Target Information

Target General Infomation
Target ID
T11241
Former ID
TTDI02523
Target Name
Sphingosine-1-phosphate receptor-3
Gene Name
S1PR3
Synonyms
Endothelial differentiation G-protein coupled receptor 3; S1P receptor 3; S1P receptor Edg-3; S1P3; Sphingosine 1-phosphate receptor Edg-3; S1PR3
Target Type
Research
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Function
Receptor for the lysosphingolipid sphingosine 1- phosphate (S1P). S1P is a bioactive lysophospholipid that elicits diverse physiological effect on most types of cells and tissues. When expressed in rat HTC4 hepatoma cells, is capable of mediating S1P-induced cell proliferation and suppression of apoptosis.
BioChemical Class
GPCR rhodopsin
UniProt ID
Q99500
Sequence
MATALPPRLQPVRGNETLREHYQYVGKLAGRLKEASEGSTLTTVLFLVICSFIVLENLMV
LIAIWKNNKFHNRMYFFIGNLALCDLLAGIAYKVNILMSGKKTFSLSPTVWFLREGSMFV
ALGASTCSLLAIAIERHLTMIKMRPYDANKRHRVFLLIGMCWLIAFTLGALPILGWNCLH
NLPDCSTILPLYSKKYIAFCISIFTAILVTIVILYARIYFLVKSSSRKVANHNNSERSMA
LLRTVVIVVSVFIACWSPLFILFLIDVACRVQACPILFKAQWFIVLAVLNSAMNPVIYTL
ASKEMRRAFFRLVCNCLVRGRGARASPIQPALDPSRSKSSSSNNSSHSPKVKEDLPHTAP
SSCIMDKNAALQNGIFCN
Agonist (S)-FTY720-phosphate Drug Info [528529]
AFD(R) Drug Info [526319]
AUY954 Drug Info [528528]
compound 26 Drug Info [527767]
FTY720-phosphate Drug Info [526947]
VPC12249 Drug Info [528528]
Antagonist VPC03090-P Drug Info [531499]
VPC23019 Drug Info [527334]
VPC44116 Drug Info [528528]
Pathways
KEGG Pathway Sphingolipid signaling pathway
Neuroactive ligand-receptor interaction
Pathway Interaction Database S1P3 pathway
Sphingosine 1-phosphate (S1P) pathway
Reactome G alpha (i) signalling events
Lysosphingolipid and LPA receptors
WikiPathways Signal Transduction of S1P Receptor
Small Ligand GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 526319The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem. 2002 Jun 14;277(24):21453-7. Epub 2002 Apr 19.
Ref 526947Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes. J Pharmacol Exp Ther. 2004 May;309(2):758-68. Epub 2004 Jan 27.
Ref 527334Sphingosine 1-phosphate analogs as receptor antagonists. J Biol Chem. 2005 Mar 18;280(11):9833-41. Epub 2004 Dec 8.
Ref 527767Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3. J Med Chem. 2005 Oct 6;48(20):6169-73.
Ref 528528Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists. Bioorg Med Chem. 2007 Jan 15;15(2):663-77. Epub2006 Nov 1.
Ref 528529A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem Biol. 2006 Nov;13(11):1227-34.
Ref 531499Characterization of a sphingosine 1-phosphate receptor antagonist prodrug. J Pharmacol Exp Ther. 2011 Sep;338(3):879-89.
Ref 543708(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 277).

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