Published in J Med Chem on August 11, 2005
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Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis. Nat Rev Drug Discov (2010) 5.55
FTY720 (fingolimod) in Multiple Sclerosis: therapeutic effects in the immune and the central nervous system. Br J Pharmacol (2009) 2.49
Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors. Nat Chem Biol (2009) 2.47
A mechanistically novel, first oral therapy for multiple sclerosis: the development of fingolimod (FTY720, Gilenya). Discov Med (2011) 1.65
Therapeutic opportunities for manipulating T(Reg) cells in autoimmunity and cancer. Nat Rev Drug Discov (2013) 1.50
Asymmetric synthesis of conformationally constrained fingolimod analogues--discovery of an orally active sphingosine 1-phosphate receptor type-1 agonist and receptor type-3 antagonist. J Med Chem (2007) 1.22
Chiral vinylphosphonate and phosphonate analogues of the immunosuppressive agent FTY720. J Org Chem (2009) 1.19
Immunomodulator FTY720 induces myofibroblast differentiation via the lysophospholipid receptor S1P3 and Smad3 signaling. Am J Pathol (2007) 1.17
Synthetic analogs of FTY720 [2-amino-2-(2-[4-octylphenyl]ethyl)-1,3-propanediol] differentially regulate pulmonary vascular permeability in vivo and in vitro. J Pharmacol Exp Ther (2009) 1.11
Fingolimod modulates microglial activation to augment markers of remyelination. J Neuroinflammation (2011) 0.97
FTY720 story. Its discovery and the following accelerated development of sphingosine 1-phosphate receptor agonists as immunomodulators based on reverse pharmacology. Perspect Medicin Chem (2007) 0.97
Sphingosine 1-phosphate chemical biology. Biochim Biophys Acta (2008) 0.93
Different response patterns of several ligands at the sphingosine-1-phosphate receptor subtype 3 (S1P(3)). Br J Pharmacol (2009) 0.89
FTY720 normalizes hyperglycemia by stimulating β-cell in vivo regeneration in db/db mice through regulation of cyclin D3 and p57(KIP2). J Biol Chem (2011) 0.88
FTY720 (fingolimod) increases vascular tone and blood pressure in spontaneously hypertensive rats via inhibition of sphingosine kinase. Br J Pharmacol (2012) 0.83
Sphingosine-1-phosphate evokes unique segment-specific vasoconstriction of the renal microvasculature. J Am Soc Nephrol (2014) 0.82
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis. ACS Med Chem Lett (2013) 0.79
4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1. ACS Med Chem Lett (2011) 0.79
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs. Bioorg Med Chem Lett (2010) 0.78
The sphingosine-1-phosphate analogue, FTY-720, promotes the proliferation of embryonic neural stem cells, enhances hippocampal neurogenesis and learning and memory abilities in adult mice. Br J Pharmacol (2016) 0.78
Elevated Nuclear and Cytoplasmic FTY720-Phosphate in Mouse Embryonic Fibroblasts Suggests the Potential for Multiple Mechanisms in FTY720-Induced Neural Tube Defects. Toxicol Sci (2015) 0.76
Endocytosis of Ligand-Activated Sphingosine 1-Phosphate Receptor 1 Mediated by the Clathrin-Pathway. Traffic (2015) 0.76
Preclinical Metabolism, Pharmacokinetics and In Vivo Analysis of New Blood-Brain-Barrier Penetrant Fingolimod Analogues: FTY720-C2 and FTY720-Mitoxy. PLoS One (2016) 0.75
Identification and Characterization of FTY720 for the Treatment of Human African Trypanosomiasis. Antimicrob Agents Chemother (2015) 0.75
Use of intensity quotients and differences in absolute structure refinement. Acta Crystallogr B Struct Sci Cryst Eng Mater (2013) 32.55
Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1. Nature (2004) 12.72
Novel cell death program leads to neutrophil extracellular traps. J Cell Biol (2007) 10.92
The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem (2002) 6.96
Netting neutrophils in autoimmune small-vessel vasculitis. Nat Med (2009) 6.72
Neutrophil extracellular traps contain calprotectin, a cytosolic protein complex involved in host defense against Candida albicans. PLoS Pathog (2009) 5.40
Impairment of neutrophil extracellular trap degradation is associated with lupus nephritis. Proc Natl Acad Sci U S A (2010) 5.05
Neutrophil extracellular traps capture and kill Candida albicans yeast and hyphal forms. Cell Microbiol (2006) 4.47
Reciprocal coupling of coagulation and innate immunity via neutrophil serine proteases. Nat Med (2010) 4.32
Calcium and a calcium-dependent protein kinase regulate gamete formation and mosquito transmission in a malaria parasite. Cell (2004) 4.30
Dynamic T cell migration program provides resident memory within intestinal epithelium. J Exp Med (2010) 4.09
Restoration of NET formation by gene therapy in CGD controls aspergillosis. Blood (2009) 4.06
Monocytes, neutrophils, and platelets cooperate to initiate and propagate venous thrombosis in mice in vivo. J Exp Med (2012) 3.63
Apoptosis facilitates antigen presentation to T lymphocytes through MHC-I and CD1 in tuberculosis. Nat Med (2003) 3.24
Increased vaccine efficacy against tuberculosis of recombinant Mycobacterium bovis bacille Calmette-Guérin mutants that secrete listeriolysin. J Clin Invest (2005) 3.19
Phosphorylation and action of the immunomodulator FTY720 inhibits vascular endothelial cell growth factor-induced vascular permeability. J Biol Chem (2003) 2.98
Apoptotic vesicles crossprime CD8 T cells and protect against tuberculosis. Immunity (2006) 2.61
Proton-sensing G-protein-coupled receptors. Nature (2003) 2.58
Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors. Nat Chem Biol (2009) 2.47
T cells become licensed in the lung to enter the central nervous system. Nature (2012) 2.45
Prohibitin is required for Ras-induced Raf-MEK-ERK activation and epithelial cell migration. Nat Cell Biol (2005) 2.41
Metal ion roles and the movement of hydrogen during reaction catalyzed by D-xylose isomerase: a joint x-ray and neutron diffraction study. Structure (2010) 2.20
Oxysterols direct immune cell migration via EBI2. Nature (2011) 2.19
Chlamydia causes fragmentation of the Golgi compartment to ensure reproduction. Nature (2008) 2.04
Saposin C is required for lipid presentation by human CD1b. Nat Immunol (2004) 1.88
Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria. J Med Chem (2010) 1.84
Sphingosine-1-phosphate stimulates the functional capacity of progenitor cells by activation of the CXCR4-dependent signaling pathway via the S1P3 receptor. Arterioscler Thromb Vasc Biol (2006) 1.80
Mouse neutrophil extracellular traps in microbial infections. J Innate Immun (2009) 1.79
From the inside out--processing of the Chlamydial autotransporter PmpD and its role in bacterial adhesion and activation of human host cells. Mol Microbiol (2004) 1.78
A small non-coding RNA of the invasion gene island (SPI-1) represses outer membrane protein synthesis from the Salmonella core genome. Mol Microbiol (2007) 1.72
The adaptor molecule CARD9 is essential for tuberculosis control. J Exp Med (2010) 1.70
The heart rate decrease caused by acute FTY720 administration is mediated by the G protein-gated potassium channel I. Am J Transplant (2005) 1.70
A mechanistically novel, first oral therapy for multiple sclerosis: the development of fingolimod (FTY720, Gilenya). Discov Med (2011) 1.65
Optimal deconvolution of transcriptional profiling data using quadratic programming with application to complex clinical blood samples. PLoS One (2011) 1.62
Flow-regulated endothelial S1P receptor-1 signaling sustains vascular development. Dev Cell (2012) 1.62
Fingolimod provides long-term protection in rodent models of cerebral ischemia. Ann Neurol (2010) 1.62
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Lung-residing myeloid-derived suppressors display dual functionality in murine pulmonary tuberculosis. Am J Respir Crit Care Med (2014) 1.54
A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem Biol (2006) 1.47
FTY720, a synthetic sphingosine 1 phosphate analogue, inhibits development of atherosclerosis in low-density lipoprotein receptor-deficient mice. Circulation (2007) 1.46
Prevalence of Propionibacterium acnes in diseased prostates and its inflammatory and transforming activity on prostate epithelial cells. Int J Med Microbiol (2010) 1.45
Human neutrophils kill Bacillus anthracis. PLoS Pathog (2005) 1.38
The IFN-inducible Golgi- and endoplasmic reticulum- associated 47-kDa GTPase IIGP is transiently expressed during listeriosis. J Immunol (2002) 1.34
The sphingosine-1-phosphate receptor agonist FTY720 modulates dendritic cell trafficking in vivo. Am J Transplant (2005) 1.32
Rab6 and Rab11 regulate Chlamydia trachomatis development and golgin-84-dependent Golgi fragmentation. PLoS Pathog (2009) 1.31
The sphingosine 1-phosphate receptor agonist FTY720 differentially affects the sequestration of CD4+/CD25+ T-regulatory cells and enhances their functional activity. J Immunol (2005) 1.30
Phosphorylated FTY720 promotes astrocyte migration through sphingosine-1-phosphate receptors. J Neurochem (2007) 1.30
The sphingosine 1-phosphate receptor agonist FTY720 supports CXCR4-dependent migration and bone marrow homing of human CD34+ progenitor cells. Blood (2004) 1.29
Delay of phagosome maturation by a mycobacterial lipid is reversed by nitric oxide. Cell Microbiol (2008) 1.26
Modified immunohistological staining allows detection of Ziehl-Neelsen-negative Mycobacterium tuberculosis organisms and their precise localization in human tissue. J Pathol (2005) 1.26
Inhibition of Th1- and Th2-mediated airway inflammation by the sphingosine 1-phosphate receptor agonist FTY720. J Immunol (2003) 1.25
Expression and translocation of chlamydial protease during acute and persistent infection of the epithelial HEp-2 cells with Chlamydophila (Chlamydia) pneumoniae. Cell Microbiol (2003) 1.25
FTY720 induces apoptosis in multiple myeloma cells and overcomes drug resistance. Cancer Res (2005) 1.25
Requirement for O-linked N-acetylglucosaminyltransferase in lymphocytes activation. EMBO J (2007) 1.22
A comparative functional analysis of plasma membrane Ca2+ pump isoforms in intact cells. J Biol Chem (2003) 1.22
Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo. J Med Chem (2008) 1.19
Metabolism and disposition of imatinib mesylate in healthy volunteers. Drug Metab Dispos (2005) 1.18
FTY720 preferentially depletes naive T cells from peripheral and lymphoid organs. Int Immunopharmacol (2006) 1.15
Neutrophilia in LFA-1-deficient mice confers resistance to listeriosis: possible contribution of granulocyte-colony-stimulating factor and IL-17. J Immunol (2003) 1.15
Type I IFN signaling triggers immunopathology in tuberculosis-susceptible mice by modulating lung phagocyte dynamics. Eur J Immunol (2014) 1.15
The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J Pharmacol Exp Ther (2009) 1.14
Immunomodulator FTY720 Induces eNOS-dependent arterial vasodilatation via the lysophospholipid receptor S1P3. Circ Res (2005) 1.14
Distinct mechanisms of internalization of Neisseria gonorrhoeae by members of the CEACAM receptor family involving Rac1- and Cdc42-dependent and -independent pathways. EMBO J (2002) 1.14
FTY720, an immunomodulatory sphingolipid mimetic: translation of a novel mechanism into clinical benefit in multiple sclerosis. Expert Opin Investig Drugs (2007) 1.13
The Helicobacter pylori CagA protein disrupts matrix adhesion of gastric epithelial cells by dephosphorylation of vinculin. Cell Microbiol (2007) 1.10
Bacterial porin disrupts mitochondrial membrane potential and sensitizes host cells to apoptosis. PLoS Pathog (2009) 1.09
Propionibacterium acnes host cell tropism contributes to vimentin-mediated invasion and induction of inflammation. Cell Microbiol (2012) 1.09
Insights into the mechanism of FTY720 and compatibility with regulatory T cells for the inhibition of graft-versus-host disease (GVHD). Blood (2007) 1.07
Anticancer activity of FTY720: phosphorylated FTY720 inhibits autotaxin, a metastasis-enhancing and angiogenic lysophospholipase D. Cancer Lett (2008) 1.07
Helicobacter pylori induces AGS cell motility and elongation via independent signaling pathways. Infect Immun (2004) 1.07
Structural basis of guanine nucleotide exchange mediated by the T-cell essential Vav1. J Mol Biol (2008) 1.05
Helicobacter pylori HP0518 affects flagellin glycosylation to alter bacterial motility. Mol Microbiol (2010) 1.04
Interaction of Chlamydia trachomatis serovar L2 with the host autophagic pathway. Infect Immun (2004) 1.04
The O-linked N-acetylglucosamine modification in cellular signalling and the immune system. 'Protein modifications: beyond the usual suspects' review series. EMBO Rep (2008) 1.04
Small molecule-facilitated degradation of ANO1 protein: a new targeting approach for anticancer therapeutics. J Biol Chem (2014) 1.03
A proposed role for neutrophil extracellular traps in cancer immunoediting. Front Immunol (2013) 1.02
Wnt/β-catenin signalling induces MLL to create epigenetic changes in salivary gland tumours. EMBO J (2013) 1.02
Ring-modified analogues and molecular dynamics studies to probe the requirements for fungicidal activities of malayamycin A and its N-nucleoside variants. J Org Chem (2007) 1.01
FTY720 pretreatment reduces warm hepatic ischemia reperfusion injury through inhibition of T-lymphocyte infiltration. Am J Transplant (2002) 1.01
Improved lymphocyte function-associated antigen-1 (LFA-1) inhibition by statin derivatives: molecular basis determined by x-ray analysis and monitoring of LFA-1 conformational changes in vitro and ex vivo. J Biol Chem (2004) 1.00
Argyrins, immunosuppressive cyclic peptides from myxobacteria. I. Production, isolation, physico-chemical and biological properties. J Antibiot (Tokyo) (2002) 1.00
Critical role for heat shock protein 20 (HSP20) in migration of malarial sporozoites. J Biol Chem (2011) 1.00
Bim and Bmf synergize to induce apoptosis in Neisseria gonorrhoeae infection. PLoS Pathog (2009) 0.99
Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain. Bioorg Med Chem Lett (2004) 0.99
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes. J Med Chem (2009) 0.99
A potent and selective S1P(1) antagonist with efficacy in experimental autoimmune encephalomyelitis. Chem Biol (2012) 0.98
Angiogenesis is present in experimental autoimmune encephalomyelitis and pro-angiogenic factors are increased in multiple sclerosis lesions. J Neuroinflammation (2010) 0.97
The exported Plasmodium berghei protein IBIS1 delineates membranous structures in infected red blood cells. Mol Microbiol (2012) 0.95
A key role for lung-resident memory lymphocytes in protective immune responses after BCG vaccination. Eur J Immunol (2010) 0.95
Constrained azacyclic analogues of the immunomodulatory agent FTY720 as molecular probes for sphingosine 1-phosphate receptors. Bioorg Med Chem Lett (2006) 0.95
Transient T cell accumulation in lymph nodes and sustained lymphopenia in mice treated with FTY720. Eur J Immunol (2005) 0.94
Reversible translocation of p115-RhoGEF by G(12/13)-coupled receptors. J Cell Biochem (2008) 0.93
Lack of stage-specific proteins in coccoid Helicobacter pylori cells. Infect Immun (2004) 0.93