-60.
91. Maines LW et al. (2008) Suppression of ulcerative colitis in mice by orally available inhibitors of sphingosine kinase. Dig. Dis. Sci. 53, 997-1012.
92. Nishiuma T et al. (2008) Inhalation of sphingosine kinase inhibitor attenuates airway inflammation in asthmatic mouse model. Am. J. Physiol. Lung Cell. Mol. Physiol. 294, L1085-93.
93. Lai WQ et al. (2008) Anti-inflammatory effects of spohingosine kinase moudulation in inflammatory arthritis. J. Immunol. 1, 8010-8017.
94. Snider AJ et al. (2009) A role for sphingosine kinase 1 in dextran sulfate sodium-induced colitis. FASEB J. 23, 143-152.
95. Caballero S et al. (2009) Anti-sphingosine-1-phosphate monoclonal antibodies inhibit angiogenesis and sub-retinal fibrosis in a murine model of laser-induced choroidal neovascularization. Exp. Eye Res. 88, 367-377.
96. Xie B et al. (2009) Blockade of sphingosine-1-phosphate reduces macrophage influx and retinal and choroidal neovascularization. J. Cell. Physiol. 218, 192-198