Target Information

Target General Infomation
Target ID
T92640
Former ID
TTDR00580
Target Name
Lysophosphatidic acid receptor Edg-2
Gene Name
LPAR1
Synonyms
EDG 2 receptor; LPA receptor 1; LPA-1; LPAR1
Target Type
Clinical Trial
Disease Fibrosis [ICD9: 709.2; ICD10: L90.5]
Idiopathic pulmonary fibrosis [ICD9: 516.3; ICD10: J84.1]
Function
Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities. Seems to be coupled to the G(i)/G(o), G(12)/G(13), and G(q) families of heteromeric G proteins. Stimulates phospholipase C (PLC) activity in a manner that is dependent on RALA activation.
BioChemical Class
GPCR rhodopsin
Target Validation
T92640
UniProt ID
Q92633
Sequence
MAAISTSIPVISQPQFTAMNEPQCFYNESIAFFYNRSGKHLATEWNTVSKLVMGLGITVC
IFIMLANLLVMVAIYVNRRFHFPIYYLMANLAAADFFAGLAYFYLMFNTGPNTRRLTVST
WLLRQGLIDTSLTASVANLLAIAIERHITVFRMQLHTRMSNRRVVVVIVVIWTMAIVMGA
IPSVGWNCICDIENCSNMAPLYSDSYLVFWAIFNLVTFVVMVVLYAHIFGYVRQRTMRMS
RHSSGPRRNRDTMMSLLKTVVIVLGAFIICWTPGLVLLLLDVCCPQCDVLAYEKFFLLLA
EFNSAMNPIIYSYRDKEMSATFRQILCCQRSENPTGPTEGSDRSASSLNHTILAGVHSND
HSVV
Drugs and Mode of Action
Drug(s) SAR-100842 Drug Info Phase 2 Fibrosis [523991]
BMS-986202 Drug Info Preclinical Idiopathic pulmonary fibrosis [542017], [548922]
Inhibitor (1,1-Difluoro-pentadecyl)-phosphonic acid Drug Info [527648]
Decyl-phosphonic acid Drug Info [527648]
Dodecyl-phosphonic acid Drug Info [527648]
Phosphoric acid mono-((E)-dec-4-enyl) ester Drug Info [527648]
Phosphoric acid mono-((E)-dodec-9-enyl) ester Drug Info [527648]
Phosphoric acid mono-((E)-tetradec-11-enyl) ester Drug Info [527648]
Phosphoric acid mono-((E)-tetradec-9-enyl) ester Drug Info [527648]
Phosphoric acid monodec-9-enyl ester Drug Info [527648]
Phosphoric acid monododecyl ester Drug Info [527648]
Phosphoric acid monotetradecyl ester Drug Info [527648]
Tetradecyl-phosphonic acid Drug Info [527648]
Thiophosphoric acid (E)-dodec-9-enyl ester Drug Info [527648]
Thiophosphoric acid (E)-tetradec-9-enyl ester Drug Info [527648]
Thiophosphoric acid dec-9-enyl ester Drug Info [527648]
Thiophosphoric acid decyl ester Drug Info [527648]
Thiophosphoric acid dodecyl ester Drug Info [527648]
Agonist 2-oleoyl-LPA Drug Info [525840]
alkyl OMPT Drug Info [528359]
LPA Drug Info [530944]
NAEPA Drug Info [529681]
oleoyl-thiophosphate Drug Info [531119]
T13 Drug Info [531119]
Antagonist anti-BrP-LPA Drug Info [530196]
BMS-986202 Drug Info [531303]
BrP-LPA Drug Info [530196]
dioctanoylglycerol pyrophosphate Drug Info [526147]
Ki16425 Drug Info [531748]
ONO-3080573 Drug Info [533273]
ONO-9780307 Drug Info [533273]
ONO-9910539 Drug Info [533273]
syn-BrP-LPA Drug Info [530196]
VPC12249 Drug Info [526205]
VPC32183 Drug Info [527065]
Modulator SAR-100842 Drug Info [544454]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Rap1 signaling pathway
Neuroactive ligand-receptor interaction
PI3K-Akt signaling pathway
Gap junction
Pathways in cancer
NetPath Pathway TGF_beta_Receptor Signaling Pathway
Pathway Interaction Database LPA receptor mediated events
Reactome G alpha (q) signalling events
G alpha (i) signalling events
Lysosphingolipid and LPA receptors
WikiPathways Myometrial Relaxation and Contraction Pathways
Gastrin-CREB signalling pathway via PKC and MAPK
Small Ligand GPCRs
GPCR ligand binding
GPCR downstream signaling
References
Ref 523991ClinicalTrials.gov (NCT01651143) Proof of Biological Activity of SAR100842 in Systemic Sclerosis. U.S. National Institutes of Health.
Ref 542017(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. (Ligand id: 6988).
Ref 548922Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030351)
Ref 525840Lysophosphatidic 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.
Ref 526147Short-chain phosphatidates are subtype-selective antagonists of lysophosphatidic acid receptors. Mol Pharmacol. 2001 Oct;60(4):776-84.
Ref 526205Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA1/LPA3 receptor antagonist. Mol Pharmacol. 2001 Dec;60(6):1173-80.
Ref 527065Initial structure-activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2735-40.
Ref 527648J Med Chem. 2005 Jul 28;48(15):4919-30.Synthesis, structure-activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of PPARgamma, and inhibitors of autotaxin.
Ref 528359Phosphorothioate analogues of alkyl lysophosphatidic acid as LPA3 receptor-selective agonists. ChemMedChem. 2006 Mar;1(3):376-83.
Ref 529681LPA and its analogs-attractive tools for elucidation of LPA biology and drug development. Curr Med Chem. 2008;15(21):2122-31.
Ref 530196Dual 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.
Ref 530944Diversity of lysophosphatidic acid receptor-mediated intracellular calcium signaling in early cortical neurogenesis. J Neurosci. 2010 May 26;30(21):7300-9.
Ref 531119Pharmacological tools for lysophospholipid GPCRs: development of agonists and antagonists for LPA and S1P receptors. Acta Pharmacol Sin. 2010 Sep;31(9):1213-22.
Ref 531303Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700.
Ref 531748Targeting lysophosphatidic acid receptor type 1 with Debio 0719 inhibits spontaneous metastasis dissemination of breast cancer cells independently of cell proliferation and angiogenesis. Int J Oncol. 2012 Apr;40(4):1133-41.
Ref 533273Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1. Cell. 2015 Jun 18;161(7):1633-43.
Ref 544454Promising Pharmacological Directions in the World of Lysophosphatidic Acid Signaling. Biomol Ther (Seoul) 2015 January; 23(1): 1-11.

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