Property Summary

NCBI Gene PubMed Count 67
PubMed Score 148.37
PubTator Score 86.68

Knowledge Summary

Patent (18,250)

Expression

MLP Assay (18)

AID Type Active / Inconclusive / Inactive Description
373 screening 62 / 0 / 59743 S1P3 Agonist Primary HTS and Confirmation Assays
439 confirmatory 13 / 0 / 56 S1P3 Agonist Dose-Response Potency Assay
484 confirmatory 14 / 0 / 182 Dose Response Assay for S1P3 Antagonists
485 screening 462 / 0 / 168776 Primary HTS Assay for S1P3 Antagonists
730 confirmatory 1 / 0 / 50 S1P3 Dose Response Assay Counterscreen for 5-Hydroxytryptamine(Serotonin) Receptor Subtype 1E Agonists
776 confirmatory 21 / 0 / 23 S1P3 Dose Response Assay Counterscreen for 5-Hydroxytryptamine(Serotonin) Receptor Subtype 1E Antagonists
1192 confirmatory 2 / 0 / 8 Dose Response Cell-Based Assay for Agonists of the Sphingosine 1-Phosphate Receptor 3 (S1P3): Purchased Analogues
1429 screening 63 / 0 / 174 Confirmation cell-based assay to identify antagonists of the Sphingosine 1-Phosphate Receptor 3 (S1P3)
1518 confirmatory 17 / 0 / 14 Dose response cell-based high throughput screening assay for antagonists of the Sphingosine 1-Phosphate Receptor 3 (S1P3)
1820 summary 0 / 0 / 0 Summary of probe development efforts to identify antagonists of Sphingosine 1-Phosphate Receptor 3 (S1P3)
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Gene RIF (40)

PMID Text
25971967 TRPC1 functions as a major regulator of S1P3 and VEGFR2 expression.
25832730 S1pr3 promotes leukocyte rolling by mobilization of endothelial P-selectin.
25254944 Stimulation with sphingosine-1-phosphate enhances cancer stem cells via S1PR3 and subsequent Notch1 activation.
24903384 Data show that sphingosine kinase SphK1 and sphingosine-1-phosphate (S1P) receptors S1P1, S1P2, S1P3, and S1P5 were expressed from primary, up to recurrent and secondary glioblastomas, with sphingosine kinase SphK2 levels were highest in primary tumors.
24851274 Data indicate that sphingosine 1-phosphate (S1P) and hepatocyte growth factor (HGF) induced transloaction of integrin beta4, S1P receptors S1PR2 and S1PR3 to endothelial cell membrane caveolin-enriched microdomains (CEMs).
24064218 a novel signaling axis, i.e., ROCK-JNK-ETS-1-CD44 pathway, which plays an essential role in the S1P3-regulated chemotactic response.
24038457 we provide evidences that S1PR1/3, but not S1PR2, negatively regulate the expression of collagen in hMSCs using cellular and molecular approaches in vitro
23918395 Sphingosine 1-phosphate receptor 3 regulates recruitment of anti-inflammatory monocytes to microvessels during implant arteriogenesis.
23911438 associations were found for 2 promoter SNPs across 2 European descent samples supporting association of alleles -1899G and -1785C with decreased risk for sepsis-associated acute respiratory distress syndrome (ARDS); alleles reduced transcription factor binding to S1PR3 promoter and S1PR3 promoter activity; associated with lower plasma S1PR3 protein in ARDS patients
23589284 S1PR agonists are pro-fibrotic via S1P2R and S1P3R stimulation using Smad-independent pathways.
23466305 key role of Sphk1, S1PR1 and S1PR3 in angiogenesis underlying the liver fibrosis process
23392686 S1P3 receptors are detected in virtually all neurons in dorsal root ganglion and mediate pain behavior.
23142484 Inhibition of S1P3 receptors prevented E2-induced activation of Cdc42, supporting the important role of the S1P receptor in E2 signaling.
22889737 S1P receptors S1P1,2,3 are expressed in human anaplastic thyroid cancer C643 and THJ-16T cells at both mRNA and protein levels
22771388 S1PR3 is nitrated on specific tyrosine residues and released as endothelial cell microparticles during acute lung injury.
22595806 However, growing evidence strongly suggests that the assessment of Sphingosine-1-phosphate receptor 1/3 (S1P1/3) own advantages over present measurements in predicting the risk of developing diabetic cardiovascular diseases.
22547907 abdominal aortic aneurysms have down-regulation of the S1P2 protein with simultaneous up-regulation of the S1P3 protein, but not S1P1
22344462 Suggest that the enhanced S1P3-EGFR signaling axis may contribute to the tumorigenesis or progression of lung adenocarcinomas.
22308044 S1PR3 was higher in iliac-femoral arteries compared with carotid arteries.
21660960 These data have identified an additional function regulated by S1P/S1PR1,3 axis involving migration and fibrogenic activation of hepatic stellate cells.
21652634 S1P regulates MMP-9 induction and invasiveness through coupling of S1P3 and G(alphaq) in MCF10A cells, thus providing a molecular basis for the crucial role of S1P in promoting breast cell invasion.
21145832 SphK/S1P/S1PRs signaling axis plays an important role in liver fibrosis and is involved in the directed migration of hepatic myofibroblasts into the damaged areas.
20980685 The follicular fluid-HDL-associated S1P promotes granulosa lutein cell migration via S1PR3 and RAC1 activation. This may represent a novel mechanism contributing to the development of the corpus luteum.
20979115 These results suggest a potential role for HDL and S1P receptors in the pathogenesis of prostate cancer.
20889557 These results support a model in which the interaction between sphingosine kinase 1, sphingosine 1-phosphate receptors 1 and/or 3, and ERK-1/2 might drive breast cancer progression
20648639 this study demonstrated that reactive astrocytes in MS lesions and cultured under proinflammatory conditions strongly enhance expression of S1P receptors 1 and 3.
20628086 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
19913121 Observational study of gene-disease association. (HuGE Navigator)
19748727 amplification of SHC3 and EDG3 genes suggests that the two proteins co-operate and are important for ependymomas in vivo.
19633297 IGFBP-3 in MCF-10A cells requires SphK1 activity and S1P1/S1P3, suggesting that S1P, the product of SphK activity and ligand for S1P1 and S1P3
19309361 Report different response patterns of several ligands at the sphingosine-1-phosphate receptor subtype 3 (S1P(3)).
18658144 Plays essential roles in the pathogenesis of rheumatoid arthritis by modulating fibroblast-like synoviocyte migration, cytokine/chemokine production, and cell survival.
18612546 Results suggest that S1PR3 is involved in COX2 dependent effects of high-density lipoprotein on vascular smooth muscle.
18502815 Cytosolic phospholipase A2alpha activation induced by S1P is mediated by the S1P3 receptor in lung epithelial cells.(
17395891 Reults describe the role of mu opioid receptors and S1P3 transactivation in the attenuation of vascular permeability by methylnaltrexone.
17331465 Sphingosine 1-phosphate-induced inflammatory response genes expression is mediated through S1P(1) and S1P(3)
16527273 Expression of the sphingosine 1 phosphate receptor in primary endothelial cells is both sufficient and necessary for the expression of Akt3.
15894172 S1P(3) function is not subject to conventional regulation by GRK phosphorylation
12763936 a 9-amino acid peptide (KRX-725), derived from the second intracellular loop of S1P3 (EDG3) mimics sphingosine 1-phosphate (S1P) by triggering a Gi-dependent mitogen-activated protein kinase kinase and extracellular signal-regulated kinase signal.
11915348 activates Rho family G proteins and cell motility

AA Sequence

MATALPPRLQPVRGNETLREHYQYVGKLAGRLKEASEGSTLTTVLFLVICSFIVLENLMVLIAIWKNNKF      1 - 70
HNRMYFFIGNLALCDLLAGIAYKVNILMSGKKTFSLSPTVWFLREGSMFVALGASTCSLLAIAIERHLTM     71 - 140
IKMRPYDANKRHRVFLLIGMCWLIAFTLGALPILGWNCLHNLPDCSTILPLYSKKYIAFCISIFTAILVT    141 - 210
IVILYARIYFLVKSSSRKVANHNNSERSMALLRTVVIVVSVFIACWSPLFILFLIDVACRVQACPILFKA    211 - 280
QWFIVLAVLNSAMNPVIYTLASKEMRRAFFRLVCNCLVRGRGARASPIQPALDPSRSKSSSSNNSSHSPK    281 - 350
VKEDLPHTAPSSCIMDKNAALQNGIFCN                                              351 - 378
//

Text Mined References (70)

PMID Year Title
25971967 2015 Transient Receptor Potential Canonical 1 (TRPC1) Channels as Regulators of Sphingolipid and VEGF Receptor Expression: IMPLICATIONS FOR THYROID CANCER CELL MIGRATION AND PROLIFERATION.
25832730 2015 Sphingosine-1-phosphate receptor 3 promotes leukocyte rolling by mobilizing endothelial P-selectin.
25254944 2014 Sphingosine-1-phosphate promotes expansion of cancer stem cells via S1PR3 by a ligand-independent Notch activation.
24903384 2014 The role of sphingosine kinase isoforms and receptors S1P1, S1P2, S1P3, and S1P5 in primary, secondary, and recurrent glioblastomas.
24851274 2014 Interaction of integrin ?4 with S1P receptors in S1P- and HGF-induced endothelial barrier enhancement.
24602016 2014 Lysophospholipid receptor nomenclature review: IUPHAR Review 8.
24064218 2013 ETS-1-mediated transcriptional up-regulation of CD44 is required for sphingosine-1-phosphate receptor subtype 3-stimulated chemotaxis.
24038457 2014 Sphingosine 1-phosphate receptors negatively regulate collagen type I/III expression in human bone marrow-derived mesenchymal stem cell.
23918395 2013 Sphingosine 1-phosphate receptor 3 regulates recruitment of anti-inflammatory monocytes to microvessels during implant arteriogenesis.
23911438 2013 Functional promoter variants in sphingosine 1-phosphate receptor 3 associate with susceptibility to sepsis-associated acute respiratory distress syndrome.
23589284 2013 Sphingosine 1-phosphate (S1P) receptor agonists mediate pro-fibrotic responses in normal human lung fibroblasts via S1P2 and S1P3 receptors and Smad-independent signaling.
23466305 2013 Sphingosine kinase/sphingosine 1-phosphate (S1P)/S1P receptor axis is involved in liver fibrosis-associated angiogenesis.
23392686 2013 Sphingosine-1-phosphate-induced nociceptor excitation and ongoing pain behavior in mice and humans is largely mediated by S1P3 receptor.
23186163 2013 Toward a comprehensive characterization of a human cancer cell phosphoproteome.
23142484 2013 Estrogen defines the dynamics and destination of transactivated EGF receptor in breast cancer cells: role of S1P? receptor and Cdc42.
22889737 2012 Sphingosine 1-phosphate and human ether-a'-go-go-related gene potassium channels modulate migration in human anaplastic thyroid cancer cells.
22771388 2012 Sphingosine-1-phosphate receptor-3 is a novel biomarker in acute lung injury.
22595806 2012 S1P1 and S1P3 are potential markers of cardiac microangiopathy in diabetes.
22547907 2012 Differential expression of sphingosine-1-phosphate receptors in abdominal aortic aneurysms.
22344462 2012 Sphingosine-1-phosphate receptor-3 signaling up-regulates epidermal growth factor receptor and enhances epidermal growth factor receptor-mediated carcinogenic activities in cultured lung adenocarcinoma cells.
22331829 2012 Genetic determinants of statin-induced low-density lipoprotein cholesterol reduction: the Justification for the Use of Statins in Prevention: an Intervention Trial Evaluating Rosuvastatin (JUPITER) trial.
22308044 2012 Sphingosine-1-phosphate receptor 3 promotes neointimal hyperplasia in mouse iliac-femoral arteries.
21660960 2011 Essential roles of sphingosine 1-phosphate receptor types 1 and 3 in human hepatic stellate cells motility and activation.
21652634 2011 Sphingosine 1-phosphate regulates matrix metalloproteinase-9 expression and breast cell invasion through S1P3-G?q coupling.
21145832 2011 Sphingosine 1-phosphate (S1P)/S1P receptors are involved in human liver fibrosis by action on hepatic myofibroblasts motility.
20980685 2011 Follicular fluid high-density lipoprotein-associated sphingosine 1-phosphate (S1P) promotes human granulosa lutein cell migration via S1P receptor type 3 and small G-protein RAC1.
20979115 2011 HDL and sphingosine-1-phosphate activate stat3 in prostate cancer DU145 cells via ERK1/2 and S1P receptors, and promote cell migration and invasion.
20889557 2010 High expression of sphingosine 1-phosphate receptors, S1P1 and S1P3, sphingosine kinase 1, and extracellular signal-regulated kinase-1/2 is associated with development of tamoxifen resistance in estrogen receptor-positive breast cancer patients.
20648639 2010 Sphingosine 1-phosphate receptor 1 and 3 are upregulated in multiple sclerosis lesions.
20628086 2010 Variation at the NFATC2 locus increases the risk of thiazolidinedione-induced edema in the Diabetes REduction Assessment with ramipril and rosiglitazone Medication (DREAM) study.
19913121 2009 Gene-centric association signals for lipids and apolipoproteins identified via the HumanCVD BeadChip.
19748727 2010 EDG3 and SHC3 on chromosome 9q22 are co-amplified in human ependymomas.
19633297 2009 Potentiation of growth factor signaling by insulin-like growth factor-binding protein-3 in breast epithelial cells requires sphingosine kinase activity.
19309361 2009 Different response patterns of several ligands at the sphingosine-1-phosphate receptor subtype 3 (S1P(3)).
18658144 2008 Specific and overlapping sphingosine-1-phosphate receptor functions in human synoviocytes: impact of TNF-alpha.
18612546 2008 Prostacyclin induction by high-density lipoprotein (HDL) in vascular smooth muscle cells depends on sphingosine 1-phosphate receptors: effect of simvastatin.
18577758 2008 Dissociation of heterotrimeric g proteins in cells.
18502815 2008 Cytosolic phospholipase A2alpha activation induced by S1P is mediated by the S1P3 receptor in lung epithelial cells.
17395891 2007 Attenuation of vascular permeability by methylnaltrexone: role of mOP-R and S1P3 transactivation.
17331465 2007 Sphingosine 1-phosphate regulates inflammation-related genes in human endothelial cells through S1P1 and S1P3.
16527273 2006 Modulation of total Akt kinase by increased expression of a single isoform: requirement of the sphingosine-1-phosphate receptor, Edg3/S1P3, for the VEGF-dependent expression of Akt3 in primary endothelial cells.
16344560 2006 Diversification of transcriptional modulation: large-scale identification and characterization of putative alternative promoters of human genes.
15894172 2005 Phosphorylation-independent internalisation and desensitisation of the human sphingosine-1-phosphate receptor S1P3.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
15164053 2004 DNA sequence and analysis of human chromosome 9.
14702039 2004 Complete sequencing and characterization of 21,243 full-length human cDNAs.
12763936 2003 Induction of pro-angiogenic signaling by a synthetic peptide derived from the second intracellular loop of S1P3 (EDG3).
12648236 2003 Sphingosine-1-phosphate and its potentially paradoxical effects on critical parameters of cutaneous wound healing.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12039947 2002 Phospholipase D activation by sphingosine 1-phosphate regulates interleukin-8 secretion in human bronchial epithelial cells.
11915348 2002 [Regulation of Rho family G proteins and cell motility by the Edg family of sphingosin 1-phosphate receptors].
11854302 2002 Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation.
10908314 2000 Evidence for Edg-3 receptor-mediated activation of I(K.ACh) by sphingosine-1-phosphate in human atrial cardiomyocytes.
10818450 2000 Phospholipid growth factors and corneal wound healing.
10818441 2000 Sphingosine 1-phosphate: a ligand for the EDG-1 family of G-protein-coupled receptors.
10818438 2000 Sphingosine-1-phosphate signaling via the EDG-1 family of G-protein-coupled receptors.
10794715 2000 Sphingosine 1-phosphate stimulates proliferation and migration of human endothelial cells possibly through the lipid receptors, Edg-1 and Edg-3.
10712250 2000 Lysophosphatidic acid and sphingosine 1-phosphate stimulate endothelial cell wound healing.
10683250 2000 Sphingosine-1-phosphate activates phospholipase D in human airway epithelial cells via a G protein-coupled receptor.
10617617 2000 Sphingosine 1-phosphate-induced cell proliferation, survival, and related signaling events mediated by G protein-coupled receptors Edg3 and Edg5.
10555146 1999 Vascular endothelial cell adherens junction assembly and morphogenesis induced by sphingosine-1-phosphate.
10537322 1999 Distinctive expression and functions of the type 4 endothelial differentiation gene-encoded G protein-coupled receptor for lysophosphatidic acid in ovarian cancer.
10488065 1999 Differential coupling of the sphingosine 1-phosphate receptors Edg-1, Edg-3, and H218/Edg-5 to the G(i), G(q), and G(12) families of heterotrimeric G proteins.
10383399 1999 Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5.
10216094 1999 Sphingosine 1-phosphate stimulates fibronectin matrix assembly through a Rho-dependent signal pathway.
9988698 1999 Sphingosine 1-phosphate-induced cell rounding and neurite retraction are mediated by the G protein-coupled receptor H218.
9409733 1997 Identification of cDNAs encoding two G protein-coupled receptors for lysosphingolipids.
8878560 1996 Molecular cloning of the novel human G protein-coupled receptor (GPCR) gene mapped on chromosome 9.
8649355 1996 A distinct G(i) protein-coupled receptor for sphingosylphosphorylcholine in human leukemia HL-60 cells and human neutrophils.
2834384 1988 Presence of three distinct molecular species of Gi protein alpha subunit. Structure of rat cDNAs and human genomic DNAs.