S1pr1

Summary

Gene Symbol: S1pr1
Description: sphingosine-1-phosphate receptor 1
Alias: Edg1, EDG1 (Edg1), S1P receptor 1, S1P receptor Edg-1, S1P1, endothelial differentiation G-protein coupled receptor 1, endothelial differentiation sphingolipid G-protein-coupled receptor 1, sphingosine 1-phosphate receptor 1, sphingosine 1-phosphate receptor Edg-1
Species: rat

Top Publications

  1. doi Fingolimod inhibits PDGF-B-induced migration of vascular smooth muscle cell by down-regulating the S1PR1/S1PR3 pathway
    Yoanne Mousseau
    Department of Biochemistry and Molecular Genetic, CHU Dupuytren, Limoges, France
    Biochimie 94:2523-31. 2012
  2. pmc Sphingosine-1-phosphate acting via the S1P₁ receptor is a downstream signaling pathway in ceramide-induced hyperalgesia
    Tim Doyle
    Department of Pharmacological and Physiological Science, Saint Louis University School of Medicine, 1402 South Grand Blvd, St Louis, MO 63104, USA
    Neurosci Lett 499:4-8. 2011
  3. pmc Purification and identification of activating enzymes of CS-0777, a selective sphingosine 1-phosphate receptor 1 modulator, in erythrocytes
    Kiyoaki Yonesu
    Cardiovascular Metabolics Research Laboratories, Daiichi Sankyo Co, Ltd, Tokyo 134 8630, Japan
    J Biol Chem 286:24765-75. 2011
  4. doi Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity
    Lewis D Pennington
    Medicinal Chemistry, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, USA
    Bioorg Med Chem Lett 22:527-31. 2012
  5. pmc Knockdown of the sphingosine-1-phosphate receptor S1PR1 reduces pain behaviors induced by local inflammation of the rat sensory ganglion
    Wenrui Xie
    Pain Research Center, Department of Anesthesiology, University of Cincinnati College of Medicine, Cincinnati, OH 45267 0531, USA
    Neurosci Lett 515:61-5. 2012
  6. pmc Expression of sphingosine 1-phosphate receptors in the rat dorsal root ganglia and defined single isolated sensory neurons
    J S Kays
    Department of Pharmacology and Toxicology, School of Medicine, Indiana University, Indianapolis, Indiana 46202, USA
    Physiol Genomics 44:889-901. 2012
  7. pmc FTY720 (Gilenya) phosphate selectivity of sphingosine 1-phosphate receptor subtype 1 (S1P1) G protein-coupled receptor requires motifs in intracellular loop 1 and transmembrane domain 2
    William J Valentine
    Department of Physiology, College of Medicine, University of Tennessee Health Science Center, Memphis, Tennessee 38163, USA
    J Biol Chem 286:30513-25. 2011
  8. pmc Chronic sphingosine 1-phosphate 1 receptor activation attenuates early-stage diabetic nephropathy independent of lymphocytes
    Alaa S Awad
    Department of Medicine, University of Virginia, Charlottesville, Virginia, USA
    Kidney Int 79:1090-8. 2011
  9. pmc The sphingosine 1-phosphate receptor, S1PR₁, plays a prominent but not exclusive role in enhancing the excitability of sensory neurons
    Xian Xuan Chi
    Department of Pharmacology and Toxicology, School of Medicine, Indiana University, Indianapolis, IN 46202, USA
    J Neurophysiol 104:2741-8. 2010
  10. pmc Sphingosine-1-phosphate prevents permeability increases via activation of endothelial sphingosine-1-phosphate receptor 1 in rat venules
    Gengqian Zhang
    Department of Physiology and Pharmacology, School of Medicine, West Virginia University, Morgantown, West Virginia 26506 9229, USA
    Am J Physiol Heart Circ Physiol 299:H1494-504. 2010

Research Grants

Scientific Experts

  • Wenrui Xie
  • P Robert
  • Laura J Sim-Selley
  • Brian R Wamhoff
  • Laura Sim Selley
  • Laura J Sim Selley
  • Alaa S Awad
  • Yoanne Mousseau
  • Lewis D Pennington
  • J S Kays
  • Tim Doyle
  • Kiyoaki Yonesu
  • G D Nicol
  • William J Valentine
  • Xian Xuan Chi
  • Sven Christian Sensken
  • Gengqian Zhang
  • Mark D Okusa
  • Kevin R Lynch
  • Liping Huang
  • H Okamoto
  • Delyth Graham
  • Atsushi Kimura
  • Soichiro Usui
  • Christopher Fotsch
  • Laurent Fourcade
  • Yasser Baaj
  • Benoit Funalot
  • Yang Xu
  • Andrew S Tasker
  • Brian A Lanman
  • Matthew R Lee
  • Séverine Mollard
  • Franck G Sturtz
  • Kelvin K C Sham
  • Anthony B Reed
  • Henry G Morrison
  • Hao Qiu
  • Michael Fiorino
  • Laurence Richard
  • Chao Li
  • Heather A Arnett
  • Michelle Horner
  • M J Kluk
  • Alexander J Pickrell
  • Karine Faucher-Durand
  • Michele McElvain
  • Paul E Harrington
  • Michael J Frohn
  • Min Wong
  • Han Xu
  • Jeanne Cook-Moreau
  • Xuxia Zhang
  • Angélique Nizou
  • Victor J Cee
  • Michael D Croghan
  • W Kline Bolton
  • Daniela Salvemini
  • Konstantine Khutsishvili
  • Tatsuji Matsuoka
  • Lina M Obeid
  • Virginia I Godwin
  • Chizuko Yahara
  • Gabor Tigyi
  • Kazuishi Kubota
  • Yuko Fujiwara
  • Michael D Rouse
  • Shin ichi Inaba
  • James Van Brocklyn
  • Futoshi Nara
  • Masakazu Tamura
  • Zhoumou Chen
  • Tomohiro Honda
  • Nobuaki Watanabe
  • Robert Bittman
  • Daniel A Osborne
  • Jianxiong Liu
  • Abby L Parrill
  • A L Parrill
  • Sulei Xu
  • Pingnian He
  • Yan Qian
  • Markus H Gräler
  • H Shigematsu
  • Y Takuwa
  • N Takuwa
  • Ryunosuke Ohkawa
  • Jun Mimuro
  • Eiji Kobayashi
  • Yuichi Hoshino

Detail Information

Publications23

  1. doi Fingolimod inhibits PDGF-B-induced migration of vascular smooth muscle cell by down-regulating the S1PR1/S1PR3 pathway
    Yoanne Mousseau
    Department of Biochemistry and Molecular Genetic, CHU Dupuytren, Limoges, France
    Biochimie 94:2523-31. 2012
    ..We then compared siRNA and/or fingolimod (100 nM) treatments on PDGFR-β, S1PR1 S1PR2 and S1PR3 expression...
  2. pmc Sphingosine-1-phosphate acting via the S1P₁ receptor is a downstream signaling pathway in ceramide-induced hyperalgesia
    Tim Doyle
    Department of Pharmacological and Physiological Science, Saint Louis University School of Medicine, 1402 South Grand Blvd, St Louis, MO 63104, USA
    Neurosci Lett 499:4-8. 2011
    ..Our results further demonstrate that S1P contributes to the development of hyperalgesia via the S1P receptor 1 subtype (S1PR(1)), since responses were blocked by a well characterized S1PR(1) antagonist, W146, but not by ..
  3. pmc Purification and identification of activating enzymes of CS-0777, a selective sphingosine 1-phosphate receptor 1 modulator, in erythrocytes
    Kiyoaki Yonesu
    Cardiovascular Metabolics Research Laboratories, Daiichi Sankyo Co, Ltd, Tokyo 134 8630, Japan
    J Biol Chem 286:24765-75. 2011
    ..Identification of the kinases responsible for CS-0777 activation will permit a better understanding of the pharmacokinetics and pharmacodynamics of this promising new drug...
  4. doi Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity
    Lewis D Pennington
    Medicinal Chemistry, Amgen, One Amgen Center Drive, Thousand Oaks, CA 91320, USA
    Bioorg Med Chem Lett 22:527-31. 2012
    ..15 L/h/kg, V(dss)=5.1L/kg, T(1/2)=24h, %F=110; 5: CL=0.93L/h/kg, V(dss)=11L/kg, T(1/2)=15 h, %F=60) and pharmacodynamics (17: 1.0mg/kg po, 24h PLC POC=-67%; 5: 3mg/kg po, 24h PLC POC=-51%) in rat...
  5. pmc Knockdown of the sphingosine-1-phosphate receptor S1PR1 reduces pain behaviors induced by local inflammation of the rat sensory ganglion
    Wenrui Xie
    Pain Research Center, Department of Anesthesiology, University of Cincinnati College of Medicine, Cincinnati, OH 45267 0531, USA
    Neurosci Lett 515:61-5. 2012
    ..receptors, and in vitro S1P has excitatory effects on small-diameter sensory neurons, many mediated by the S1P receptor 1 (S1PR1). This study investigated the role of S1P in regulating the sensitivity of DRG neurons...
  6. pmc Expression of sphingosine 1-phosphate receptors in the rat dorsal root ganglia and defined single isolated sensory neurons
    J S Kays
    Department of Pharmacology and Toxicology, School of Medicine, Indiana University, Indianapolis, Indiana 46202, USA
    Physiol Genomics 44:889-901. 2012
    ..1-phosphate (S1P) increased the excitability of small-diameter sensory neurons, in part, through activation of S1P receptor 1 (S1PR(1)), suggesting that other S1PRs can modulate neuronal excitability...
  7. pmc FTY720 (Gilenya) phosphate selectivity of sphingosine 1-phosphate receptor subtype 1 (S1P1) G protein-coupled receptor requires motifs in intracellular loop 1 and transmembrane domain 2
    William J Valentine
    Department of Physiology, College of Medicine, University of Tennessee Health Science Center, Memphis, Tennessee 38163, USA
    J Biol Chem 286:30513-25. 2011
    ..sequence from the N terminus to transmembrane domain 2 (TM2) was activated by FTY720P, and the S1P(2)(IC1-TM2)(S1P1) domain insertion chimera showed S1P(1)-like activation...
  8. pmc Chronic sphingosine 1-phosphate 1 receptor activation attenuates early-stage diabetic nephropathy independent of lymphocytes
    Alaa S Awad
    Department of Medicine, University of Virginia, Charlottesville, Virginia, USA
    Kidney Int 79:1090-8. 2011
    ..As S1P1 receptor (S1P1R) activation blocks kidney inflammation in acute renal injury, we tested whether activation of ..
  9. pmc The sphingosine 1-phosphate receptor, S1PR₁, plays a prominent but not exclusive role in enhancing the excitability of sensory neurons
    Xian Xuan Chi
    Department of Pharmacology and Toxicology, School of Medicine, Indiana University, Indianapolis, IN 46202, USA
    J Neurophysiol 104:2741-8. 2010
    ..These results indicate that S1PR(1) plays a prominent, although not exclusive, role in mediating the enhancement of excitability produced by S1P...
  10. pmc Sphingosine-1-phosphate prevents permeability increases via activation of endothelial sphingosine-1-phosphate receptor 1 in rat venules
    Gengqian Zhang
    Department of Physiology and Pharmacology, School of Medicine, West Virginia University, Morgantown, West Virginia 26506 9229, USA
    Am J Physiol Heart Circ Physiol 299:H1494-504. 2010
    ....
  11. pmc Down-regulation of S1P1 receptor surface expression by protein kinase C inhibition
    Sven Christian Sensken
    Institute for Immunology, Hannover Medical School, 30625 Hanover, Germany
    J Biol Chem 285:6298-307. 2010
    ..3-3 mg/kg/day FTY720 showed increasing concentration-dependent effectiveness. PKC inhibition therefore may contribute to lymphopenia by down-regulating S1P(1) receptor cell surface expression independently from its activation...
  12. pmc Sphingosine-1-phosphate receptors mediate neuromodulatory functions in the CNS
    Laura J Sim-Selley
    Department of Pharmacology and Toxicology and Institute for Drug and Alcohol Studies, Virginia Commonwealth University School of Medicine, Richmond, Virginia 23298, USA
    J Neurochem 110:1191-202. 2009
    ..These results indicate that CNS S1P receptors are part of a physiologically relevant and widespread neuromodulatory system, and that the S1P(1) receptor contributes to S1P-mediated antinociception...
  13. pmc Sphingosine-1-phosphate receptor subtypes differentially regulate smooth muscle cell phenotype
    Brian R Wamhoff
    Department of Medicine, Cardiovascular Division, University of Virginia, Charlottesville, VA 22901, USA
    Arterioscler Thromb Vasc Biol 28:1454-61. 2008
    ..The role of sphingosine-1-phosphate (S1P) receptors in acute vascular injury and smooth muscle cell (SMC) phenotypic modulation is not completely resolved...
  14. ncbi EDG1 is a functional sphingosine-1-phosphate receptor that is linked via a Gi/o to multiple signaling pathways, including phospholipase C activation, Ca2+ mobilization, Ras-mitogen-activated protein kinase activation, and adenylate cyclase inhibition
    H Okamoto
    Department of Molecular and Cellular Physiology, University of Tokyo Graduate School of Medicine, Tokyo 113 0033, Japan
    J Biol Chem 273:27104-10. 1998
    In Chinese hamster ovary (CHO) cells transiently transfected with an expression vector for EDG1, but not an empty vector, sphingosine-1-phosphate (SP) at a concentration as low as 10(-10) M caused an increase in the intracellular free Ca2+..
  15. ncbi Identification of Edg1 receptor residues that recognize sphingosine 1-phosphate
    A L Parrill
    Department of Chemistry and Computational Research on Materials Institute, University of Memphis, Memphis, Tennessee 38152 6060, USA
    J Biol Chem 275:39379-84. 2000
    Originating from its DNA sequence, a computational model of the Edg1 receptor has been developed that predicts critical interactions with its ligand, sphingosine 1-phosphate...
  16. pmc Inhibitory regulation of Rac activation, membrane ruffling, and cell migration by the G protein-coupled sphingosine-1-phosphate receptor EDG5 but not EDG1 or EDG3
    H Okamoto
    Department of Physiology, Kanazawa University School of Medicine, Kanazawa, Japan
    Mol Cell Biol 20:9247-61. 2000
    ..responses are mediated by members of the EDG (endothelial differentiation gene) family G protein-coupled receptors EDG1, EDG3, and EDG5 (AGR16)...
  17. ncbi EDG1 receptor stimulation leads to cardiac hypertrophy in rat neonatal myocytes
    P Robert
    GlaxoSmithKline Laboratoires Pharmaceutiques, 4 rue du Chesnay Beauregard, 35762 Saint Grégoire, PA, BP 58, France
    J Mol Cell Cardiol 33:1589-606. 2001
    ..6 microM). The effect of S1P could be related to a stimulation of the EDG1 receptor since we showed that the EDG1 receptor is predominantly expressed at the mRNA and protein levels in rat ..
  18. ncbi Role of the sphingosine 1-phosphate receptor EDG-1 in vascular smooth muscle cell proliferation and migration
    M J Kluk
    Center for Vascular Biology, Department of Physiology, University of Connecticut Health Center, Farmington, Connecticut, USA
    Circ Res 89:496-502. 2001
    ..Since EDG-1 is expressed in the pup-intimal phenotype of VSMCs, S1P signaling via EDG-1 may play a role in vascular diseases in which the proliferation and migration of VSMCs are dysregulated...
  19. ncbi Blood lipid mediator sphingosine 1-phosphate potently stimulates platelet-derived growth factor-A and -B chain expression through S1P1-Gi-Ras-MAPK-dependent induction of Kruppel-like factor 5
    Soichiro Usui
    Department of Molecular and Cellular Physiology, Kanazawa University Graduate School of Medical Sciences, 13 1 Takara machi, Kanazawa, Ishikawa 920 8640, Japan
    J Biol Chem 279:12300-11. 2004
    ..of PDGF mRNA and protein expression was abolished by the small interfering RNA duplexes targeting S1P(1)/Edg1 receptor subtype...
  20. ncbi Selective sphingosine 1-phosphate 1 receptor activation reduces ischemia-reperfusion injury in mouse kidney
    Alaa S Awad
    Department of Medicine, Univ of Virginia, Charlottesville, VA, USA
    Am J Physiol Renal Physiol 290:F1516-24. 2006
    ..Sphingosine 1-phosphate (S1P) induces peripheral T cell depletion. Therefore, we hypothesized that S1P1 receptor activation protects kidney from IRI...
  21. ncbi Essential roles of sphingosine 1-phosphate/S1P1 receptor axis in the migration of neural stem cells toward a site of spinal cord injury
    Atsushi Kimura
    Department of Orthopedic Surgery, Jichi Medical University School of Medicine, Tochigi, Japan
    Stem Cells 25:115-24. 2007
    ..This is the first report to identify a physiological role for a lipid mediator in NSPC migration toward a pathological area of the CNS and further indicates that the Sph-1-P/S1P(1) pathway may have therapeutic potential for CNS injuries...
  22. ncbi Candidate genes that determine response to salt in the stroke-prone spontaneously hypertensive rat: congenic analysis
    Delyth Graham
    BHF Glasgow Cardiovascular Research Centre, 126 University Pl, Glasgow, G12 8TA United Kingdom
    Hypertension 50:1134-41. 2007
    ..Examination of expression data within the minimal congenic interval identified the positional candidates Edg1 and Vcam1, demonstrating significantly elevated renal RNA expression levels in the SHRSP compared with WKY and SP...
  23. ncbi Cloning of the rat edg-1 immediate-early gene: expression pattern suggests diverse functions
    D C Lado
    Department of Neuroscience, University of Florida Brain Institute, University of Florida College of Medicine, Gainesville 32610
    Gene 149:331-6. 1994
    ..Therefore, edg-1 may play a cell-type-specific role in differentiation and also participate in neurotransmission...

Research Grants7

  1. Brain Cannabinoid Signaling: Selectivity and Adaptation
    Laura Sim Selley; Fiscal Year: 2006
    ..These studies will contribute to elucidation of the mechanisms of action of CB1 receptors in brain, as well as determine the effects of chronic cannabinoid administration on cellular function during tolerance. ..
  2. Brain Cannabinoid Signaling: Selectivity and Adaptation
    Laura J Sim Selley; Fiscal Year: 2010
    ..This project will determine roles of specific signaling proteins in the effects of acute and long-term CB1R activation by THC and are relevant to cannabinoid therapeutics and drug abuse. ..