Nomenclature: S1P1 receptor

Family: Lysophospholipid (S1P) receptors

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing. 

Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 381 1p21 S1PR1 sphingosine-1-phosphate receptor 1
Mouse 7 382 3 G1 S1pr1 sphingosine-1-phosphate receptor 1
Rat 7 383 2q41 S1pr1 sphingosine-1-phosphate receptor 1
Previous and Unofficial Names
edg1
lpB1
edg-1
D1S3362
CD363
endothelial differentiation, sphingolipid G-protein-coupled receptor, 1
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
sphingosine-1-phosphate receptor 1
S1P
AI849002
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the S1P1 receptor in complex with sphingolipid mimic ML056
PDB Id:  3V2W
Ligand:  W146
Resolution:  3.35Å
Species:  Human
References:  15
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the S1P1 receptor in complex with sphingolipid mimic ML056
PDB Id:  3V2Y
Ligand:  W146
Resolution:  2.8Å
Species:  Human
References:  15
Natural/Endogenous Ligands
sphingosine 1-phosphate
sphingosylphosphorylcholine
Comments: sphingosine 1-phosphate exhibits greater potency than sphingosylphosphorylcholine. LPA is a low potency agonist.
Rank order of potency
sphingosine 1-phosphate > dihydrosp​hingosine​-1-phosph​ate > sphingosylphosphorylcholine  [5,25]
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
sphingosine 1-phosphate Hs Agonist 7.88 – 9.41 pKd 10,19
pKd 7.88 – 9.41 (Kd 3.9x10-10 – 1.32x10-8 M) [10,19]
LPA Hs Agonist 5.6 pKd 20
pKd 5.6 [20]
SEW2871 Hs Agonist 5.5 – 7.7 pKi 30
pKi 5.5 – 7.7 (Ki 1.8x10-8 – 2.89x10-6 M) [30]
KRP 203-phosphate Mm Agonist 9.07 pEC50 32
pEC50 9.07 [32]
AUY954 Mm Agonist 9.05 pEC50 27
pEC50 9.05 (EC50 9x10-10 M) [27]
AUY954 Hs Agonist 8.92 pEC50 27
pEC50 8.92 (EC50 1.2x10-9 M) [27]
CYM-5442 Hs Agonist 8.91 pEC50 14
pEC50 8.91 [14]
sphingosine 1-phosphate Mm Agonist 8.85 pEC50 27,30
pEC50 8.85 (EC50 1.4x10-9 M) [27,30]
FTY720-phosphate Mm Agonist 8.2 – 9.5 pEC50 6,32
pEC50 8.2 – 9.5 [6,32]
FTY720-phosphate Hs Agonist 8.1 – 9.52 pEC50 6,12,27
pEC50 9.52 (EC50 3x10-10 M) [12,27]
pEC50 8.1 – 8.2 [6]
AFD(R) Hs Agonist 8.4 – 8.8 pEC50 6
pEC50 8.4 – 8.8 [6]
CYM5181 Hs Agonist 8.47 pEC50 14
pEC50 8.47 [14]
sphingosine 1-phosphate Hs Agonist 7.1 – 9.4 pEC50 6,16,25,27,30
pEC50 7.1 – 9.4 (EC50 4x10-10 – 1x10-9 M) [6,16,25,27,30]
SEW2871 Hs Agonist 7.54 – 7.86 pEC50 14,30
pEC50 7.54 – 7.86 [14,30]
SEW2871 Mm Agonist 7.68 pEC50 30
pEC50 7.68 (EC50 2.07x10-8 M) [30]
FTY720-phosphate Hs Agonist 9.52 pIC50 12
pIC50 9.52 (IC50 3x10-10 M) [12]
compound 26 [PMID:16190743] Hs Agonist 9.22 pIC50 21
pIC50 9.22 [21]
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
NIBR-0213 Hs Antagonist 9.43 pKd 29
pKd 9.43 (Kd 3.7x10-10 M) [29]
VPC44116 Hs Antagonist 8.52 pKi 13
pKi 8.52 (Ki 3x10-9 M) [13]
VPC03090-P Mm Antagonist 7.67 – 7.85 pKi 18
pKi 7.67 – 7.85 (Ki 1.4x10-8 – 2.13x10-8 M) [18]
VPC03090-P Hs Antagonist 7.62 – 7.68 pKi 18
pKi 7.62 – 7.68 (Ki 2.1x10-8 – 2.4x10-8 M) [18]
W146 Hs Antagonist 7.11 pKi 31
pKi 7.11 (Ki 7.7x10-8 M) [31]
VPC44116 Hs Antagonist 7.57 pEC50 13
pEC50 7.57 [13]
NIBR-0213 Hs Antagonist 8.6 pIC50 29
pIC50 8.6 (IC50 2.5x10-9 M) [29]
View species-specific antagonist tables
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Adenylate cyclase inhibition
Phospholipase C stimulation
Calcium channel
Phospholipase D stimulation
Other - See Comments
Comments:  Involved in ERK phosphorylation [26] and stimulation of the PI3K/PKB and MEK/ERK pathways [7], and activation of Rac [11].
References:  8,19,25
Tissue Distribution
Brain, heart, lung, liver, spleen, kidney, thymus, and muscle
Species:  Mouse
Technique:  Northern blot
References:  34
Naive T cell and regulatory T cell
Species:  Mouse
Technique:  RT-PCR
References:  33
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Physiological Consequences of Altering Gene Expression
Blockade in the egress of mature T-cells into the periphery in knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockouts
References:  1,24
Attenuation of autoimmune demyelination in astrocyte specific receptor knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockouts
References:  9
Blockade of plasma cell homing and immature B cell migration in knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockouts
References:  2,17,28
Reduction of NKT cells distribution in peripheral tissues
Species:  Mouse
Tissue: 
Technique:  Gene knockouts
References:  4
Blockade of regulatory T cell differenciation in knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockouts
References:  22
Embryonic lethality, defective vascular maturation due to lack of pericytes and alterations in signalling indicated by a decrease in Rac-mediated chemotaxis
Species:  Mouse
Tissue: 
Technique:  Gene targeting:- replacement vector, deletion of ORF, creation of s1p1–LacZ hybrid transcript
References:  23
Incomplete vascular maturation
Species:  Mouse
Tissue: 
Technique:  Gene knockouts
References:  3,23
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
S1pr1tm1Rlp|S1pr2tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:99569  MP:0000260 abnormal angiogenesis PMID: 15138255 
S1pr1tm1Rlp|S1pr2tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MGI:99569  MP:0000260 abnormal angiogenesis PMID: 15138255 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0009865 abnormal aorta smooth muscle morphology PMID: 15138255 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0001614 abnormal blood vessel morphology PMID: 11032855 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0002127 abnormal cardiovascular system morphology PMID: 12869509 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0001544 abnormal cardiovascular system physiology PMID: 12869509 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0003091 abnormal cell migration PMID: 11032855 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac
MGI:1096355  MP:0000830 abnormal diencephalon morphology PMID: 16314531 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac
MGI:1096355  MP:0000783 abnormal forebrain morphology PMID: 16314531 
S1pr1tm1.1Thla S1pr1tm1.1Thla/S1pr1tm1.1Thla
B6.Cg-S1pr1
MGI:1096355  MP:0003156 abnormal leukocyte migration PMID: 20584883 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0002109 abnormal limb morphology PMID: 12869509 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0002109 abnormal limb morphology PMID: 11032855  15138255 
S1pr1tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MP:0002109 abnormal limb morphology PMID: 15138255 
S1pr1tm1.1Thla S1pr1tm1.1Thla/S1pr1tm1.1Thla
B6.Cg-S1pr1
MGI:1096355  MP:0003945 abnormal lymphocyte physiology PMID: 20584883 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac
MGI:1096355  MP:0008053 abnormal NK cell differentiation PMID: 19808259 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0003719 abnormal pericyte morphology PMID: 11032855 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac
MGI:1096355  MP:0000787 abnormal telencephalon morphology PMID: 16314531 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0006055 abnormal vascular endothelial cell morphology PMID: 11032855 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0005592 abnormal vascular smooth muscle morphology PMID: 11032855 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0001718 abnormal yolk sac morphology PMID: 12869509 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0001718 abnormal yolk sac morphology PMID: 11032855 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac
MGI:1096355  MP:0008045 decreased NK cell number PMID: 19808259 
S1pr1tm1.1Thla S1pr1tm1.1Thla/S1pr1tm1.1Thla
B6.Cg-S1pr1
MGI:1096355  MP:0008874 decreased physiological sensitivity to xenobiotic PMID: 20584883 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0001785 edema PMID: 11032855 
S1pr1tm1Rlp|S1pr2tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:99569  MP:0006207 embryonic lethality during organogenesis PMID: 15138255 
S1pr1tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MP:0006207 embryonic lethality during organogenesis PMID: 15138255 
S1pr1tm1Rlp|S1pr2tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MGI:99569  MP:0006207 embryonic lethality during organogenesis PMID: 15138255 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0000291 enlarged pericardium PMID: 12869509 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0000291 enlarged pericardium PMID: 11032855 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0001914 hemorrhage PMID: 12869509 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0001914 hemorrhage PMID: 11032855  15138255 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac
MGI:1096355  MP:0001914 hemorrhage PMID: 16314531 
S1pr1tm1Rlp|S1pr2tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:99569  MP:0001914 hemorrhage PMID: 15138255 
S1pr1tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MP:0001914 hemorrhage PMID: 15138255 
S1pr1tm1Rlp|S1pr2tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MGI:99569  MP:0001914 hemorrhage PMID: 15138255 
S1pr1tm1.1Thla S1pr1tm1.1Thla/S1pr1tm1.1Thla
B6.Cg-S1pr1
MGI:1096355  MP:0008074 increased CD4-positive T cell number PMID: 20584883 
S1pr1tm1.1Thla S1pr1tm1.1Thla/S1pr1tm1.1Thla
B6.Cg-S1pr1
MGI:1096355  MP:0008078 increased CD8-positive T cell number PMID: 20584883 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0006208 lethality throughout fetal growth and development PMID: 12869509 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0006208 lethality throughout fetal growth and development PMID: 11032855  15138255 
S1pr1tm2Rlp S1pr1tm2Rlp/S1pr1tm2Rlp
involves: 129S6/SvEvTac
MGI:1096355  MP:0002169 no abnormal phenotype detected PMID: 12869509 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0001787 pericardial edema PMID: 11032855 
S1pr1tm1Rlp|S1pr1tm2Rlp|Tg(Tek-cre)1Ywa S1pr1tm1Rlp/S1pr1tm2Rlp,Tg(Tek-cre)1Ywa/?
involves: 129S6/SvEvTac * C57BL/6 * SJL
MGI:1096355  MGI:2450309  MP:0000262 poor arterial differentiation PMID: 12869509 
S1pr1tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MP:0003814 vascular smooth muscle cell hypoplasia PMID: 11032855 
Available Assays
DiscoveRx PathHunter® CHO-K1 EDG1 β-Arrestin Cell Line (Cat no. 93-0207C2)
PathHunter® eXpress EDG1 CHO-K1 β-Arrestin GPCR Assay (Cat no. 93-0207E2CP4M)
more info

REFERENCES

1. Allende ML, Dreier JL, Mandala S, Proia RL. (2004) Expression of the sphingosine 1-phosphate receptor, S1P1, on T-cells controls thymic emigration. J. Biol. Chem.279 (15): 15396-401. [PMID:14732704]

2. Allende ML, Tuymetova G, Lee BG, Bonifacino E, Wu YP, Proia RL. (2010) S1P1 receptor directs the release of immature B cells from bone marrow into blood. J. Exp. Med.207 (5): 1113-24. [PMID:20404103]

3. Allende ML, Yamashita T, Proia RL. (2003) G-protein-coupled receptor S1P1 acts within endothelial cells to regulate vascular maturation. Blood102 (10): 3665-7. [PMID:12869509]

4. Allende ML, Zhou D, Kalkofen DN, Benhamed S, Tuymetova G, Borowski C, Bendelac A, Proia RL. (2008) S1P1 receptor expression regulates emergence of NKT cells in peripheral tissues. FASEB J.22 (1): 307-15. [PMID:17785606]

5. Ancellin N, Hla T. (1999) Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5. J. Biol. Chem.274 (27): 18997-9002. [PMID:10383399]

6. Brinkmann V, Davis MD, Heise CE, Albert R, Cottens S, Hof R, Bruns C, Prieschl E, Baumruker T, Hiestand P et al.. (2002) The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J. Biol. Chem.277 (24): 21453-7. [PMID:11967257]

7. Brizuela L, Rábano M, Gangoiti P, Narbona N, Macarulla JM, Trueba M, Gómez-Muñoz A. (2007) Sphingosine-1-phosphate stimulates aldosterone secretion through a mechanism involving the PI3K/PKB and MEK/ERK 1/2 pathways. J. Lipid Res.48 (10): 2264-74. [PMID:17609523]

8. Brizuela L, Rábano M, Peña A, Gangoiti P, Macarulla JM, Trueba M, Gómez-Muñoz A. (2006) Sphingosine 1-phosphate: a novel stimulator of aldosterone secretion. J. Lipid Res.47 (6): 1238-49. [PMID:16554657]

9. Choi JW, Gardell SE, Herr DR, Rivera R, Lee CW, Noguchi K, Teo ST, Yung YC, Lu M, Kennedy G et al.. (2011) 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.108 (2): 751-6. [PMID:21177428]

10. Deng Q, Clemas JA, Chrebet G, Fischer P, Hale JJ, Li Z, Mills SG, Bergstrom J, Mandala S, Mosley R et al.. (2007) 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. Mol. Pharmacol.71 (3): 724-35. [PMID:17170199]

11. Faroudi M, Hons M, Zachacz A, Dumont C, Lyck R, Stein JV, Tybulewicz VL. (2010) Critical roles for Rac GTPases in T-cell migration to and within lymph nodes. Blood116 (25): 5536-47. [PMID:20870900]

12. Forrest M, Sun SY, Hajdu R, Bergstrom J, Card D, Doherty G, Hale J, Keohane C, Meyers C, Milligan J et al.. (2004) Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes. J. Pharmacol. Exp. Ther.309 (2): 758-68. [PMID:14747617]

13. Foss FW, Snyder AH, Davis MD, Rouse M, Okusa MD, Lynch KR, Macdonald TL. (2007) Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists. Bioorg. Med. Chem.15 (2): 663-77. [PMID:17113298]

14. Gonzalez-Cabrera PJ, Jo E, Sanna MG, Brown S, Leaf N, Marsolais D, Schaeffer MT, Chapman J, Cameron M, Guerrero M et al.. (2008) Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like headgroup interactions. Mol. Pharmacol.74 (5): 1308-18. [PMID:18708635]

15. Hanson MA, Roth CB, Jo E, Griffith MT, Scott FL, Reinhart G, Desale H, Clemons B, Cahalan SM, Schuerer SC et al.. (2012) Crystal structure of a lipid G protein-coupled receptor. Science335 (6070): 851-5. [PMID:22344443]

16. Im DS, Clemens J, Macdonald TL, Lynch KR. (2001) Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors. Biochemistry40 (46): 14053-60. [PMID:11705398]

17. Kabashima K, Haynes NM, Xu Y, Nutt SL, Allende ML, Proia RL, Cyster JG. (2006) Plasma cell S1P1 expression determines secondary lymphoid organ retention versus bone marrow tropism. J. Exp. Med.203 (12): 2683-90. [PMID:17101733]

18. Kennedy PC, Zhu R, Huang T, Tomsig JL, Mathews TP, David M, Peyruchaud O, Macdonald TL, Lynch KR. (2011) Characterization of a sphingosine 1-phosphate receptor antagonist prodrug. J. Pharmacol. Exp. Ther.338 (3): 879-89. [PMID:21632869]

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To cite this database page, please use the following:

Jerold Chun, Yasuyuki Kihara, Chido Mpamhanga.
Lysophospholipid (S1P) receptors: S1P1 receptor. Last modified on 31/03/2014. Accessed on 26/07/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=275.

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