New players on the center stage: Sphingosine 1-phosphate and its receptors as drug targets

Biochemical Pharmacology

Volumn 75, Issue 10, 2008, Pages 1893-1900

  Huwiler, Andrea ^a   Pfeilschifter, Josef ^b  

^a UNIVERSITY OF BERN   (Switzerland)

^b UNIVERSITY HOSPITAL FRANKFURT   (Germany)

Author keywords

Cancer; Drug therapy; S1P receptors; Sphingolipids; Sphingosine 1 phosphate

Indexed keywords

1 [1,3 DIMETHYL 4 (2 METHYLETHYL) 1H PYRAZOLO[3,4 B]PYRIDIN 6 YL] 4 (3,5 DICHLORO 4 PYRIDINYL)SEMICARBAZIDE; 2 AMINO 2 [2 [ 4 (3 BENZYLOXYPHENYLTHIO) 2 CHLOROPHENYL]ETHYL] 1,3 PROPANEDIOL; 2 UNDECYLTHIAZOLIDINE 4 CARBOXYLIC ACID; 3 [[(3 HEXYLPHENYLCARBAMOYL)METHYL]AMINO]PROPIONIC ACID; 5 (4 PHENYL 5 TRIFLUOROMETHYL 2 THIENYL) 3 (3 TRIFLUOROMETHYLPHENYL) 1,2,4 OXADIAZOLE; BML 241; CONNECTIVE TISSUE GROWTH FACTOR; FINGOLIMOD; G PROTEIN COUPLED RECEPTOR; IMMUNOMODULATING AGENT; JTE 013; KRP 203; NEUTRALIZING ANTIBODY; PHOSPHOLIPASE A; PHOSPHOLIPASE A2; PHOSPHORIC ACID [2 AMINO 2 ( OCTYLPHENYLCARBAMOYL)ETHYL] ESTER; PHOSPHOTRANSFERASE INHIBITOR; SAFINGOL; SPHINGOLIPID; SPHINGOSINE 1 PHOSPHATE; SPHINGOSINE 1 PHOSPHATE ANTIBODY; SPHINGOSINE 1 PHOSPHATE RECEPTOR; SPHINGOSINE KINASE INHIBITOR; VPC 23019; W 123;

ARTICLE; BRADYCARDIA; CANCER CELL; CELL DEATH; CELL GROWTH; CELL SURVIVAL; DRUG RESEARCH; DRUG WITHDRAWAL; GRAFT REJECTION; HUMAN; IMMUNOMODULATION; NONHUMAN; PHOSPHOLIPID METABOLISM; PRIORITY JOURNAL; RETINA MACULA DEGENERATION; SIGNAL TRANSDUCTION;

ANIMALS; HUMANS; LYSOPHOSPHOLIPIDS; OXADIAZOLES; PHOSPHOTRANSFERASES (ALCOHOL GROUP ACCEPTOR); PROPYLENE GLYCOLS; PYRAZOLES; PYRIDINES; RECEPTORS, LYSOSPHINGOLIPID; SPHINGOSINE; SULFHYDRYL COMPOUNDS; THIAZOLIDINES; THIOPHENES;

EID: 42649146192     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2007.12.018     Document Type: Article

References (68)

1. Huwiler A., Kolter T., Pfeilschifter J., and Sandhoff K. Physiology and pathophysiology of sphingolipid metabolism and signaling. Biochim Biophys Acta 1485 (2000) 63-99
2. Spiegel S., and Milstien S. Sphingosine-1-phosphate: an enigmatic signalling lipid. Nat Rev Mol Cell Biol 4 (2003) 397-406
3. Hait N.C., Oskeritzian C.A., Paugh S.W., Milstien S., and Spiegel S. Sphingosine kinases, sphingosine 1-phosphate, apoptosis and diseases. Biochim Biophys Acta 1758 (2006) 2016-2026
4. Le Stunff H., Milstien S., and Spiegel S. Generation and metabolism of bioactive sphingosine-1-phosphate. J Cell Biochem 92 (2004) 882-899
5. Alemany R., van Koppen C.J., Danneberg K., ter Braak M., and Meyer zu Heringdorf D. Regulation and functional roles of sphingosine kinases. Naunyn Schmiedebergs Arch Pharmacol 374 (2007) 413-428
6. Olivera A., and Spiegel S. Sphingosine-1-phosphate as second messenger in cell proliferation induced by PDGF and FCS mitogens. Nature 365 (1993) 557-560
7. Xia P., Gamble J.R., Wang L., Pitson S.M., Moretti P.A., Wattenberg B.W., et al. An oncogenic role of sphingosine kinase. Curr Biol 10 (2000) 1527-1530
8. French K.J., Schrencengost R.S., Lee B.D., Zhuang Y., Smith S.N., Eberly J.L., et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res 63 (2003) 5962-5969
9. French K.J., Upson J.J., Keller S.N., Zhuang Y., Yun J.K., and Smith C.D. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther 318 (2006) 596-603
10. Huwiler A., and Pfeilschifter J. Altering the sphingosine-1-phosphate/ceramide balance: a promising approach for tumor therapy. Curr Pharm Des 12 (2006) 4625-4635
11. Milstien S., and Spiegel S. Targeting sphingosine-1-phosphate: a novel avenue for cancer therapeutics. Cancer Cell 9 (2006) 148-150
12. Huwiler A., and Zangemeister-Wittke U. Targeting the conversion of ceramide to sphingosine 1-phosphate as a novel strategy for cancer therapy. Crit Rev Oncol Hematol 63 (2007) 150-159
13. Brinkmann V., Davis M.D., Heise C.E., Albert R., Cottens S., Hof R., et al. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem 277 (2002) 21453-21457
14. Mandala S., Haidu R., Bergstrom J., Quackenbush E., Xie J., Milligan J., et al. Alteration of lymphocyte trafficking by sphingosine-1-phosphate receptor agonists. Science 296 (2002) 346-349
15. Billich A., Bornancin F., Devay P., Mechtcheriakova D., Urtz N., and Baumruker T. Phosphorylation of the immunomodulatory drug FTY720 by sphingosine kinases. J Biol Chem 278 (2003) 47408-47415
16. Paugh S.W., Payne S.G., Barbour S.E., Milstien S., and Spiegel S. The immunosuppressant FTY720 is phosphorylated by sphingosine kinase type 2. FEBS Lett 554 (2003) 189-193
17. Matloubian M., Lo C.G., Cinamon G., Lesneski M.J., Xu Y., Brinkmann V., et al. Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor. Nature 427 (2004) 355-360
18. Chiba K., Matsuyuki H., Maeda Y., and Sugahara K. Role of sphingosine 1-phosphate receptor type 1 in lymphocyte egress from secondary lymphoid tissues and thymus. Cell Mol Immunol 3 (2006) 11-19
19. Pappu R., Schwab S.R., Cornelissen I., Pereira J.P., Regard J.B., Xu Y., et al. Promotion of lymphocyte egress into blood and lymph by distinct sources of sphingosine-1-phosphate. Science 316 (2007) 295-298
20. Gräler M.H., and Goetzl E.J. The immunosuppressant FTY720 down-regulates sphingosine 1-phosphate G-protein-coupled receptors. FASEB J 18 (2004) 551-553
21. Wang J.D., Takahara S., Nonomura N., Ichimaru N., Toki K., Azuma H., et al. Early induction of apoptosis in androgen-independent prostate cancer cell line by FTY720 requires caspase-3 activation. Prostate 40 (1999) 50-55
22. Azuma H., Takahara S., Ichimaru N., Wang J.D., Itoh Y., Otsuki Y., et al. Marked prevention of tumor growth and metastasis by a novel immunosuppressive agent, FTY720, in mouse breast cancer models. Cancer Res 62 (2002) 1410-1419
23. Ho J.W., Man K., Sun C.K., Lee T.K., Poon R.T., and Fan S.T. Effects of a novel immunomodulating agent, FTY720, on tumor growth and angiogenesis in hepatocellular carcinoma. Mol Cancer Ther 4 (2005) 1430-1438
24. Ubai T., Azuma H., Kotake Y., Inamoto T., Takahara K., Ito Y., et al. FTY720 induced Bcl-associated and Fas-independent apoptosis in human renal cancer cells in vitro and significantly reduced in vivo tumor growth in mouse xenograft. Anticancer Res 27 (2007) 75-88
25. Shen Y., Cai M., Xia W., Liu J., Zhang Q., Xie H., et al. FTY720, a synthetic compound from Isaria sinclairii, inhibits proliferation and induces apoptosis in pancreatic cancer cells. Cancer Lett 254 (2007) 288-297
26. Matsuoka Y., Nagahara Y., Ikekita M., and Shinomiya T. A novel immunosuppressive agent FTY720 induced Akt dephosphorylation in leukemia cells. Br J Pharmacol 138 (2003) 1303-1312
27. Neviani P., Santhanam R., Oaks J.J., Eiring A.M., Notari M., Blaser B.W., et al. FTY720, a new alternative for treating blast crisis chronic myelogenous leukemia and Philadelphia chromosome-positive acute lymphocytic leukemia. J Clin Invest 117 (2007) 2408-2421
28. Liu Q., Zhao X., Frissora F., Ma Y., Santhanam R., Jarjoura D., et al. FTY720 demonstrates promising pre-clinical activity for chronic lymphocytic leukemia and lymphoblastic leukemia/lymphoma. Blood 111 (2008) 275-284
29. Lee T.K., Man K., Ho J.W., Sun C.K., Ng K.T., Wang X.H., et al. FTY720 induces apoptosis of human hepatoma cell lines through PI3-K-mediated Akt dephosphorylation. Carcinogenesis 25 (2004) 2397-2405
30. Brinkmann V., Cyster J.G., and Hla T. FTY720: sphingosine 1-phosphate receptor-1 in the control of lymphocyte egress and endothelial barrier function. Am J Transplant 4 (2004) 1019-1025
31. LaMontagne K., Littlewood-Evans A., Schnell C., O'Reilly T., Wyder L., Sanchez T., et al. Antagonism of sphingosine-1-phosphate receptors by FTY720 inhibits angiogenesis and tumor vascularization. Cancer Res 66 (2006) 221-231
32. Budde K., Schmouder R.L., Brunkhorst R., Nashan B., Lucker P.W., Mayer T., et al. First human trial of FTY720, a novel immunomodulator, in stable renal transplant patients. J Am Soc Nephrol 13 (2002) 1073-1083
33. Sanna M.G., Liao J., Jo E., Alfonso C., Ahn M.Y., Peterson M.S., et al. Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem 279 (2004) 13839-13848
34. Koyrakh L., Roman M.L., Brinkmann V., and Wickman K. The heart rate decrease caused by acute FTY720 administration is mediated by the G protein-gated potassium channel I. Am J Transplant 5 (2005) 529-536
35. Michels S., Schmidt-Erfurth U., and Rosenfeld P.J. Promising new treatments for neovascular age-related macular degeneration. Expert Opin Investig Drugs 15 (2006) 779-793
36. Panetti T.S. Differential effects of sphingosine 1-phosphate and lysophosphatidic acid on endothelial cells. Biochim Biophys Acta 1582 (2002) 190-196
37. Schmid G., Guba M., Ischenko I., Papyan A., Joka M., Schrepfer S., et al. The immunosuppressant FTY720 inhibits angiogenesis via the sphingosine 1-phosphate receptor 1. J Cell Biochem 101 (2007) 259-270
38. 2 expression in renal mesangial cells by a transcriptional mechanism. Br J Pharmacol 150 (2007) 943-950
39. Xin C., Ren S., Eberhardt W., Pfeilschifter J., and Huwiler A. The immunomodulator FTY720 and its phosphorylated derivative activate the Smad signalling cascade and upregulate connective tissue growth factor and collagen type IV expression in renal mesangial cells. Br J Pharmacol 147 (2006) 164-174
40. Keller C.D., Rivera Gil P., Tolle M., van der Giet M., Chun J., Radeke H.H., et al. Immunomodulator FTY720 induces myofibroblast differentiation via the lysophospholipid receptor S1P3 and Smad3 signaling. Am J Pathol 170 (2007) 281-292
41. Payne S.G., Oskeritzian C.A., Griffiths R., Subramanian P., Barbour S.E., Chalfant C.E., et al. The immunosuppressant drug FTY720 inhibits cytosolic phospholipase A2 independently of sphingosine-1-phosphate receptors. Blood 109 (2007) 1077-1085
42. Paugh S.W., Cassidy M.P., He H., Milstien S., Sim-Selley L.J., Spiegel S., et al. its analog, the immunosuppressant 2-amino-2-(2-[4-octylphenyl]ethyl)-1,3-propanediol, interact with the CB1 cannabinoid receptor. Mol Pharmacol 70 (2006) 41-50
43. Shimizu H., Takahashi M., Kaneko T., Murakami T., Hakamata Y., Kudou S., et al. KRP-203, a novel synthetic immunosuppressant, prolongs graft survival and attenuates chronic rejection in rat skin and heart allografts. Circulation 111 (2005) 222-229
44. Fujishiro J., Kudou S., Iwai S., Takahashi M., Hakamata Y., Kinoshita M., et al. 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 (2006) 804-812
45. Fujishiro J., Suzuki C., Kudou S., Yasue T., Hakamata Y., Takahashi M., et al. Change from cyclosporine to combination therapy of mycophenolic acid with the new sphingosine-1-phosphate receptor agonist, KRP-203, prevents host nephrotoxicity and transplant vasculopathy in rats. J Heart Lung Transplant 25 (2006) 825-833
46. Ogawa R., Takahashi M., Hirose S., Morimoto H., Ise H., Murakami T., et al. A novel sphingosine-1-phosphate receptor agonist KRP-203 attenuates rat autoimmune myocarditis. Biochem Biophys Res Commun 361 (2007) 621-628
47. Song J., Matsuda C., Kai Y., Nishida T., Nakajima K., Mizushima T., et al. A novel sphingosine 1-phosphate receptor agonist, KRP-203, regulates chronic colitis in IL-10 gene-deficient mice. J Pharmacol Exp Ther 324 (2008) 276-283
48. Jo E., Sanna M.G., Gonzalez-Cabrera P.J., Thangada S., Tigyi G., Osborne D.A., et al. S1P1-selective in vivo-active agonist from high throughput screening: off-the-shelf chemical probes of receptor interactions, signaling and fate. Chem Biol 12 (2005) 703-715
49. Wei S.H., Rosen H., Matheu M.P., Sanna M.G., Wang S.K., Jo E., et al. Cahalan MD. Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses. Nat Immunol 6 (2005) 1228-1235
50. Lien Y.H., Yong K.C., Cho C., Igarashi S., and Lai L.W. S1P1-selective agonist, SEW2871, ameliorates ischemic acute renal failure. Kidney Int 69 (2006) 1601-1608
51. Whetzel A.M., Bolick D.T., Srinivasan S., Macdonald T.L., Morris M.A., Ley K., et al. Sphingosine-1 phosphate prevents monocyte/endothelial interactions in type 1 diabetic NOD mice through activation of the S1P1 receptor. Circ Res 99 (2006) 731-739
52. Davis M.D., Clemens J.J., Macdonald T.L., and Lynch K.R. Sphingosine 1-phosphate analogs as receptor antagonists. J Biol Chem 280 (2005) 9833-9841
53. Balthasar S., Samulin J., Ahlgren H., Bergelin N., Lundquist M., Toescu E.C., et al. Sphingosine 1-phosphate receptor expression profile and regulation of migration in human thyroid cancer cells. Biochem J 398 (2006) 547-556
54. Osada M., Yatomi Y., Ohmori T., Ikeda H., and Ozaki Y. Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist. Biochem Biophys Res Commun 299 (2002) 483-487
55. Young N., and van Brocklyn J.R. Roles of sphingosine-1-phosphate (S1P) receptors in malignant behavior of glioma cells. Differential effects of S1P2 on cell migration and invasiveness. Exp Cell Res 313 (2007) 1615-1627
56. Allende M.L., Yamashita T., and Proia R.L. G-protein-coupled receptor S1P1 acts within endothelial cells to regulate vascular maturation. Blood 102 (2003) 3665-3667
57. Waeber C., Blondeau N., and Salomone S. Vascular sphingosine-1-phosphate S1P1 and S1P3 receptors. Drug News Perspect 17 (2004) 365-382
58. Inoki I., Takuwa N., Sugimoto N., Yoshioka K., Takata S., Kaneko S., et al. Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor. Biochem Biophys Res Commun 346 (2006) 293-300
59. Sanchez T., Skoura A., Wu M.T., casserly B., Harrington E.O., and Hla T. Induction of vascular permeability by the sphingosine-1-phosphate receptor-2 (S1P2R) and its downstream effectors ROCK and PTEN. Arterioscler Thromb Vasc Biol 27 (2007) 1312-1318
60. Kawanabe T., Kawakami T., Yatomi Y., Shimada S., and Soma Y. Sphingosine 1-phosphate accelerates wound healing in diabetic mice. J Dermatol Sci 48 (2007) 53-60
61. Skoura A., Sanchez T., Claffey K., Mandala S.M., Proia R.L., and Hla T. Essential role of sphingosine 1-phosphate receptor 2 in pathological angiogenesis of the mouse retina. J Clin Invest 117 (2007) 2506-2516
62. Kono M., Mi Y., Liu Y., Sasaki T., Allende M.L., Wu Y.P., et al. The sphingosine-1-phosphate receptors S1P1, S1P2, and S1P3 function coordinately during embryonic angiogenesis. J Biol Chem 279 (2004) 29367-29373
63. Kono M., Belyantseva I.A., Skoura A., Frolenkov G.I., Starost M.F., Dreier J.L., et al. Deafness and stria vascularis defects in S1P2 receptor-null mice. J Biol Chem 282 (2007) 10690-10696
64. Koide Y., Hasegawa T., Takahasji A., Endo A., Mochizuki N., Nakagawa M., et al. Development of novel EDG3 antagonists using a 3D database search and their structure-activity relationships. J Med Chem 45 (2002) 4629-4638
65. Jongsma M., Hendriks-Balk M.C., Michel M.C., Peters S.L., and Alewijnse A.E. BML-241 fails to display selective antagonism at the sphingosine-1-phosphate receptor, S1P(3). Br J Pharmacol 149 (2006) 277-282
66. Visentin B., Vekich J.A., Sibbald B.J., Cavalli A.L., Moreno K.M., Matteo R.G., et al. Validation of an anti-sphingosine-1-phosphate antibody as a potential therapeutic in reducing growth, invasion, and angiogenesis in multiple tumor lineages. Cancer Cell 9 (2006) 225-238
67. Schwartz G.K., Ward D., Saltz L., Casper E.S., Spiess T., Mullen E., et al. A pilot clinical/pharmacological study of the protein kinase C-specific inhibitor safingol alone and in combination with doxorubicin. Clin Cancer Res 3 (1997) 537-543
68. Leroux M.E., Auzenne E., Evans R., Hail Jr. N., Spohn W., Ghosh S.C., et al. Sphingolipids and the sphingosine kinase inhibitor, SKI II, induce BCL-2-independent apoptosis in human prostatic adenocarcinoma cells. Prostate 67 (2007) 1699-1717