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S1P1 receptor

Family: Lysophospholipid (S1P) receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Selected 3D Structures
Agonists
Antagonists
Transduction Mechanisms
Expression Datasets
Physiological Consequences of Altering Gene Expression
Phenotypes, Alleles and Disease Models
References
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
S1P
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
AI849002
Database Links
ChEMBL Target
Ensembl
Entrez Gene
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.
UniProt
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:  3V2Y
Resolution:  2.8Å
Species:  Human
References:  7
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the S1P1 receptor in complex with sphingolipid mimic ML056
PDB Id:  3V2W
Resolution:  3.35Å
Species:  Human
References:  7
Search for other structures on the PDB
Search by keyword: Lysophospholipid (S1P) receptors S1P1 receptor
Natural/Endogenous Ligand(s)
sphingosine 1-phosphate
sphingosyl phosphorylcholine
Rank order of potency
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
LPA Hs Agonist 5.6 pKd 10
SEW2871 Hs Agonist 5.5 – 7.7 pKi 17
KRP 203-phosphate Mm Agonist 9.07 pEC50 18
AUY954 Mm Agonist 9.04 pEC50 15
AUY954 Hs Agonist 8.92 pEC50 15
CYM-5442 Hs Agonist 8.91 pEC50 6
FTY720-phosphate Mm Agonist 8.2 – 9.5 pEC50 2,18
AFD(R) Hs Agonist 8.6 pEC50 2
CYM5181 Hs Agonist 8.41 pEC50 6
sphingosine 1-phosphate Hs Agonist 7.1 – 9.05 pEC50 2,8
SEW2871 Hs Agonist 7.54 pEC50 6
analogue26_3,5-diphenyl-1,2,4-oxadiazole Hs Agonist 9.22 pIC50 11
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
W146 Hs Antagonist 7.7 pKi 16-17
VPC44116 Hs Antagonist 7.57 pEC50 5
Primary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family Phospholipase C stimulation
Calcium channel
Phospholipase D stimulation
Other - See Comments
Comments:  involved in ERK phosphorylation[14] and stimulation of the PI3K/PKB and MEK/ERK pathways [3]
References:  4,9,13
Expression Datasets

Click here to show/hide data

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
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:  12
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 

REFERENCES

To cite this database page, please use the following:

Chido Mpamhanga.
Lysophospholipid (S1P) receptors: S1P1 receptor. Last modified on 31/01/2013. Accessed on 22/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=275.


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