Target Information
Target General Infomation | |||||
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Target ID |
T95923
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Former ID |
TTDI02116
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Target Name |
Lysophosphatidate-3 receptor
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Gene Name |
LPAR3
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Synonyms |
LPA receptor 3; LPA3; Lysophosphatidic acid receptor 3; Lysophosphatidic acid receptor Edg7; LPAR3
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Target Type |
Clinical Trial
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Disease | Fibrosis [ICD9: 709.2; ICD10: L90.5] | ||||
Function |
Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities. May play a role in the development of ovarian cancer. Seems to be coupled to the G(i)/G(o) and G(q) families of heteromeric G proteins.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | |||||
Sequence |
MNECHYDKHMDFFYNRSNTDTVDDWTGTKLVIVLCVGTFFCLFIFFSNSLVIAAVIKNRK
FHFPFYYLLANLAAADFFAGIAYVFLMFNTGPVSKTLTVNRWFLRQGLLDSSLTASLTNL LVIAVERHMSIMRMRVHSNLTKKRVTLLILLVWAIAIFMGAVPTLGWNCLCNISACSSLA PIYSRSYLVFWTVSNLMAFLIMVVVYLRIYVYVKRKTNVLSPHTSGSISRRRTPMKLMKT VMTVLGAFVVCWTPGLVVLLLDGLNCRQCGVQHVKRWFLLLALLNSVVNPIIYSYKDEDM YGTMKKMICCFSQENPERRPSRIPSTVLSRSDTGSQYIEDSISQGAVCNKSTS |
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Drugs and Mode of Action | |||||
Agonist | 2-oleoyl-LPA | Drug Info | [525840] | ||
alkyl OMPT | Drug Info | [528359] | |||
alpha-fluoromethylenephosphonate | Drug Info | [527535] | |||
LPA | Drug Info | [525588] | |||
NAEPA | Drug Info | [529681] | |||
oleoyl-thiophosphate | Drug Info | [527648] | |||
OMPT | Drug Info | [526525] | |||
T13 | Drug Info | [529681] | |||
Antagonist | compound 12 | Drug Info | [530422] | ||
dioctanoylglycerol pyrophosphate | Drug Info | [526147] | |||
dodecyl-thiophosphate | Drug Info | [527648] | |||
dodecylphosphate | Drug Info | [526598] | |||
Ki16425 | Drug Info | [526829] | |||
VPC12249 | Drug Info | [526205] | |||
VPC32183 | Drug Info | [527065] | |||
Modulator | SAR-100842 | Drug Info | [544454] | ||
Pathways | |||||
KEGG Pathway | Rap1 signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
PI3K-Akt signaling pathway | |||||
Pathways in cancer | |||||
Pathway Interaction Database | LPA receptor mediated events | ||||
Reactome | G alpha (q) signalling events | ||||
G alpha (i) signalling events | |||||
Lysosphingolipid and LPA receptors | |||||
WikiPathways | Gastrin-CREB signalling pathway via PKC and MAPK | ||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 525588 | Molecular cloning and characterization of a novel human G-protein-coupled receptor, EDG7, for lysophosphatidic acid. J Biol Chem. 1999 Sep 24;274(39):27776-85. | ||||
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 526525 | Identification of a phosphothionate analogue of lysophosphatidic acid (LPA) as a selective agonist of the LPA3 receptor. J Biol Chem. 2003 Apr 4;278(14):11962-9. Epub 2003 Jan 27. | ||||
Ref 526598 | Fatty alcohol phosphates are subtype-selective agonists and antagonists of lysophosphatidic acid receptors. Mol Pharmacol. 2003 May;63(5):1032-42. | ||||
Ref 526829 | Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol Pharmacol. 2003 Oct;64(4):994-1005. | ||||
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 527535 | Structure-activity relationships of fluorinated lysophosphatidic acid analogues. J Med Chem. 2005 May 5;48(9):3319-27. | ||||
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. |
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