Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTVSMOH)

• DTT Name: Sphingosine-1-phosphate receptor 2 (S1PR2)
• Synonyms: Sphingosine 1-phosphate receptor Edg-5; S1PR2; S1P2; S1P receptor Edg-5; S1P receptor 2; Endothelial differentiation G-protein coupled receptor 5
• Gene Name: S1PR2
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: S1PR2_HUMAN
• TTD ID: T47888
• Sequence:
  MGSLYSEYLNPNKVQEHYNYTKETLETQETTSRQVASAFIVILCCAIVVENLLVLIAVAR
  NSKFHSAMYLFLGNLAASDLLAGVAFVANTLLSGSVTLRLTPVQWFAREGSAFITLSASV
  FSLLAIAIERHVAIAKVKLYGSDKSCRMLLLIGASWLISLVLGGLPILGWNCLGHLEACS
  TVLPLYAKHYVLCVVTIFSIILLAIVALYVRIYCVVRSSHADMAAPQTLALLKTVTIVLG
  VFIVCWLPAFSILLLDYACPVHSCPILYKAHYFFAVSTLNSLLNPVIYTWRSRDLRREVL
  RPLQCWRPGVGVQGRRRGGTPGHHLLPLRSSSSLERGMHMPTSPTFLEGNTVV
• 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.
• KEGG Pathway:
  Sphingolipid signaling pathway (hsa04071)
  Neuroactive ligand-receptor interaction (hsa04080)
• Reactome Pathway:
  Lysosphingolipid and LPA receptors (R-HSA-419408)
  G alpha (i) signalling events (R-HSA-418594)

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amiselimod	DMI7CYZ	Ulcerative colitis	DD71	Phase 2	[2]

6 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Jte 013	DMS3HNM	Discovery agent	N.A.	Patented	[3]
SCHEMBL15295829	DMK0T9E	N. A.	N. A.	Patented	[3]
Unii-R228S06soh	DMUHSAZ	N. A.	N. A.	Patented	[3]
US8975409, Comparative compound B	DM4S5DF	N. A.	N. A.	Patented	[4]
US8975409, Example 13	DMVB42P	N. A.	N. A.	Patented	[4]
US8975409, Example 9(3)	DMJQOAE	N. A.	N. A.	Patented	[4]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AUY954	DMVGIO5	Discovery agent	N.A.	Investigative	[5]

References

• [1] URL: 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: 276).
• [2] Amiselimod, a novel sphingosine 1-phosphate receptor-1 modulator, has potent therapeutic efficacy for autoimmune diseases, with low bradycardia risk. Br J Pharmacol. 2017 Jan;174(1):15-27.
• [3] Sphingosine 1-phosphate receptor antagonists. US9663511.
• [4] Phenyl derivative. US8975409.
• [5] A 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.