Recent Advances in the Discovery and Development of Sphingosine-1-Phosphate-1 Receptor Agonists

[1]  J. Moberly,et al.  Pharmacological Modulation of Peripheral T and B Lymphocytes by a Selective Sphingosine 1‐Phosphate Receptor‐1 Modulator , 2012, Journal of clinical pharmacology.

[2]  S. Dowell,et al.  The utility of pharmacokinetic–pharmacodynamic modeling in the discovery and optimization of selective S1P1 agonists , 2012, Xenobiotica; the fate of foreign compounds in biological systems.

[3]  T. Vollmer,et al.  Pharmacological effects of CS-0777, a selective sphingosine 1-phosphate receptor-1 modulator: Results from a 12-week, open-label pilot study in multiple sclerosis patients , 2012, Journal of Neuroimmunology.

[4]  Tsuyoshi Nakamura,et al.  Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist. , 2012, European journal of medicinal chemistry.

[5]  Tsuyoshi Nakamura,et al.  Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists. , 2012, Bioorganic & medicinal chemistry letters.

[6]  J. D. Elliott,et al.  Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists. , 2012, Bioorganic & medicinal chemistry letters.

[7]  S. Reber,et al.  Practical and Scalable Synthesis of S1P1 Receptor Agonist ACT-209905 , 2012 .

[8]  Hugh Rosen,et al.  Crystal Structure of a Lipid G Protein–Coupled Receptor , 2012, Science.

[9]  Tsuyoshi Nakamura,et al.  Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist. , 2012, Bioorganic & medicinal chemistry letters.

[10]  D. Hafler,et al.  Fingolimod for multiple sclerosis. , 2012, The New England journal of medicine.

[11]  Matthew R. Lee,et al.  Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core. , 2012, ACS medicinal chemistry letters.

[12]  Y. Igarashi,et al.  Amelioration of Collagen-Induced Arthritis by a Novel S1P1 Antagonist with Immunomodulatory Activities , 2012, The Journal of Immunology.

[13]  Matthew R. Lee,et al.  Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity. , 2012, Bioorganic & medicinal chemistry letters.

[14]  M. Minami,et al.  Structure-activity relationship studies of S1P agonists with a dihydronaphthalene scaffold. , 2012, Bioorganic & medicinal chemistry letters.

[15]  C. Sage,et al.  Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P₁ agonists. , 2011, Bioorganic & medicinal chemistry letters.

[16]  S. Dowell,et al.  Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose. , 2011, Journal of medicinal chemistry.

[17]  H. Hartung,et al.  Critical appraisal of the role of fingolimod in the treatment of multiple sclerosis , 2011, Neuropsychiatric disease and treatment.

[18]  Matthew R. Lee,et al.  4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1. , 2011, ACS medicinal chemistry letters.

[19]  M. Minami,et al.  Discovery of S1P agonists with a dihydronaphthalene scaffold. , 2011, Bioorganic & medicinal chemistry letters.

[20]  S. Dowell,et al.  Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate. , 2011, ACS medicinal chemistry letters.

[21]  M. Anson,et al.  Development of a Fully Telescoped Synthesis of the S1P1 Agonist GSK1842799 , 2011 .

[22]  T. Ohnuki,et al.  Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist. , 2011, ACS medicinal chemistry letters.

[23]  Jennifer E. Golden,et al.  Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1). , 2011, ACS medicinal chemistry letters.

[24]  Jennifer E. Golden,et al.  Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5. , 2011, ACS medicinal chemistry letters.

[25]  R. Bürli,et al.  Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS. , 2011, ACS medicinal chemistry letters.

[26]  J. Chun,et al.  Roles for lysophospholipid S1P receptors in multiple sclerosis , 2011, Critical reviews in biochemistry and molecular biology.

[27]  A. Olivera,et al.  An emerging role for the lipid mediator sphingosine-1-phosphate in mast cell effector function and allergic disease. , 2011, Advances in experimental medicine and biology.

[28]  Sarah Spiegel,et al.  International Union of Basic and Clinical Pharmacology. LXXVIII. Lysophospholipid Receptor Nomenclature , 2010, Pharmacological Reviews.

[29]  M. Bolli,et al.  2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists. , 2010, Journal of medicinal chemistry.

[30]  A. Saha,et al.  Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists. , 2010, Bioorganic & medicinal chemistry letters.

[31]  B. Nuesslein-Hildesheim,et al.  Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists. , 2010, Bioorganic & medicinal chemistry letters.

[32]  V. Brinkmann.  FTY720 (fingolimod) in Multiple Sclerosis: therapeutic effects in the immune and the central nervous system , 2009, British journal of pharmacology.

[33]  A. Saha,et al.  Synthesis and evaluation of arylalkoxy- and biarylalkoxy-phenylamide and phenylimidazoles as potent and selective sphingosine-1-phosphate receptor subtype-1 agonists. , 2009, Bioorganic & medicinal chemistry letters.

[34]  A. Saha,et al.  Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists. , 2009, Bioorganic & medicinal chemistry letters.

[35]  T. Nishida,et al.  A Novel Sphingosine 1-Phosphate Receptor Agonist, 2-Amino-2-propanediol Hydrochloride (KRP-203), Regulates Chronic Colitis in Interleukin-10 Gene-Deficient Mice , 2008, Journal of Pharmacology and Experimental Therapeutics.

[36]  J. Cyster,et al.  Promotion of Lymphocyte Egress into Blood and Lymph by Distinct Sources of Sphingosine-1-Phosphate , 2007, Science.

[37]  Y. Fujiwara,et al.  Identification of the Hydrophobic Ligand Binding Pocket of the S1P1 Receptor* , 2007, Journal of Biological Chemistry.

[38]  M. Salvadori,et al.  Randomized Controlled Trial of FTY720 Versus MMF in De Novo Renal Transplantation , 2006, Transplantation.

[39]  M. Salvadori,et al.  FTY720 versus MMF with Cyclosporine in de novo Renal Transplantation: A 1‐Year, Randomized Controlled Trial in Europe and Australasia , 2006, American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons.

[40]  S. A. Parent,et al.  Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3. , 2005, Journal of medicinal chemistry.

[41]  S. Enosawa,et al.  KRP-203, a Novel Synthetic Immunosuppressant, Prolongs Graft Survival and Attenuates Chronic Rejection in Rat Skin and Heart Allografts , 2005, Circulation.

[42]  M. Ferrer,et al.  A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists. , 2004, Journal of medicinal chemistry.

[43]  G. Chrebet,et al.  Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists. , 2004, Bioorganic & medicinal chemistry letters.

[44]  R. Proia,et al.  Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1 , 2004, Nature.

[45]  A. Billich,et al.  Phosphorylation of the Immunomodulatory Drug FTY720 by Sphingosine Kinases* , 2003, Journal of Biological Chemistry.

[46]  S. Payne,et al.  The immunosuppressant FTY720 is phosphorylated by sphingosine kinase type 2 , 2003, FEBS letters.

[47]  Michael D. Davis,et al.  The Immune Modulator FTY720 Targets Sphingosine 1-Phosphate Receptors* , 2002, The Journal of Biological Chemistry.

[48]  H. Rosen,et al.  Alteration of Lymphocyte Trafficking by Sphingosine-1-Phosphate Receptor Agonists , 2002, Science.

[49]  S. Spiegel,et al.  Identification of Edg1 Receptor Residues That Recognize Sphingosine 1-Phosphate* , 2000, The Journal of Biological Chemistry.

[50]  H. Kataoka,et al.  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 homing. , 1998, Journal of immunology.

[51]  D. Schmitz,et al.  Metabolism of methapyrilene by rat-liver homogenate. , 1986, Xenobiotica; the fate of foreign compounds in biological systems.