Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis (Q34624835)

3 August 2017

Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis (English)

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3 August 2017

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Volker Brinkmann

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3 August 2017

Andreas Billich

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3 August 2017

Thomas Baumruker

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3 August 2017

Peter Heining

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3 August 2017

Robert Schmouder

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3 August 2017

Gordon Francis

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3 August 2017

Shreeram Aradhye

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3 August 2017

Pascale Burtin

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3 August 2017

29 October 2010

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Nature Reviews Drug Discovery

3 August 2017

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3 August 2017

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3 August 2017

883-897

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https://scigraph.springernature.com/pub.10.1038/nrd3248

3 August 2017

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The prevalence of multiple sclerosis in the world: an update

31 March 2020

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31 March 2020

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Effect of relapses on development of residual deficit in multiple sclerosis

31 March 2020

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The natural history of multiple sclerosis: a geographically based study. I. Clinical course and disability

31 March 2020

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Randomised double-blind placebo-controlled study of interferon β-1a in relapsing/remitting multiple sclerosis

31 March 2020

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Interferon beta-1b is effective in relapsing-remitting multiple sclerosis. I. Clinical results of a multicenter, randomized, double-blind, placebo-controlled trial. The IFNB Multiple Sclerosis Study Group

31 March 2020

1 reference

Intramuscular interferon beta-1a for disease progression in relapsing multiple sclerosis. The Multiple Sclerosis Collaborative Research Group (MSCRG)

31 March 2020

1 reference

Copolymer 1 reduces relapse rate and improves disability in relapsing-remitting multiple sclerosis: results of a phase III multicenter, double-blind placebo-controlled trial. The Copolymer 1 Multiple Sclerosis Study Group

31 March 2020

1 reference

Disease modifying therapies in multiple sclerosis: report of the Therapeutics and Technology Assessment Subcommittee of the American Academy of Neurology and the MS Council for Clinical Practice Guidelines

31 March 2020

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Optimizing the benefit of multiple sclerosis therapy: the importance of treatment adherence

31 March 2020

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Interferon in relapsing-remitting multiple sclerosis

31 March 2020

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Blocking adhesion molecules as therapy for multiple sclerosis: natalizumab

31 March 2020

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Natalizumab reduces clinical and MRI activity in multiple sclerosis patients with high disease activity: results from a multicenter study in Switzerland.

31 March 2020

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Cardiotoxicity and other adverse events associated with mitoxantrone treatment for MS.

31 March 2020

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Treating multiple sclerosis with monoclonal antibodies: a 2010 update.

31 March 2020

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Update on the treatment options for multiple sclerosis

31 March 2020

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A new immunosuppressant, FTY720, induces bcl-2-associated apoptotic cell death in human lymphocytes

31 March 2020

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Design, synthesis, and structure-activity relationships of 2-substituted-2-amino-1,3-propanediols: Discovery of a novel immunosuppressant, FTY720

31 March 2020

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FTY720: targeting G-protein-coupled receptors for sphingosine 1-phosphate in transplantation and autoimmunity

31 March 2020

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Serine palmitoyltransferase is the primary target of a sphingosine-like immunosuppressant, ISP-1/myriocin

31 March 2020

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The identification of myriocin-binding proteins

31 March 2020

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FTY720 alters lymphocyte homing and protects allografts without inducing general immunosuppression

31 March 2020

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FTY720: a novel transplantation drug that modulates lymphocyte traffic rather than activation

31 March 2020

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Graft-versus-host disease can be separated from graft-versus-lymphoma effects by control of lymphocyte trafficking with FTY720.

31 March 2020

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Transient T cell accumulation in lymph nodes and sustained lymphopenia in mice treated with FTY720.

31 March 2020

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FTY720 therapy exerts differential effects on T cell subsets in multiple sclerosis.

31 March 2020

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CC chemokine receptor 7-dependent and -independent pathways for lymphocyte homing: modulation by FTY720.

31 March 2020

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Induction of selective cell death targeting on mature T-lymphocytes in rats by a novel immunosuppressant, FTY720

31 March 2020

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The immunosuppressant drug FTY720 inhibits cytosolic phospholipase A2 independently of sphingosine-1-phosphate receptors

31 March 2020

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The immune modulator FTY720 inhibits sphingosine-1-phosphate lyase activity

31 March 2020

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The immune modulator FTY720 targets sphingosine 1-phosphate receptors

31 March 2020

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Alteration of lymphocyte trafficking by sphingosine-1-phosphate receptor agonists

31 March 2020

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Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1

31 March 2020

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FTY720: sphingosine 1-phosphate receptor-1 in the control of lymphocyte egress and endothelial barrier function.

31 March 2020

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FTY720 immunosuppression impairs effector T cell peripheral homing without affecting induction, expansion, and memory.

31 March 2020

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FTY720: dissection of membrane receptor-operated, stereospecific effects on cell migration from receptor-independent antiproliferative and apoptotic effects

31 March 2020

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Sphingosine kinase type 2 is essential for lymphopenia induced by the immunomodulatory drug FTY720.

31 March 2020

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Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer

31 March 2020

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Identification of Edg1 receptor residues that recognize sphingosine 1-phosphate.

31 March 2020

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Identification of Leu276 of the S1P1 receptor and Phe263 of the S1P3 receptor in interaction with receptor specific agonists by molecular modeling, site-directed mutagenesis, and affinity studies.

31 March 2020

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Brain penetration of the oral immunomodulatory drug FTY720 and its phosphorylation in the central nervous system during experimental autoimmune encephalomyelitis: consequences for mode of action in multiple sclerosis

31 March 2020

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Recent trials for FTY720 (fingolimod): a new generation of immunomodulators structurally similar to sphingosine

31 March 2020

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Sphingosine 1-phosphate receptors in health and disease: mechanistic insights from gene deletion studies and reverse pharmacology

31 March 2020

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Sphingosine-1-phosphate and modulation of vascular tone

31 March 2020

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Lysophospholipid activation of G protein-coupled receptors

31 March 2020

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Finding a way out: lymphocyte egress from lymphoid organs

31 March 2020

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Lysophospholipid receptors in vertebrate development, physiology, and pathology

31 March 2020

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The immunosuppressant FTY720 down-regulates sphingosine 1-phosphate G-protein-coupled receptors

31 March 2020

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Expression of the sphingosine 1-phosphate receptor, S1P1, on T-cells controls thymic emigration

31 March 2020

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S1P1 receptor signaling overrides retention mediated by G alpha i-coupled receptors to promote T cell egress

31 March 2020

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Lymphatic endothelial cell sphingosine kinase activity is required for lymphocyte egress and lymphatic patterning

31 March 2020

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Promotion of lymphocyte egress into blood and lymph by distinct sources of sphingosine-1-phosphate

31 March 2020

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Cortical sinus probing, S1P1-dependent entry and flow-based capture of egressing T cells

31 March 2020

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Cell-surface residence of sphingosine 1-phosphate receptor 1 on lymphocytes determines lymphocyte egress kinetics

31 March 2020

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Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses

31 March 2020

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Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo.

31 March 2020

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Central memory and effector memory T cell subsets: function, generation, and maintenance

31 March 2020

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Migration and function of antigen-primed nonpolarized T lymphocytes in vivo

31 March 2020

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The duration of antigenic stimulation determines the fate of naive and effector T cells.

31 March 2020

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Dynamics of T lymphocyte responses: intermediates, effectors, and memory cells

31 March 2020

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Visualizing the generation of memory CD4 T cells in the whole body

31 March 2020

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Two subsets of memory T lymphocytes with distinct homing potentials and effector functions

31 March 2020

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In vivo priming of CD4 T cells that produce interleukin (IL)-2 but not IL-4 or interferon (IFN)-gamma, and can subsequently differentiate into IL-4- or IFN-gamma-secreting cells

31 March 2020

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Priming of memory but not effector CD8 T cells by a killed bacterial vaccine

31 March 2020

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Preferential localization of effector memory cells in nonlymphoid tissue

31 March 2020

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Modulation of T cell homeostasis and alloreactivity under continuous FTY720 exposure

31 March 2020

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FTY720 (fingolimod) in Multiple Sclerosis: therapeutic effects in the immune and the central nervous system

31 March 2020

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Expression of CCR7 in multiple sclerosis: implications for CNS immunity.

31 March 2020

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In vivo detection of myelin proteins in cervical lymph nodes of MS patients using ultrasound-guided fine-needle aspiration cytology

31 March 2020

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Effector T cell interactions with meningeal vascular structures in nascent autoimmune CNS lesions

31 March 2020

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VEGF and angiogenesis in acute and chronic MOG((35-55)) peptide induced EAE.

31 March 2020

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Recovery from EAE is associated with decreased survival of encephalitogenic T cells in the CNS of B7-1/B7-2-deficient mice

31 March 2020

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Amelioration of experimental autoimmune encephalomyelitis in Lewis rats by FTY720 treatment

31 March 2020

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Th17 central memory T cells are reduced by FTY720 in patients with multiple sclerosis

31 March 2020

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FTY720 ameliorates experimental autoimmune neuritis by inhibition of lymphocyte and monocyte infiltration into peripheral nerves

31 March 2020

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FTY720 attenuates lesional interleukin-17(+) cell accumulation in rat experimental autoimmune neuritis

31 March 2020

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Cellular mechanisms of IL-17-induced blood-brain barrier disruption

31 March 2020

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Human TH17 lymphocytes promote blood-brain barrier disruption and central nervous system inflammation

31 March 2020

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Neuronal damage in autoimmune neuroinflammation mediated by the death ligand TRAIL.

31 March 2020

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Predictability of FTY720 efficacy in experimental autoimmune encephalomyelitis by in vivo macrophage tracking: clinical implications for ultrasmall superparamagnetic iron oxide-enhanced magnetic resonance imaging

31 March 2020

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Immunosuppressant FTY720 inhibits thymocyte emigration

31 March 2020

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VEGF and vascular changes in chronic neuroinflammation

31 March 2020

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In vitro and in vivo modulation of vascular barrier integrity by sphingosine 1-phosphate: mechanistic insights

31 March 2020

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Tipping the gatekeeper: S1P regulation of endothelial barrier function

31 March 2020

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Phosphorylation and action of the immunomodulator FTY720 inhibits vascular endothelial cell growth factor-induced vascular permeability.

31 March 2020

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Protective effects of sphingosine 1-phosphate in murine endotoxin-induced inflammatory lung injury

31 March 2020

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FTY720 rescue therapy in the dark agouti rat model of experimental autoimmune encephalomyelitis: expression of central nervous system genes and reversal of blood-brain-barrier damage

31 March 2020

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FTY720 sustains and restores neuronal function in the DA rat model of MOG-induced experimental autoimmune encephalomyelitis

31 March 2020

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Antagonism of sphingosine-1-phosphate receptors by FTY720 inhibits angiogenesis and tumor vascularization

31 March 2020

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Immunosuppressive and anti-angiogenic sphingosine 1-phosphate receptor-1 agonists induce ubiquitinylation and proteasomal degradation of the receptor

31 March 2020

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G-protein-coupled receptor S1P1 acts within endothelial cells to regulate vascular maturation.

31 March 2020

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Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors.

31 March 2020

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VEGF induces S1P1 receptors in endothelial cells: Implications for cross-talk between sphingolipid and growth factor receptors

31 March 2020

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Edg8/S1P5: an oligodendroglial receptor with dual function on process retraction and cell survival.

31 March 2020

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Essential roles of sphingosine 1-phosphate/S1P1 receptor axis in the migration of neural stem cells toward a site of spinal cord injury.

31 March 2020

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Sphingosine kinase 1/S1P receptor signaling axis controls glial proliferation in mice with Sandhoff disease.

31 March 2020

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Common signaling pathways link activation of murine PAR-1, LPA, and S1P receptors to proliferation of astrocytes.

31 March 2020

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Sphingosine 1-phosphate induces the production of glial cell line-derived neurotrophic factor and cellular proliferation in astrocytes

31 March 2020

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Pharmacological characterization of lysophospholipid receptor signal transduction pathways in rat cerebrocortical astrocytes.

31 March 2020

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Phosphorylated FTY720 promotes astrocyte migration through sphingosine-1-phosphate receptors.

31 March 2020

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FTY720 modulates human oligodendrocyte progenitor process extension and survival.

31 March 2020

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Fingolimod (FTY720) enhances remyelination following demyelination of organotypic cerebellar slices.

31 March 2020

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Essential role for sphingosine kinases in neural and vascular development

31 March 2020

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Sphingosine 1-phosphate and ceramide 1-phosphate: expanding roles in cell signaling

31 March 2020

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Sphingosine kinase 1 regulates the expression of proinflammatory cytokines and nitric oxide in activated microglia.

31 March 2020

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Intrathecal increase of sphingosine 1-phosphate at early stage multiple sclerosis

31 March 2020

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S1P inhibits gap junctions in astrocytes: involvement of G and Rho GTPase/ROCK.

31 March 2020

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Astrocyte-restricted ablation of interleukin-17-induced Act1-mediated signaling ameliorates autoimmune encephalomyelitis

31 March 2020

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Sphingosine 1-phosphate receptor 1 and 3 are upregulated in multiple sclerosis lesions

31 March 2020

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Sphingosine 1-phosphate receptor agonists attenuate relapsing-remitting experimental autoimmune encephalitis in SJL mice.

31 March 2020

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Oral-intravenous crossover study of fingolimod pharmacokinetics, lymphocyte responses and cardiac effects

31 March 2020

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Overview of FTY720 clinical pharmacokinetics and pharmacology

31 March 2020

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Pharmacodynamics, pharmacokinetics, and safety of multiple doses of FTY720 in stable renal transplant patients: a multicenter, randomized, placebo-controlled, phase I study

31 March 2020

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Oral fingolimod or intramuscular interferon for relapsing multiple sclerosis

31 March 2020

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Phase II study of oral fingolimod (FTY720) in multiple sclerosis: 3-year results

31 March 2020

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A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis

31 March 2020

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Oral fingolimod (FTY720) for relapsing multiple sclerosis

31 March 2020

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Oral fingolimod (FTY720) in multiple sclerosis: two-year results of a phase II extension study

31 March 2020

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Cell type-specific localization of human cardiac S1P receptors

31 March 2020

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The heart rate decrease caused by acute FTY720 administration is mediated by the G protein-gated potassium channel I.

31 March 2020

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G protein regulation of cardiac muscarinic potassium channel

31 March 2020

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The ability of atropine to prevent and reverse the negative chronotropic effect of fingolimod in healthy subjects

31 March 2020

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A mechanistic study to assess whether isoproterenol can reverse the negative chronotropic effect of fingolimod

31 March 2020

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Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.

31 March 2020

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Activation of muscarinic K+ current in guinea-pig atrial myocytes by sphingosine-1-phosphate.

31 March 2020

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Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate

31 March 2020

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Sphingosine 1-phosphate pathway therapeutics: a lipid ligand-receptor paradigm

31 March 2020

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Balance of S1P1 and S1P2 signaling regulates peripheral microvascular permeability in rat cremaster muscle vasculature

31 March 2020

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Hypertension in mice lacking the gene for endothelial nitric oxide synthase

31 March 2020

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Critical vasospasm during fingolimod (FTY720) treatment in a patient with multiple sclerosis

31 March 2020

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Effects of immunosuppressant FTY720 on renal and hepatic hemodynamics in the rat.

31 March 2020

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Protective effects of early CD4(+) T cell reduction in hepatic ischemia/reperfusion injury

31 March 2020

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Phenotype and function of human T lymphocyte subsets: consensus and issues

31 March 2020

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The 5-year direct medical cost of neonatal and childhood stroke in a population-based cohort

31 March 2020

1 reference

Requirement of secondary lymphoid tissues for the induction of primary and secondary T cell responses against Listeria monocytogenes.

31 March 2020

1 reference

Novel therapeutic strategies for multiple sclerosis--a multifaceted adversary

31 March 2020

1 reference

Interferon beta-1b is effective in relapsing-remitting multiple sclerosis. II. MRI analysis results of a multicenter, randomized, double-blind, placebo-controlled trial. UBC MS/MRI Study Group and the IFNB Multiple Sclerosis Study Group

31 March 2020

1 reference

European/Canadian multicenter, double-blind, randomized, placebo-controlled study of the effects of glatiramer acetate on magnetic resonance imaging-measured disease activity and burden in patients with relapsing multiple sclerosis

31 March 2020

1 reference

A randomized, placebo-controlled trial of natalizumab for relapsing multiple sclerosis

31 March 2020

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MRI outcomes in a placebo-controlled trial of natalizumab in relapsing MS.

31 March 2020

1 reference

European/Canadian multicenter, double-blind, randomized, placebo-controlled study of the effects of glatiramer acetate on magnetic resonance imaging--measured disease activity and burden in patients with relapsing multiple sclerosis. European/Canadi

31 March 2020

1 reference

12 December 2020

FTY720, a novel immunosuppressant, induces sequestration of circulating mature lymphocytes by acceleration of lymphocyte homing in rats. I. FTY720 selectively decreases the number of circulating mature lymphocytes by acceleration of lymphocyte homin

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12 December 2020

Changing responsiveness to chemokines allows medullary plasmablasts to leave lymph nodes

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12 December 2020

First human trial of FTY720, a novel immunomodulator, in stable renal transplant patients

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12 December 2020

Randomised double-blind placebo-controlled study of interferon beta-1a in relapsing/remitting multiple sclerosis. PRISMS (Prevention of Relapses and Disability by Interferon beta-1a Subcutaneously in Multiple Sclerosis) Study Group

1 reference

12 December 2020

FTY720, a novel immunomodulator: efficacy and safety results from the first phase 2A study in de novo renal transplantation

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12 December 2020

FTY720, a novel immunosuppressant possessing unique mechanisms. I. Prolongation of skin allograft survival and synergistic effect in combination with cyclosporine in rats

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12 December 2020

FTY720, a novel immunosuppressant, induces sequestration of circulating mature lymphocytes by acceleration of lymphocyte homing in rats. II. FTY720 prolongs skin allograft survival by decreasing T cell infiltration into grafts but not cytokine produ

1 reference

12 December 2020

FTY720, sphingosine 1-phosphate receptor modulator, ameliorates experimental autoimmune encephalomyelitis by inhibition of T cell infiltration.

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12 December 2020

Identifiers

DOI

10.1038/NRD3248

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3 August 2017

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