Target Information

Target General Infomation
Target ID
T50089
Former ID
TTDI02167
Target Name
Sphingosine 1-phosphate receptor 5
Gene Name
S1PR5
Synonyms
Endothelial differentiation G-protein-coupled receptor 8; S1P receptor 5; S1P receptor Edg-8; S1P5; Sphingosine 1-phosphate receptor Edg-8; S1PR5
Target Type
Clinical Trial
Disease Multiple scierosis [ICD9: 340; ICD10: G35]
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. Is coupled to both the G(i/0)alpha and G(12) subclass of heteromeric G-proteins (By similarity). May play a regulatory role in the transformation of radial glial cells into astrocytes and may affect proliferative activity of these cells.
BioChemical Class
GPCR rhodopsin
UniProt ID
Q9H228
Sequence
MESGLLRPAPVSEVIVLHYNYTGKLRGARYQPGAGLRADAVVCLAVCAFIVLENLAVLLV
LGRHPRFHAPMFLLLGSLTLSDLLAGAAYAANILLSGPLTLKLSPALWFAREGGVFVALT
ASVLSLLAIALERSLTMARRGPAPVSSRGRTLAMAAAAWGVSLLLGLLPALGWNCLGRLD
ACSTVLPLYAKAYVLFCVLAFVGILAAICALYARIYCQVRANARRLPARPGTAGTTSTRA
RRKPRSLALLRTLSVVLLAFVACWGPLFLLLLLDVACPARTCPVLLQADPFLGLAMANSL
LNPIIYTLTNRDLRHALLRLVCCGRHSCGRDPSGSQQSASAAEASGGLRRCLPPGLDGSF
SGSERSSPQRDGLDTSGSTGSPGAPTAARTLVSEPAAD
Drugs and Mode of Action
Drug(s) ASP-4058 Drug Info Phase 1 Multiple scierosis [533005]
Agonist AFD(R) Drug Info [526934]
AUY954 Drug Info [528529]
compound 26 Drug Info [527767]
FTY720-phosphate Drug Info [526947]
VPC03090-P Drug Info [531499]
VPC44116 Drug Info [528528]
Modulator ASP-4058 Drug Info [533005]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Sphingolipid signaling pathway
Neuroactive ligand-receptor interaction
Pathway Interaction Database S1P4 pathway
S1P5 pathway
Sphingosine 1-phosphate (S1P) pathway
Reactome G alpha (i) signalling events
Lysosphingolipid and LPA receptors
WikiPathways Signal Transduction of S1P Receptor
GPCR ligand binding
GPCR downstream signaling
References
Ref 533005ASP4058, a novel agonist for sphingosine 1-phosphate receptors 1 and 5, ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile. PLoS One. 2014 Oct 27;9(10):e110819.
Ref 526934Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem. 2004 Apr 2;279(14):13839-48. Epub 2004 Jan 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 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 533005ASP4058, a novel agonist for sphingosine 1-phosphate receptors 1 and 5, ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile. PLoS One. 2014 Oct 27;9(10):e110819.

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