Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTDYP7I)

• DTT Name: Sphingosine-1-phosphate receptor 3 (S1PR3)
• Synonyms: Sphingosine 1-phosphate receptor Edg-3; S1PR3; S1P3; S1P receptor Edg-3; S1P receptor 3; Endothelial differentiation G-protein coupled receptor 3
• Gene Name: S1PR3
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: S1PR3_HUMAN
• TTD ID: T11241
• Sequence:
  MATALPPRLQPVRGNETLREHYQYVGKLAGRLKEASEGSTLTTVLFLVICSFIVLENLMV
  LIAIWKNNKFHNRMYFFIGNLALCDLLAGIAYKVNILMSGKKTFSLSPTVWFLREGSMFV
  ALGASTCSLLAIAIERHLTMIKMRPYDANKRHRVFLLIGMCWLIAFTLGALPILGWNCLH
  NLPDCSTILPLYSKKYIAFCISIFTAILVTIVILYARIYFLVKSSSRKVANHNNSERSMA
  LLRTVVIVVSVFIACWSPLFILFLIDVACRVQACPILFKAQWFIVLAVLNSAMNPVIYTL
  ASKEMRRAFFRLVCNCLVRGRGARASPIQPALDPSRSKSSSSNNSSHSPKVKEDLPHTAP
  SSCIMDKNAALQNGIFCN
• 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

35 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BDBM50080559	DMJNOB9	N. A.	N. A.	Patented	[2]
BDBM50080563	DM3VNK0	N. A.	N. A.	Patented	[2]
BDBM50080570	DMLJU5P	N. A.	N. A.	Patented	[2]
JCXGHZCWAHCYGY-UHFFFAOYSA-N	DMER7QX	N. A.	N. A.	Patented	[3]
MHHFJYABEVJNEG-UHFFFAOYSA-N	DM8UOY6	N. A.	N. A.	Patented	[3]
US10166249, Example 695	DMVMNP1	N. A.	N. A.	Patented	[4]
US10179791, Compound 171	DMGTBO3	N. A.	N. A.	Patented	[5]
US10179791, Compound 176	DMRHQLF	N. A.	N. A.	Patented	[5]
US10179791, Compound 296	DMLZBRM	N. A.	N. A.	Patented	[5]
US8524917, 10	DMCJH4F	N. A.	N. A.	Patented	[6]
US8524917, 11	DMETY0U	N. A.	N. A.	Patented	[7]
US8524917, 12	DMZ2ECB	N. A.	N. A.	Patented	[7]
US8524917, 60	DMRPD8U	N. A.	N. A.	Patented	[6]
US8563594, 152	DMDP87V	N. A.	N. A.	Patented	[7]
US9181182, 34	DMOKG3Q	N. A.	N. A.	Patented	[8]
US9181182, 40	DM3QIF4	N. A.	N. A.	Patented	[8]
US9181182, 47	DM4OHB5	N. A.	N. A.	Patented	[8]
US9187437, 24	DMVFBHD	N. A.	N. A.	Patented	[9]
US9187437, 38	DM2ULB8	N. A.	N. A.	Patented	[9]
US9187437, 8	DMEHSR7	N. A.	N. A.	Patented	[9]
US9216972, 132	DMD803F	N. A.	N. A.	Patented	[10]
US9216972, 61	DM7AHQE	N. A.	N. A.	Patented	[10]
US9216972, 67	DMXR5SZ	N. A.	N. A.	Patented	[10]
US9216972, 94	DMKLCZF	N. A.	N. A.	Patented	[10]
US9522888, 412	DMR1Z3I	N. A.	N. A.	Patented	[4]
US9522888, 575	DM6UXZK	N. A.	N. A.	Patented	[11]
US9522888, 618	DMG0QZ1	N. A.	N. A.	Patented	[4]
US9522888, 695	DMTRZI7	N. A.	N. A.	Patented	[11]
US9617250, Example 1 Example 204 of D1	DM89LKQ	N. A.	N. A.	Patented	[2]
US9670220, 33	DM9JCL2	N. A.	N. A.	Patented	[12]
US9670220, 76	DMNZD8T	N. A.	N. A.	Patented	[12]
US9670220, 77	DMZG1HO	N. A.	N. A.	Patented	[12]
US9707205, 40	DMSI09Y	N. A.	N. A.	Patented	[13]
YYDJCLCSBYCSCO-UHFFFAOYSA-N	DMA91FM	N. A.	N. A.	Patented	[3]
ZNFTXQFGUIKQQE-UHFFFAOYSA-N	DM3OPBR	N. A.	N. A.	Patented	[3]

1 Preclinical Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
EDD7H9	DMELPJM	Breast cancer	2C60-2C65	Preclinical	[1]

7 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AFD(R)	DME9Y8Q	Discovery agent	N.A.	Investigative	[14]
AUY954	DMVGIO5	Discovery agent	N.A.	Investigative	[15]
FTY720-phosphate	DMDZBQH	Discovery agent	N.A.	Investigative	[16]
VPC03090-P	DMIXUM3	Discovery agent	N.A.	Investigative	[17]
VPC12249	DM6F0VR	Discovery agent	N.A.	Investigative	[15]
VPC23019	DMVQFY4	Discovery agent	N.A.	Investigative	[18]
VPC44116	DMQ4OTJ	Discovery agent	N.A.	Investigative	[15]

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: 277).
• [2] Pyridin-4-yl derivatives. US9617250.
• [3] 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis. US9150519.
• [4] Substituted bicyclic compounds. US10166249.
• [5] Spiro-cyclic amine derivatives as S1P modulators. US10179791.
• [6] 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity. US8524917.
• [7] S1P3 receptor inhibitors for treating pain. US8563594.
• [8] S1P receptors modulators. US9181182.
• [9] Substituted oxadiazole compounds. US9187437.
• [10] Tricyclic heterocyclic compounds. US9216972.
• [11] Substituted bicyclic compounds. US9522888.
• [12] Fused heterocyclic derivatives as S1P modulators. US9670220.
• [13] S1P receptors modulators and their use thereof. US9707205.
• [14] The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol Chem. 2002 Jun 14;277(24):21453-7.
• [15] Synthesis 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.
• [16] Immune 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.
• [17] Characterization of a sphingosine 1-phosphate receptor antagonist prodrug. J Pharmacol Exp Ther. 2011 Sep;338(3):879-89.
• [18] Sphingosine 1-phosphate analogs as receptor antagonists. J Biol Chem. 2005 Mar 18;280(11):9833-41.