Target Information

Target General Infomation
Target ID
T95923
Former ID
TTDI02116
Target Name
Lysophosphatidate-3 receptor
Gene Name
LPAR3
Synonyms
LPA receptor 3; LPA3; Lysophosphatidic acid receptor 3; Lysophosphatidic acid receptor Edg7; LPAR3
Target Type
Clinical Trial
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.
BioChemical Class
GPCR rhodopsin
UniProt ID
Q9UBY5
Sequence
MNECHYDKHMDFFYNRSNTDTVDDWTGTKLVIVLCVGTFFCLFIFFSNSLVIAAVIKNRK
FHFPFYYLLANLAAADFFAGIAYVFLMFNTGPVSKTLTVNRWFLRQGLLDSSLTASLTNL
LVIAVERHMSIMRMRVHSNLTKKRVTLLILLVWAIAIFMGAVPTLGWNCLCNISACSSLA
PIYSRSYLVFWTVSNLMAFLIMVVVYLRIYVYVKRKTNVLSPHTSGSISRRRTPMKLMKT
VMTVLGAFVVCWTPGLVVLLLDGLNCRQCGVQHVKRWFLLLALLNSVVNPIIYSYKDEDM
YGTMKKMICCFSQENPERRPSRIPSTVLSRSDTGSQYIEDSISQGAVCNKSTS
Drugs and Mode of Action
Drug(s) SAR-100842 Drug Info Phase 2 Fibrosis [523991]
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 523991ClinicalTrials.gov (NCT01651143) Proof of Biological Activity of SAR100842 in Systemic Sclerosis. U.S. National Institutes of Health.
Ref 525588Molecular 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 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 526525Identification 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 526598Fatty alcohol phosphates are subtype-selective agonists and antagonists of lysophosphatidic acid receptors. Mol Pharmacol. 2003 May;63(5):1032-42.
Ref 526829Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol Pharmacol. 2003 Oct;64(4):994-1005.
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 527535Structure-activity relationships of fluorinated lysophosphatidic acid analogues. J Med Chem. 2005 May 5;48(9):3319-27.
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 530422Structure-based drug design identifies novel LPA3 antagonists. Bioorg Med Chem. 2009 Nov 1;17(21):7457-64.
Ref 544454Promising Pharmacological Directions in the World of Lysophosphatidic Acid Signaling. Biomol Ther (Seoul) 2015 January; 23(1): 1-11.

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