Target Information
Target General Infomation | |||||
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Target ID |
T92640
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Former ID |
TTDR00580
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Target Name |
Lysophosphatidic acid receptor Edg-2
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Gene Name |
LPAR1
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Synonyms |
EDG 2 receptor; LPA receptor 1; LPA-1; LPAR1
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Target Type |
Clinical Trial
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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.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T92640
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UniProt ID | |||||
Sequence |
MAAISTSIPVISQPQFTAMNEPQCFYNESIAFFYNRSGKHLATEWNTVSKLVMGLGITVC
IFIMLANLLVMVAIYVNRRFHFPIYYLMANLAAADFFAGLAYFYLMFNTGPNTRRLTVST WLLRQGLIDTSLTASVANLLAIAIERHITVFRMQLHTRMSNRRVVVVIVVIWTMAIVMGA IPSVGWNCICDIENCSNMAPLYSDSYLVFWAIFNLVTFVVMVVLYAHIFGYVRQRTMRMS RHSSGPRRNRDTMMSLLKTVVIVLGAFIICWTPGLVLLLLDVCCPQCDVLAYEKFFLLLA EFNSAMNPIIYSYRDKEMSATFRQILCCQRSENPTGPTEGSDRSASSLNHTILAGVHSND HSVV |
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Drugs and Mode of Action | |||||
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 523991 | ClinicalTrials.gov (NCT01651143) Proof of Biological Activity of SAR100842 in Systemic Sclerosis. U.S. National Institutes of Health. | ||||
Ref 525840 | 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. | ||||
Ref 526147 | Short-chain phosphatidates are subtype-selective antagonists of lysophosphatidic acid receptors. Mol Pharmacol. 2001 Oct;60(4):776-84. | ||||
Ref 526205 | Activity 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 527065 | Initial 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 527648 | J 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 528359 | Phosphorothioate analogues of alkyl lysophosphatidic acid as LPA3 receptor-selective agonists. ChemMedChem. 2006 Mar;1(3):376-83. | ||||
Ref 529681 | LPA and its analogs-attractive tools for elucidation of LPA biology and drug development. Curr Med Chem. 2008;15(21):2122-31. | ||||
Ref 530196 | 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. | ||||
Ref 530944 | Diversity of lysophosphatidic acid receptor-mediated intracellular calcium signaling in early cortical neurogenesis. J Neurosci. 2010 May 26;30(21):7300-9. | ||||
Ref 531119 | Pharmacological tools for lysophospholipid GPCRs: development of agonists and antagonists for LPA and S1P receptors. Acta Pharmacol Sin. 2010 Sep;31(9):1213-22. | ||||
Ref 531303 | Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700. | ||||
Ref 531748 | Targeting 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. |
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