Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTB7Y8I)

• DTT Name: Lysophosphatidic acid receptor 2 (LPAR2)
• Synonyms: Lysophosphatidic acid receptor Edg-4; LPA2; LPA-2; LPA receptor 2; EDG4
• Gene Name: LPAR2
• DTT Type: Literature-reported target; [1]
• BioChemical Class: GPCR rhodopsin
• UniProt ID: LPAR2_HUMAN
• TTD ID: T39380
• Sequence:
  MVIMGQCYYNETIGFFYNNSGKELSSHWRPKDVVVVALGLTVSVLVLLTNLLVIAAIASN
  RRFHQPIYYLLGNLAAADLFAGVAYLFLMFHTGPRTARLSLEGWFLRQGLLDTSLTASVA
  TLLAIAVERHRSVMAVQLHSRLPRGRVVMLIVGVWVAALGLGLLPAHSWHCLCALDRCSR
  MAPLLSRSYLAVWALSSLLVFLLMVAVYTRIFFYVRRRVQRMAEHVSCHPRYRETTLSLV
  KTVVIILGAFVVCWTPGQVVLLLDGLGCESCNVLAVEKYFLLLAEANSLVNAAVYSCRDA
  EMRRTFRRLLCCACLRQSTRESVHYTSSAQGGASTRIMLPENGHPLMDSTL
• Function: Seems to be coupled to the G(i)/G(o), G(12)/G(13), and G(q) families of heteromeric G proteins. Plays a key role in phospholipase C-beta (PLC-beta) signaling pathway. Stimulates phospholipase C (PLC) activity in a manner that is independent of RALA activation. Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities.
• Reactome Pathway:
  G alpha (i) signalling events (R-HSA-418594)
  Lysosphingolipid and LPA receptors (R-HSA-419408)
  G alpha (q) signalling events (R-HSA-416476)

Molecular Interaction Atlas (MIA) of This DTT

11 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-oleoyl-LPA	DMN9OS1	Discovery agent	N.A.	Investigative	[2]
BrP-LPA	DMPGEO1	Discovery agent	N.A.	Investigative	[3]
decyl dihydrogen phosphate	DMNKDT5	Discovery agent	N.A.	Investigative	[4]
dodecyl-thiophosphate	DMAJVPI	Discovery agent	N.A.	Investigative	[5]
dodecylphosphate	DMPCLTW	Discovery agent	N.A.	Investigative	[4]
GRI977143	DM3A0TE	Discovery agent	N.A.	Investigative	[6]
Ki16425	DMJTDK9	Discovery agent	N.A.	Investigative	[7]
LPA	DMI5XR1	Discovery agent	N.A.	Investigative	[8]
NAEPA	DM38XWZ	Discovery agent	N.A.	Investigative	[1]
oleoyl-thiophosphate	DM1TAM9	Discovery agent	N.A.	Investigative	[5]
PMID18178086C15	DMA2OWK	Discovery agent	N.A.	Investigative	[9]

References

• [1] LPA and its analogs-attractive tools for elucidation of LPA biology and drug development. Curr Med Chem. 2008;15(21):2122-31.
• [2] Lysophosphatidic acid (LPA) receptors of the EDG family are differentially activated by LPA species. Structure-activity relationship of cloned LPA receptors. FEBS Lett. 2000 Jul 28;478(1-2):159-65.
• [3] Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo. Cancer Res. 2009 Jul 1;69(13):5441-9.
• [4] Fatty alcohol phosphates are subtype-selective agonists and antagonists of lysophosphatidic acid receptors. Mol Pharmacol. 2003 May;63(5):1032-42.
• [5] Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activ... J Med Chem. 2005 Jul 28;48(15):4919-30.
• [6] Virtual screening for LPA2-specific agonists identifies a nonlipid compound with antiapoptotic actions. Mol Pharmacol. 2012 Dec;82(6):1162-73.
• [7] Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol Pharmacol. 2003 Oct;64(4):994-1005.
• [8] Synthesis and biological evaluation of phosphonic and thiophosphoric acid derivatives of lysophosphatidic acid. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3473-6.
• [9] Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1037-41.