propylene glycols

Summary

Summary: Derivatives of propylene glycol (1,2-propanediol). They are used as humectants and solvents in pharmaceutical preparations.

Top Publications

  1. Fowles J, Banton M, Pottenger L. A toxicological review of the propylene glycols. Crit Rev Toxicol. 2013;43:363-90 pubmed publisher
    ..The existing safety evaluations of the FDA, USEPA, NTP and ATSDR for these compounds are consistent and point to the conclusion that the propylene glycols present a very low risk to human health.
  2. Masuko K, Murata M, Beppu M, Nakamura H, Kato T, Yudoh K. Sphingosine-1-phosphate modulates expression of vascular endothelial growth factor in human articular chondrocytes: a possible new role in arthritis. Int J Rheum Dis. 2012;15:366-73 pubmed publisher
    ..Our results suggest that S1P may contribute to the regulation of VEGF expression in human chondrocytes. S1P may therefore play a unique role in the pathophysiology of OA by regulating VEGF expression in chondrocytes. ..
  3. Commodaro A, Pedregosa J, Peron J, Brandão W, Rizzo L, Bueno V. The imbalance between Treg and Th17 cells caused by FTY720 treatment in skin allograft rejection. Clinics (Sao Paulo). 2012;67:805-13 pubmed
    ..To further understand the process of graft rejection/acceptance, we evaluated skin allograft survival and associated events after FTY720 treatment...
  4. Zhao Z, Choi J, Zhao C, Ma Z. FTY720 normalizes hyperglycemia by stimulating ?-cell in vivo regeneration in db/db mice through regulation of cyclin D3 and p57(KIP2). J Biol Chem. 2012;287:5562-73 pubmed publisher
    ..Therapeutic strategies targeting this network may promote in vivo regeneration of ?-cells in patients and prevent and/or cure type 2 diabetes...
  5. Deogracias R, Yazdani M, Dekkers M, Guy J, Ionescu M, Vogt K, et al. Fingolimod, a sphingosine-1 phosphate receptor modulator, increases BDNF levels and improves symptoms of a mouse model of Rett syndrome. Proc Natl Acad Sci U S A. 2012;109:14230-5 pubmed publisher
  6. Liu Y, Deng J, Wang L, Lee H, Armstrong B, Scuto A, et al. S1PR1 is an effective target to block STAT3 signaling in activated B cell-like diffuse large B-cell lymphoma. Blood. 2012;120:1458-65 pubmed publisher
  7. Norimatsu Y, Ohmori T, Kimura A, Madoiwa S, Mimuro J, Seichi A, et al. FTY720 improves functional recovery after spinal cord injury by primarily nonimmunomodulatory mechanisms. Am J Pathol. 2012;180:1625-35 pubmed publisher
    ..Our data highlight the importance of immune-independent functions of FTY720 in decreasing vascular permeability and astrogliosis in the injured spinal cord and promoting locomotor function recovery after SCI...
  8. Li C, Shao Y, Ng K, Liu X, Ling C, Ma Y, et al. FTY720 suppresses liver tumor metastasis by reducing the population of circulating endothelial progenitor cells. PLoS ONE. 2012;7:e32380 pubmed publisher
    ..We aim to investigate the mechanism of FTY720, which was originally applied as an immunomodulator, on suppression of liver tumor metastasis after liver resection and partial hepatic I/R injury...
  9. Kipp M, Amor S. FTY720 on the way from the base camp to the summit of the mountain: relevance for remyelination. Mult Scler. 2012;18:258-63 pubmed publisher
    ..While the mechanisms of action still require firm elucidation, it is clear that FTY720 could also be reparative, extending its therapeutic potential for multiple sclerosis...

More Information

Publications62

  1. Liao A, Hu R, Zhao Q, Li J, Li Y, Yao K, et al. Autophagy induced by FTY720 promotes apoptosis in U266 cells. Eur J Pharm Sci. 2012;45:600-5 pubmed publisher
    ..Furthermore, activation of reactive oxygen species (ROS) regulates FTY720 induced apoptosis and autophagy in U266 cells. The study implicated that FTY720 could be a good candidate for MM treatment...
  2. Horga A, Castilló J, Montalban X. Fingolimod for relapsing multiple sclerosis: an update. Expert Opin Pharmacother. 2010;11:1183-96 pubmed publisher
    ..Fingolimod is an oral sphingosine-1-phosphase (S1P) receptor modulator under clinical investigation for the treatment of relapsing-remitting and primary progressive MS...
  3. Liu Q, Alinari L, Chen C, Yan F, Dalton J, Lapalombella R, et al. FTY720 shows promising in vitro and in vivo preclinical activity by downmodulating Cyclin D1 and phospho-Akt in mantle cell lymphoma. Clin Cancer Res. 2010;16:3182-92 pubmed publisher
    ..Because of the absence of curative therapy for MCL, we explored FTY720 as a novel agent against MCL...
  4. Comi G, O CONNOR P, Montalban X, Antel J, Radue E, Karlsson G, et al. Phase II study of oral fingolimod (FTY720) in multiple sclerosis: 3-year results. Mult Scler. 2010;16:197-207 pubmed publisher
    ..The efficacy and safety of oral fingolimod are being further evaluated in a large phase III MS study programme...
  5. Liu H, Xu Y, Zheng Z, Liu D. 1,3-Propanediol and its copolymers: research, development and industrialization. Biotechnol J. 2010;5:1137-48 pubmed publisher
  6. Murakami A, Takasugi H, Ohnuma S, Koide Y, Sakurai A, Takeda S, et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol Pharmacol. 2010;77:704-13 pubmed publisher
  7. Cohen J, Barkhof F, Comi G, Hartung H, Khatri B, Montalban X, et al. Oral fingolimod or intramuscular interferon for relapsing multiple sclerosis. N Engl J Med. 2010;362:402-15 pubmed publisher
    ..Fingolimod (FTY720), a sphingosine-1-phosphate-receptor modulator that prevents lymphocyte egress from lymph nodes, showed clinical efficacy and improvement on imaging in a phase 2 study involving patients with multiple sclerosis...
  8. Finney C, Hawkes C, Kain D, Dhabangi A, Musoke C, Cserti Gazdewich C, et al. S1P is associated with protection in human and experimental cerebral malaria. Mol Med. 2011;17:717-25 pubmed publisher
    ..These findings implicate dysregulation of the S1P pathway in the pathogenesis of human and murine CM and suggest a novel therapeutic strategy to improve clinical outcome in severe malaria. ..
  9. Miron V, Ludwin S, Darlington P, Jarjour A, Soliven B, Kennedy T, et al. Fingolimod (FTY720) enhances remyelination following demyelination of organotypic cerebellar slices. Am J Pathol. 2010;176:2682-94 pubmed publisher
  10. Wei Y, Yemisci M, Kim H, Yung L, Shin H, Hwang S, et al. Fingolimod provides long-term protection in rodent models of cerebral ischemia. Ann Neurol. 2011;69:119-29 pubmed publisher
  11. Nagaoka Y, Otsuki K, Fujita T, Uesato S. Effects of phosphorylation of immunomodulatory agent FTY720 (fingolimod) on antiproliferative activity against breast and colon cancer cells. Biol Pharm Bull. 2008;31:1177-81 pubmed
    ..These results indicate that the antiproliferative activity of FTY720 does not result from its phosphorylation, either endogenous or exogenous...
  12. Berdyshev E, Gorshkova I, Skobeleva A, Bittman R, Lu X, Dudek S, et al. FTY720 inhibits ceramide synthases and up-regulates dihydrosphingosine 1-phosphate formation in human lung endothelial cells. J Biol Chem. 2009;284:5467-77 pubmed publisher
    ..These findings open a novel direction for therapeutic applications of FTY720 that focuses on inhibition of ceramide biosynthesis, ceramide-dependent signaling, and the up-regulation of DHS1P generation in cells...
  13. Chun J, Brinkmann V. A mechanistically novel, first oral therapy for multiple sclerosis: the development of fingolimod (FTY720, Gilenya). Discov Med. 2011;12:213-28 pubmed
    ..This duality may herald a paradigm shift in the treatment of MS and other neurological disorders...
  14. Mullershausen F, Zécri F, Cetin C, Billich A, Guerini D, Seuwen K. Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors. Nat Chem Biol. 2009;5:428-34 pubmed publisher
    ..We show that persistent signaling translates into an increased chemokinetic migration of primary human umbilical vein endothelial cells, which suggests persistent agonism as a crucial parameter in the mechanism of action of FTY720...
  15. Kappos L, Radue E, O Connor P, Polman C, Hohlfeld R, Calabresi P, et al. A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis. N Engl J Med. 2010;362:387-401 pubmed publisher
  16. Lu X, Sun C, Valentine W, Shuyu E, Liu J, Tigyi G, et al. Chiral vinylphosphonate and phosphonate analogues of the immunosuppressive agent FTY720. J Org Chem. 2009;74:3192-5 pubmed publisher
    ..S)-5 failed to activate the sphingosine 1-phosphate type 1 (S1P(1)) receptor...
  17. Durafourt B, Lambert C, Johnson T, Blain M, Bar Or A, Antel J. Differential responses of human microglia and blood-derived myeloid cells to FTY720. J Neuroimmunol. 2011;230:10-6 pubmed publisher
    ..Despite similar receptor expression patterns, the distinct myeloid cell populations present in the human CNS, under steady-state or inflammatory conditions, exhibit differential responses to FTY720...
  18. Roberts K, Smith A, McDougall F, Carpenter H, Horan M, Neviani P, et al. Essential requirement for PP2A inhibition by the oncogenic receptor c-KIT suggests PP2A reactivation as a strategy to treat c-KIT+ cancers. Cancer Res. 2010;70:5438-47 pubmed publisher
    ..Our findings show that PP2A inhibition is essential for c-KIT-mediated tumorigenesis, and that reactivating PP2A may offer an attractive strategy to treat drug-resistant c-KIT(+) cancers...
  19. Sakaguchi N, Kojima C, Harada A, Kono K. Preparation of pH-sensitive poly(glycidol) derivatives with varying hydrophobicities: their ability to sensitize stable liposomes to pH. Bioconjug Chem. 2008;19:1040-8 pubmed publisher
    ..As a result, modification with appropriate hydrophobicity, MGluPG, produced highly potent pH-sensitive liposomes, which might be useful for efficient cytoplasmic delivery of bioactive molecules, such as proteins and genes...
  20. Lopes C, Gallo A, Palma P, Cury P, Bueno V. Skin allograft survival and analysis of renal parameters after FTY720 + tacrolimus treatment in mice. Transplant Proc. 2008;40:856-60 pubmed publisher
    ..FTY720 associated with FK506 caused fewer changes in kidney structure, and blood glucose levels were lower than in FK506 monotherapy...
  21. Lopes C, Rosin F, Cordeiro J, Bueno V. Cell phenotype evaluation at various sites after skin transplantation and FTY720 plus sirolimus therapy. Transplant Proc. 2010;42:573-7 pubmed publisher
  22. Angyal A, Egelston C, Kobezda T, Olasz K, Laszlo A, Glant T, et al. Development of proteoglycan-induced arthritis depends on T cell-supported autoantibody production, but does not involve significant influx of T cells into the joints. Arthritis Res Ther. 2010;12:R44 pubmed publisher
    ..Herein, we investigated the role of joint-homing versus lymphoid organ-homing T cells in the development of proteoglycan-induced arthritis (PGIA), an autoimmune model of RA...
  23. Commodaro A, Peron J, Lopes C, Arslanian C, Belfort R, Rizzo L, et al. Evaluation of experimental autoimmune uveitis in mice treated with FTY720. Invest Ophthalmol Vis Sci. 2010;51:2568-74 pubmed publisher
    ..In this study, the action of FTY720 in the ocular autoimmune model in mice was investigated...
  24. Jenne C, Enders A, Rivera R, Watson S, Bankovich A, Pereira J, et al. T-bet-dependent S1P5 expression in NK cells promotes egress from lymph nodes and bone marrow. J Exp Med. 2009;206:2469-81 pubmed publisher
    ..In summary, these findings identify S1P5 as a T-bet-induced gene that is required for NK cell egress from LNs and BM...
  25. Wolf A, Eller K, Zeiser R, Dürr C, Gerlach U, Sixt M, et al. The sphingosine 1-phosphate receptor agonist FTY720 potently inhibits regulatory T cell proliferation in vitro and in vivo. J Immunol. 2009;183:3751-60 pubmed publisher
  26. Pedregosa J, Haidar A, Hirata A, Franco M, Gomes G, Bueno V. TLR2 and TLR4 expression after kidney ischemia and reperfusion injury in mice treated with FTY720. Int Immunopharmacol. 2011;11:1311-8 pubmed publisher
    ..Further studies are needed in order to establish whether TLR2 and TLR4 down regulation should be therapeutically addressed as protective targets of renal function and structure after IR...
  27. Liao A, Broeg K, Fox T, Tan S, Watters R, Shah M, et al. Therapeutic efficacy of FTY720 in a rat model of NK-cell leukemia. Blood. 2011;118:2793-800 pubmed publisher
    ..These data demonstrate that therapeutic benefit of FTY720 may result from both altered sphingolipid metabolism as well as enhanced degradation of a key component of survival signaling...
  28. Pyne S, Bittman R, Pyne N. Sphingosine kinase inhibitors and cancer: seeking the golden sword of Hercules. Cancer Res. 2011;71:6576-82 pubmed publisher
    ..Herein, we provide a perspective about these recent developments and highlight the importance of translating basic pharmacologic and biochemical findings on sphingosine kinase into new drug discovery programs for treatment of cancer...
  29. Pugach M, Strother J, Darling C, Fried D, Gansky S, Marshall S, et al. Dentin caries zones: mineral, structure, and properties. J Dent Res. 2009;88:71-6 pubmed publisher
    ..5 [10.6-25.3] GPa to 1.6 [0.0-5.0] GPa and from 42.9 [39.8-44.6] vol% to 12.4 [9.1-14.2] vol%, respectively. Even the most demineralized pink zone contained considerable residual mineral...
  30. O CONNOR P, Comi G, Montalban X, Antel J, Radue E, De Vera A, et al. Oral fingolimod (FTY720) in multiple sclerosis: two-year results of a phase II extension study. Neurology. 2009;72:73-9 pubmed publisher
    ..To report the results of a 24-month extension of a phase II trial assessing the efficacy, safety, and tolerability of the once-daily oral sphingosine-1-phosphate receptor modulator, fingolimod (FTY720), in relapsing multiple sclerosis (MS)...
  31. Choi J, Gardell S, Herr D, Rivera R, Lee C, Noguchi K, 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 U S A. 2011;108:751-6 pubmed publisher
    ..These data identify nonimmunological CNS mechanisms of FTY720 efficacy and implicate S1P signaling pathways within the CNS as targets for multiple sclerosis therapies...
  32. Saxena R, Anand P, Saran S, Isar J. Microbial production of 1,3-propanediol: Recent developments and emerging opportunities. Biotechnol Adv. 2009;27:895-913 pubmed publisher
    ..The future prospect of 1,3-propanediol and its potential as a major bulk chemical are discussed under the light of the current research...
  33. Mansoor M, Melendez A. Recent trials for FTY720 (fingolimod): a new generation of immunomodulators structurally similar to sphingosine. Rev Recent Clin Trials. 2008;3:62-9 pubmed
    ..In this review, we focus on the transition of this novel compound from bench to clinical trials, and discuss the clinical potential of this drug in autoimmune diseases and in transplantation immunology...
  34. Moench T, Mumper R, Hoen T, Sun M, Cone R. Microbicide excipients can greatly increase susceptibility to genital herpes transmission in the mouse. BMC Infect Dis. 2010;10:331 pubmed publisher
    ..However, excipients have not previously been tested in susceptibility models...
  35. Sensken S, Bode C, Gräler M. Accumulation of fingolimod (FTY720) in lymphoid tissues contributes to prolonged efficacy. J Pharmacol Exp Ther. 2009;328:963-9 pubmed publisher
    ..Therefore, we conclude that cellular accumulation of FTY720 generates a reservoir in thymus and SLOs, leading to sustained FTY-P production and activation of S1P(1) within tissues...
  36. Hla T, Brinkmann V. Sphingosine 1-phosphate (S1P): Physiology and the effects of S1P receptor modulation. Neurology. 2011;76:S3-8 pubmed publisher
    ..This review highlights the normal physiologic processes modulated by S1P and S1PRs, and the therapeutic effects of S1PR modulation in the immune, central nervous, and cardiovascular systems...
  37. Sinha R, Park C, Hwang I, Davis M, Kehrl J. B lymphocytes exit lymph nodes through cortical lymphatic sinusoids by a mechanism independent of sphingosine-1-phosphate-mediated chemotaxis. Immunity. 2009;30:434-46 pubmed publisher
    ..This study identifies a major site of B lymphocyte lymph node egress, shows that FTY720 treatment blocks passage through the cortical lymphatic endothelium, and argues against a functional role for S1P chemotaxis in B lymphocyte egress. ..
  38. Yamanaka M, Anada Y, Igarashi Y, Kihara A. A splicing isoform of LPP1, LPP1a, exhibits high phosphatase activity toward FTY720 phosphate. Biochem Biophys Res Commun. 2008;375:675-9 pubmed publisher
    ..Significant levels of LPP1a expression were found in endothelial cells, suggesting that LPP1a is important for the dephosphorylation of FTY720-P in plasma...
  39. Khatri B, Barkhof F, Comi G, Hartung H, Kappos L, Montalban X, et al. Comparison of fingolimod with interferon beta-1a in relapsing-remitting multiple sclerosis: a randomised extension of the TRANSFORMS study. Lancet Neurol. 2011;10:520-9 pubmed publisher
  40. Keul P, Lucke S, von Wnuck Lipinski K, Bode C, Graler M, Heusch G, et al. Sphingosine-1-phosphate receptor 3 promotes recruitment of monocyte/macrophages in inflammation and atherosclerosis. Circ Res. 2011;108:314-23 pubmed publisher
    ..The role of sphingosine-1-phosphate (S1P) and its receptors in the pathogenesis of atherosclerosis has not been investigated...
  41. Gasperini C, Cefaro L, Borriello G, Tosto G, Prosperini L, Pozzilli C. Emerging oral drugs for multiple sclerosis. Expert Opin Emerg Drugs. 2008;13:465-77 pubmed
  42. Zeng A, Sabra W. Microbial production of diols as platform chemicals: recent progresses. Curr Opin Biotechnol. 2011;22:749-57 pubmed publisher
    ..We review and discuss here the recent development in the microbial production of these diols, especially regarding the engineering of production strains and optimization of the fermentation processes...
  43. Brinkmann V. FTY720 (fingolimod) in Multiple Sclerosis: therapeutic effects in the immune and the central nervous system. Br J Pharmacol. 2009;158:1173-82 pubmed publisher
    ..Differential effects of the drug on the trafficking of naïve, central memory and effector memory T cell subsets are discussed...
  44. Jin J, Yang S, Park J, Lee C, Lee J, Kim S, et al. Fragile maintenance of allograft tolerance induced by lymphocyte sequestration and co-stimulation blockade. Transpl Immunol. 2009;21:221-7 pubmed publisher
    ..Our data indicate that the combination treatment provides effective tool for the induction of long-term graft survival, and the maintenance of allograft in proper function is an actively regulated process...
  45. Pchejetski D, Bohler T, Brizuela L, Sauer L, Doumerc N, Golzio M, et al. FTY720 (fingolimod) sensitizes prostate cancer cells to radiotherapy by inhibition of sphingosine kinase-1. Cancer Res. 2010;70:8651-61 pubmed publisher
    ..Our findings suggest that low, well-tolerated doses of FTY720 could offer significant improvement to the clinical treatment of prostate cancer...
  46. Ishii M, Egen J, Klauschen F, Meier Schellersheim M, Saeki Y, Vacher J, et al. Sphingosine-1-phosphate mobilizes osteoclast precursors and regulates bone homeostasis. Nature. 2009;458:524-8 pubmed publisher
  47. Tsunemi S, Iwasaki T, Kitano S, Imado T, Miyazawa K, Sano H. Effects of the novel immunosuppressant FTY720 in a murine rheumatoid arthritis model. Clin Immunol. 2010;136:197-204 pubmed publisher
    ..These results indicate that FTY can inhibit arthritis in SKG mice via sequestration of autoimmune CD4(+) T cells in the thymus, enhancement of Th2 immune responses, and inhibition of PGE(2) production by synovial cells...
  48. Hasegawa Y, Suzuki H, Sozen T, Rolland W, Zhang J. Activation of sphingosine 1-phosphate receptor-1 by FTY720 is neuroprotective after ischemic stroke in rats. Stroke. 2010;41:368-74 pubmed publisher
    ..FTY720 is a known sphingosine 1-phosphate receptor agonist. In the present study, we investigated the neuroprotective effect of postischemic administration of FTY720 in rats with 2 hours transient middle cerebral artery occlusion (MCAO)...
  49. Papadopoulos D, Rundle J, Patel R, Marshall I, Stretton J, Eaton R, et al. FTY720 ameliorates MOG-induced experimental autoimmune encephalomyelitis by suppressing both cellular and humoral immune responses. J Neurosci Res. 2010;88:346-59 pubmed publisher
    ..In conclusion, our findings indicate that FTY720-mediated S1P receptor modulation ameliorates chronic relapsing MOG-EAE by suppressing both cellular and humoral immune responses...
  50. Mehling M, Hilbert P, Fritz S, Durovic B, Eichin D, Gasser O, et al. Antigen-specific adaptive immune responses in fingolimod-treated multiple sclerosis patients. Ann Neurol. 2011;69:408-13 pubmed publisher
    ..These results indicate that fingolimod-treated individuals can mount vaccine-specific adaptive immune responses comparable to healthy controls...
  51. Takabe K, Paugh S, Milstien S, Spiegel S. "Inside-out" signaling of sphingosine-1-phosphate: therapeutic targets. Pharmacol Rev. 2008;60:181-95 pubmed publisher
  52. Hofmann U, Burkard N, Vogt C, Thoma A, Frantz S, Ertl G, et al. Protective effects of sphingosine-1-phosphate receptor agonist treatment after myocardial ischaemia-reperfusion. Cardiovasc Res. 2009;83:285-93 pubmed publisher
    ..We tested the hypothesis that pharmacological S1P receptor agonists improve recovery of function when applied with reperfusion...
  53. Lahiri S, Park H, Laviad E, Lu X, Bittman R, Futerman A. Ceramide synthesis is modulated by the sphingosine analog FTY720 via a mixture of uncompetitive and noncompetitive inhibition in an Acyl-CoA chain length-dependent manner. J Biol Chem. 2009;284:16090-8 pubmed publisher
    ..Our data suggest a novel mechanism by which FTY720 might mediate some of its biological effects, which may be of mechanistic significance for understanding its mode of action...