Skip to main content Accessibility help
×
Hostname: page-component-cd9895bd7-dk4vv Total loading time: 0 Render date: 2024-12-22T17:08:02.074Z Has data issue: false hasContentIssue false

17 - S1P receptor agonists, a novel generation of immunosuppressants

from PART V - PHYSIOLOGICAL FUNCTIONS AND DRUG TARGETING OF GPCRS

Published online by Cambridge University Press:  05 June 2012

Rosa López Almagro
Affiliation:
Almirall, Barcelona
Gema Tarrasón
Affiliation:
Almirall, Barcelona
Nuria Godessart
Affiliation:
Almirall Laboratories, Llobregat
Sandra Siehler
Affiliation:
Novartis Institute for Biomedical Research
Graeme Milligan
Affiliation:
University of Glasgow
Get access

Summary

Image of the first page of this content. For PDF version, please use the ‘Save PDF’ preceeding this image.'
Type
Chapter
Information
G Protein-Coupled Receptors
Structure, Signaling, and Physiology
, pp. 380 - 397
Publisher: Cambridge University Press
Print publication year: 2010

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)

References

Pyne, Set al. (2000) Sphingosine 1-phosphate signalling in mammalian cells. Biochem J, 349 (2), 385–402.CrossRefGoogle ScholarPubMed
Pitson, SMet al. (2000) Human sphingosine kinase: Purification, molecular cloning and characterization of the native and recombinant enzymes. Biochemistry Journal, 350 (2), 429–441.CrossRefGoogle ScholarPubMed
Zhou, Jet al. (1998) Identification of the first mammalian sphingosine phosphate lyase gene and its functional expression in yeast. Biophys. Res. Commun. 242, 502–507.CrossRefGoogle ScholarPubMed
Cuvillier, Oet al. (1996) Supression of ceramide-mediated programmed cell death by sphingosine-1-phosphate. Nature, 381, 800–803.CrossRefGoogle Scholar
Alvarez, SEet al. (2007) Autocrine and paracrine roles of sphingosine-1-phosphate. Trends Endocrinol. Metab., 18¸300–307.CrossRefGoogle ScholarPubMed
Maceyka, Met al. (2005) Sphk1 and Sphk2: Sphingosine kinase isoenzymes with opposing functions in sphingolipid metabolism. J. Biol. Chem., 280, 37118–37129.CrossRefGoogle ScholarPubMed
Stunff, Het 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.CrossRefGoogle ScholarPubMed
Mizugishi, Ket al. (2005) Essential role for sphingosine kinases in neural and vascular development. Mol. Cell Biol., 25, 11113–11121.CrossRefGoogle ScholarPubMed
Xia, Pet al. (2000) An oncogenic role of sphingosine kinase. Curr. Biol. 10, 1527–1530.CrossRefGoogle ScholarPubMed
Pappu, Ret al (2007) Promotion of lymphocyte egress into blood and lymph by distinct sources of sphingosine-1-phosphate. Science, 316, 295–298.CrossRefGoogle ScholarPubMed
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.CrossRefGoogle ScholarPubMed
Yatomi, Yet 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.CrossRefGoogle ScholarPubMed
Hanel, Pet al. (2007) Erythrocytes store and release sphingosine 1-phosphate in blood. FASEB J., 21, 1202–1209.CrossRefGoogle ScholarPubMed
Kihara, Aet al. (2008) Production and release of sphingosine-1-phosphate and the phosphorylated form of the immunomodulator FTY720. Biochim. Biophys. Acta, 1781, 496–502.CrossRefGoogle ScholarPubMed
Ventakaraman, Ket al. (2008) Vascular endothelium as a contributor of plasma sphingosine 1-phosphate. Circ. Res., 102, 669–676.CrossRefGoogle Scholar
Olivera, Aet 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.CrossRefGoogle ScholarPubMed
Mitra, Pet al. (2006) Role of ABCC1 in export of sphingosine-1-phosphate from mast cells. Proc. Natl. Acad. Sci. U.S.A., 103, 16394–16399.CrossRefGoogle ScholarPubMed
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.CrossRefGoogle Scholar
Lee, YMet al. (2007) A novel method to quantify sphingosine 1-phosphate by immobilized metal affinity chromatography (IMAC). ProstaglandinsOther Lipid Mediat., 84, 154–162.CrossRefGoogle Scholar
Romiti, Eet al (2000) Neutral/alkaline and acid ceramidase activities are activily released by murine endothelial cells. Biochem. Biophys. Res. Commun., 275, 476–751.CrossRefGoogle Scholar
Tabas, I (1999) Secretory sphingomyelinase. Chem. Phys. Lipids, 102, 123–130.CrossRefGoogle ScholarPubMed
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.CrossRefGoogle ScholarPubMed
Brocklyn, JRet al. (1998) Dual actions of sphingosine-1-phosphate: extracellular through the Gi- coupled receptor Edg-1 and intracellular to regulate proliferation and survival. J. Cell Biol., 142(1), 229–240.CrossRefGoogle ScholarPubMed
Kariya, Yet al. (2005) Products by the sphingosine kinase/sphingosine-1-phosphate (S1P) lyase pathway but not S1P stimulate mitogenesis. Genes Cells, 10 (6), 605–615.CrossRefGoogle Scholar
Hla, Tet al. (1990) An abundant transcript induced in differentiating human endothelial cells encodes a polypeptide with structural similarities to G-protein-coupled receptors. J. Biol. Chem. 265, 9308–9313.Google ScholarPubMed
Okamoto, Het 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.CrossRefGoogle Scholar
Alderton, Fet 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.CrossRefGoogle Scholar
Liu, Yet al.(2000) Edg-1, the G protein-coupled receptor for sphingosine-1-phosphate, is essential for vascular maturation. J. Clin. Invest. 106, 951–961.CrossRefGoogle Scholar
Allende, MLet al. (2003) G-protein-coupled receptor S1P1 acts within endothelial cells to regulate vascular maturation. Blood 102, 3665–3667.CrossRefGoogle ScholarPubMed
Allende, MLet al. (2004) Expression of the sphingosine-1-phosphate receptor, S1P1, on T cells controls thymic emigration. J. Biol. Chem. 279 (15), 15396–15401.CrossRefGoogle Scholar
Matloubian, Met al. (2004) Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature 427 (6972), 355–360.CrossRefGoogle ScholarPubMed
Chi, Het 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.CrossRefGoogle ScholarPubMed
Kabashima, Ket al. (2006) Plasma cell S1P1 expression determines secondary lymphoid organ retention versus bone marrow tropism. J. Exp. Med. 203(12), 2683–2690.CrossRefGoogle ScholarPubMed
Singleton, PAet 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.CrossRefGoogle ScholarPubMed
Kimura, Aet 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.CrossRefGoogle Scholar
Ishii, Iet 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.CrossRefGoogle Scholar
Ancellin, Net al.(1999) Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5. J. Biol. Chem. 274, 18997–19002.CrossRefGoogle ScholarPubMed
Okamoto, Het 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.CrossRefGoogle ScholarPubMed
Paik, JHet 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.CrossRefGoogle ScholarPubMed
Goparaju, SKet al. (2005) The S1P2 receptor negatively regulates platelet-derived growth factor-induced motility and proliferation. Mol. Cell. Biol. 25(10), 4237–4249.CrossRefGoogle ScholarPubMed
Baudhuin, LMet al. (2004) S1P3-mediated Akt-activation and cross-talk with platelet-derived growth factor receptor (PDGFR). FASEB J. 18(2), 341–343.CrossRefGoogle Scholar
Ishii, Iet 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.CrossRefGoogle Scholar
Kono, Met al.(2004) The sphingosine-1-phosphate receptors S1P1, S1P2, and S1P3 function co-ordinately during embryonic angiogenesis. J. Biol. Chem. 279, 29367–29373.CrossRefGoogle Scholar
MacLennan, AJet al. (2001) An essential role for the H218/AGR16/Edg-5/LP(B2) sphingosine 1-phosphate receptor in neuronal excitability. Eur. J. Neurosci. 14, 203–209.CrossRefGoogle ScholarPubMed
Serriere-Lanneau, Vet al. (2007) The sphingosine 1-phosphate receptor S1P2 triggers hepatic wound healing. FASEB J. 21, 2005–2013.CrossRefGoogle ScholarPubMed
Hu, Wet al. (2006) Lentiviral siRNA silencing of sphingosine-1-phosphate receptors S1P1 and S1P2 in smooth muscle. Biochem. Biophys. Res. Commun. 343, 1038–1044.CrossRefGoogle ScholarPubMed
Sanna, MGet al. (2004) Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J. Biol. Chem. 279, 13839–13848.CrossRefGoogle ScholarPubMed
Theilmeier, Get al. (2006) High-density lipoproteins and their constituent, sphingosine-1-phosphate, directly protect the heart against ischemia/reperfusion injury in vivo via the S1P3 lysophospholipid receptor. Circulation 114, 1403–1409.CrossRefGoogle ScholarPubMed
Gon, Yet 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.CrossRefGoogle ScholarPubMed
Niessen, Fet al. (2008) Dendritic cell PAR1-S1P3 signalling couples coagulation and inflammation. Nature 452, 654–658.CrossRefGoogle ScholarPubMed
Graler, MHet 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.CrossRefGoogle ScholarPubMed
Malek, RLet 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.CrossRefGoogle ScholarPubMed
,Deltagen Inc. 2005: http://www.informatics.jax.org/external/ko/deltagen/302
Jaillard, Cet al. (2005) Edg8/S1P5: an oligodendroglial receptor with dual function on process retraction and cell survival. J. Neurosci. 25, 1459–1469.CrossRefGoogle ScholarPubMed
Novgorodov, ASet al. (2007) Activation of sphingosine-1-phosphate receptor S1P5 inhibits oligodendrocyte progenitor migration. FASEB J. 21, 1503–1514.CrossRefGoogle ScholarPubMed
Walzer, Tet al. (2007) Natural killer cell trafficking in vivo requires a dedicated sphingosine 1-phosphate receptor. Nat. Immunol. 8, 1337–1344.CrossRefGoogle ScholarPubMed
Rivera, Jet al. (2008) The alliance of sphingosine 1-phospahte and its receptors in immunity. Nat. Rev. Immunol. 8, 753–763.CrossRefGoogle Scholar
Cyster, JG. (2007) Specifying the patterns of immune cell migrationNovartis Found. Symp. 281; 54–61CrossRefGoogle ScholarPubMed
Grigorova, ILet al. (2009) Cortical sinus probing, S1P1-dependent entry and flow-based capture of egressing T cells. Nat Immunol.; 10 (1):58–65.CrossRefGoogle ScholarPubMed
Chaffin, KE, and Perlmutter, RM (1991) A pertussis toxin-sensitive process controls thymocyte emigration. Eur J Immunol.; 21(10):2565–73.CrossRefGoogle ScholarPubMed
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):11–9Google ScholarPubMed
Mandala, S.et al (2002) Alteration of lymphocyte trafficking by sphingosine-1-phosphate receptor agonists. Science; 296 (5566):346–9.CrossRefGoogle Scholar
Hla, Tet al. (2008) The vascular S1P gradient: cellular sources and biological significance. Biochim Biophys Acta; 1781(9):477–82.CrossRefGoogle ScholarPubMed
Vachal, Pet al. (2006) Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor. Bioorg Med Chem Lett. ;16(14):3684–7.CrossRefGoogle ScholarPubMed
Schwab, SR and Cyster, JG.(2007) Finding a way out: lymphocyte egress from lymphoid organs. Nat Immunol. 8 (12):1295–301CrossRefGoogle ScholarPubMed
Rosen, H, et al. (2009) Sphingosine 1-phosphate receptor signaling. Annu Rev Biochem; 78:743–68.CrossRefGoogle ScholarPubMed
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.CrossRefGoogle ScholarPubMed
Sanna, Get 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.CrossRefGoogle ScholarPubMed
Oo, MLet 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.CrossRefGoogle ScholarPubMed
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.CrossRefGoogle Scholar
Liao, JJet al. (2007) Cutting edge: alternative signalling of Th17 cell development by sphingosine 21-phosphate. J.Immunol. 178, 5425–5428.CrossRefGoogle Scholar
Huang, MCet 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.CrossRefGoogle Scholar
Piccirillo, CAet al. (2008) CD4+ Foxp3+ regulatory T cells in the control of autoimmunity: in vivo veritas. Curr. Opin. Immunol. 20, 655–662.CrossRefGoogle ScholarPubMed
Liu, Get al. (2009) The receptor SP1 overrides regulatory T cell mediated immune suppression through Akt-mTOR. Nat. Immunol. Jul;10 (7):769–77.CrossRefGoogle Scholar
Huwiler, Aet al. (2008) New players on the center stage: Sphingosine 1-phosphate and its receptors as drug targets. Biochem.Pharmacol. 75: 1893–1900.CrossRefGoogle ScholarPubMed
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; 283–289CrossRefGoogle Scholar
Martini, Set al. (2007) Current perspectives on FTY720. Expert Opin. Invest. Drugs 16, 505–518.CrossRefGoogle ScholarPubMed
O' Connor, Pet al. (2009) Oral fingolimod (FTY720) in multiple sclerosis, Two year results of a phase II extension study. Neurology 72, 73–79.CrossRefGoogle Scholar
Sawicka, Eet 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.CrossRefGoogle ScholarPubMed
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, Düsseldorf, Germany.
Shida, Det al. (2008) Targeting SphK1 as a new strategy against cancer. Curr Drug Targets. ;9(8):662–73.CrossRefGoogle ScholarPubMed
Pappas, C.et al. (2008) LX2931: A Potential Small Molecule Treatment for Autoimmune Disorders. Presentation # 351, American College of Rheumatology meeting.
O' Brien, Net al. (2009) Production and characterization of monoclonal anti-sphingosine-1-phosphate antibodies. J. Lipid Res. 50, 2245–2257.CrossRefGoogle Scholar
Keul, Pet al. (2007) The sphingosine-1-phosphate analogue FTY720 reduces atherosclerosis in apolipoprotein E-deficient mice. Arterioscler. Thromb. Vasc. Biol. 27, 607–613.CrossRefGoogle ScholarPubMed
Idzko, Met al. (2006) Local application of FTY720 to the lung abrogates experimental asthma by altering dendritic cell function. J. Clin. Invest. 116, 2935–2944.CrossRefGoogle ScholarPubMed
Liu, HBet al. (2008) Sphingosine-1-phosphate and its analogue FTY720 diminish acute pulmonary injury in rats with acute necrotizing pancreatitis. Pancreas 36, e10–5.CrossRefGoogle ScholarPubMed
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.CrossRefGoogle ScholarPubMed
Wenderfer, SEet al. (2008) Increased survival and reduced renal injury in MRL/lpr mice treated with a novel sphingosine-1-phosphate receptor agonist. Kidney Int. 74, 1319–1326.CrossRefGoogle ScholarPubMed
Ogawa, Ret al. (2007) A novel sphingosine-1-phosphate receptor agonist KRP-203 attenuates rat autoimmune myocarditis. Biochem. Biophys. Res. Commun. 361, 621–628.CrossRefGoogle ScholarPubMed
Kawanabe, T, et al. (2007) Sphingosine 1-phosphate accelerates wound healing in diabetic mice. J. Dermatol. Sci. 48,53–60.CrossRefGoogle ScholarPubMed
Maines, LWet al. (2008) Suppression of ulcerative colitis in mice by orally available inhibitors of sphingosine kinase. Dig. Dis. Sci. 53, 997–1012.CrossRefGoogle ScholarPubMed
Nishiuma, Tet al. (2008) Inhalation of sphingosine kinase inhibitor attenuates airway inflammation in asthmatic mouse model. Am. J. Physiol. Lung Cell. Mol. Physiol. 294, L1085–93.CrossRefGoogle ScholarPubMed
Lai, WQet al. (2008) Anti-inflammatory effects of spohingosine kinase moudulation in inflammatory arthritis. J. Immunol. 1, 8010–8017.CrossRefGoogle Scholar
Snider, AJet al. (2009) A role for sphingosine kinase 1 in dextran sulfate sodium-induced colitis. FASEB J. 23, 143–152.CrossRefGoogle ScholarPubMed
Caballero, Set 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.CrossRefGoogle Scholar
Xie, Bet al. (2009) Blockade of sphingosine-1-phosphate reduces macrophage influx and retinal and choroidal neovascularization. J. Cell. Physiol. 218, 192–198.CrossRefGoogle ScholarPubMed

Save book to Kindle

To save this book to your Kindle, first ensure no-reply@cambridge.org is added to your Approved Personal Document E-mail List under your Personal Document Settings on the Manage Your Content and Devices page of your Amazon account. Then enter the ‘name’ part of your Kindle email address below. Find out more about saving to your Kindle.

Note you can select to save to either the @free.kindle.com or @kindle.com variations. ‘@free.kindle.com’ emails are free but can only be saved to your device when it is connected to wi-fi. ‘@kindle.com’ emails can be delivered even when you are not connected to wi-fi, but note that service fees apply.

Find out more about the Kindle Personal Document Service.

Available formats
×

Save book to Dropbox

To save content items to your account, please confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your account. Find out more about saving content to Dropbox.

Available formats
×

Save book to Google Drive

To save content items to your account, please confirm that you agree to abide by our usage policies. If this is the first time you use this feature, you will be asked to authorise Cambridge Core to connect with your account. Find out more about saving content to Google Drive.

Available formats
×