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LPA1 receptor

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Target not currently curated in GtoImmuPdb

Target id: 272

Nomenclature: LPA1 receptor

Family: Lysophospholipid (LPA) receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 364 9q31.3 LPAR1 lysophosphatidic acid receptor 1 9
Mouse 7 364 4 32.2 cM Lpar1 lysophosphatidic acid receptor 1 9
Rat 7 364 5q24 Lpar1 lysophosphatidic acid receptor 1 3
Previous and Unofficial Names Click here for help
EDG2 | GPR26 | VZG1 | endothelial differentiation gene 2, lysophosphatidic acid G-protein-coupled receptor, 2 | LPA receptor 1 | Lpar1 | lysophosphatidic acid receptor Edg-2
Database Links Click here for help
Specialist databases
GPCRdb lpar1_human (Hs), lpar1_mouse (Mm), lpar1_rat (Rn)
Other databases
Alphafold Q92633 (Hs), P61793 (Mm), P61794 (Rn)
ChEMBL Target CHEMBL3819 (Hs), CHEMBL3621025 (Mm), CHEMBL4595 (Rn)
Ensembl Gene ENSG00000198121 (Hs), ENSMUSG00000038668 (Mm), ENSRNOG00000013656 (Rn)
Entrez Gene 1902 (Hs), 14745 (Mm), 116744 (Rn)
Human Protein Atlas ENSG00000198121 (Hs)
KEGG Gene hsa:1902 (Hs), mmu:14745 (Mm), rno:116744 (Rn)
OMIM 602282 (Hs)
Pharos Q92633 (Hs)
RefSeq Nucleotide NM_001401 (Hs), NM_010336 (Mm), NM_053936 (Rn)
RefSeq Protein NP_001392 (Hs), NP_034466 (Mm), NP_446388 (Rn)
SynPHARM 82425 (in complex with ONO-3080573)
82426 (in complex with ONO-9780307)
82427 (in complex with ONO-9910539)
UniProtKB Q92633 (Hs), P61793 (Mm), P61794 (Rn)
Wikipedia LPAR1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO-3080573.
PDB Id:  4Z36
Ligand:  ONO-3080573
Resolution:  2.9Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO-9910539.
PDB Id:  4Z35
Ligand:  ONO-9910539
Resolution:  2.9Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Human Lysophosphatidic Acid Receptor 1 in complex with ONO9780307.
PDB Id:  4Z34
Ligand:  ONO-9780307
Resolution:  3.0Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Lysophosphatidic acid receptor 1-Gi complex bound to LPA
PDB Id:  7TD0
Ligand:  LPA
Resolution:  2.83Å
Species:  Mouse
References:  33
Image of receptor 3D structure from RCSB PDB
Description:  Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556
PDB Id:  7YU3
Resolution:  3.5Å
Species:  Human
References:  1
Natural/Endogenous Ligands Click here for help
LPA

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
UCM-05194 Small molecule or natural product Hs Agonist 7.7 pKd 22
⤷ pKd 7.7 (Kd 1.96x10-8 M) [22]
CpY Small molecule or natural product Click here for species-specific activity table Hs Agonist 8.3 pKi 23
⤷ pKi 8.3 (Ki 5x10-9 M) [23]
CpX Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.3 pKi 23
⤷ pKi 7.3 (Ki 5x10-8 M) [23]
LPA Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Mm Full agonist 7.9 – 8.3 pEC50 13,25,30
⤷ pEC50 7.9 – 8.3 (EC50 1.17x10-8 – 5x10-9 M) [13,25,30]
CpX Small molecule or natural product Click here for species-specific activity table Hs Agonist 7.5 pEC50 23
⤷ pEC50 7.5 (EC50 3.16x10-8 M) [23]
NAEPA Small molecule or natural product Click here for species-specific activity table Mm Partial agonist 6.7 pEC50 30
⤷ pEC50 6.7 (EC50 1.97x10-7 M) [30]
oleoyl-thiophosphate Small molecule or natural product Hs Partial agonist 6.7 pEC50 14
⤷ pEC50 6.7 (EC50 1.93x10-7 M) [14]
oleoyl-thiophosphate Small molecule or natural product Click here for species-specific activity table Mm Partial agonist 6.7 pEC50 28
⤷ pEC50 6.7 (EC50 1.93x10-7 M) [28]
2-oleoyl-LPA Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.7 pEC50 5
⤷ pEC50 6.7 [5]
UCM-05194 Small molecule or natural product Hs Agonist 6.6 pEC50 22
⤷ pEC50 6.6 (EC50 2.4x10-7 M) [22]
T13 Small molecule or natural product Click here for species-specific activity table Mm Partial agonist 6.3 pEC50 28,30
⤷ pEC50 6.3 (EC50 5x10-7 M) [28,30]
CpY Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.3 pEC50 23
⤷ pEC50 6.3 (EC50 5.01x10-7 M) [23]
alkyl OMPT Small molecule or natural product Click here for species-specific activity table Hs Agonist 6.1 – 6.2 pEC50 41
⤷ pEC50 6.1 – 6.2 [41]
View species-specific agonist tables
Agonist Comments
Breakdown of affinities for various LPA species [42,44]:
LPA sp.pEC50Kd (nM)
18:17.73 ± 0.122.08 ± 1.32
14:07.26 ± 0.11
16:07.32 ± 0.161.69 ± 0.1
17:06.44 ± 0.05
18:26.84 ± 0.032.83 ± 1.64
18:36.45 ± 0.06
20:05.44 ± 0.24
20:46.85 ± 0.222.59 ± 0.48
C18 6.22 ± 0.05
C18:1 8.04 ± 0.18
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BMS-986278 Small molecule or natural product Hs Antagonist 8.2 pKB 6
⤷ pKB 8.2 (KB 6.9x10-9 M) [6]
VPC32183 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.8 pKi 24
⤷ pKi 7.8 [24]
syn-BrP-LPA Small molecule or natural product Hs Antagonist 6.6 pKi 54
⤷ pKi 6.6 (Ki 2.73x10-7 M) [54]
anti-BrP-LPA Small molecule or natural product Hs Antagonist 6.1 pKi 54
⤷ pKi 6.1 (Ki 7.52x10-7 M) [54]
BrP-LPA Small molecule or natural product Hs Antagonist 6.1 pKi 54
⤷ pKi 6.1 (Ki 8.05x10-7 M) [54]
VPC12249 Small molecule or natural product Mm Antagonist 5.2 – 6.9 pKi 26
⤷ pKi 5.2 – 6.9 (Ki 5.7x10-6 – 1.37x10-7 M) [26]
dioctanoylglycerol pyrophosphate Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 5.2 – 5.2 pKi 16,30
⤷ pKi 5.2 – 5.2 (Ki 7x10-6 – 6.6x10-6 M) [16,30]
AM966 Small molecule or natural product Click here for species-specific activity table Mm Antagonist 7.7 pEC50 47
⤷ pEC50 7.7 [47]
BMS-986020 Small molecule or natural product Primary target of this compound Hs Antagonist 8.9 pIC50
⤷ pIC50 8.9
ONO-3080573 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Antagonist 8.0 pIC50 8
⤷ pIC50 8.0 (IC50 1.1x10-8 M) [8]
Description: FLIPR intracellular calcium mobilisation assay
ONO-9910539 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Antagonist 7.7 pIC50 8
⤷ pIC50 7.7 (IC50 2.2x10-8 M) [8]
Description: FLIPR intracellular calcium mobilisation assay
ONO-9780307 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Antagonist 7.6 pIC50 8
⤷ pIC50 7.6 (IC50 2.7x10-8 M) [8]
Description: FLIPR intracellular calcium mobilisation assay
AM966 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 – 7.8 pIC50 46
⤷ pIC50 6.7 – 7.8 (IC50 1.99x10-7 – 1.58x10-8 M) [46]
mianserin Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist ~7.0 pIC50 39
⤷ pIC50 ~7.0 (IC50 ~1x10-7 M) [39]
SAR100842 Small molecule or natural product Hs Antagonist 6.7 – 7.3 pIC50 32
⤷ pIC50 6.7 – 7.3 (IC50 2x10-7 – 5x10-8 M) [32]
VPC32183 Small molecule or natural product Mm Antagonist 7.0 pIC50 24
⤷ pIC50 7.0 (IC50 1.09x10-7 M) [24]
ONO-7300243 Small molecule or natural product Primary target of this compound Hs Antagonist 6.8 pIC50 48
⤷ pIC50 6.8 (IC50 1.6x10-7 M) [48]
Ki16425 Small molecule or natural product Mm Antagonist 6.6 – 6.9 pIC50 37
⤷ pIC50 6.6 – 6.9 (IC50 2.5x10-7 – 1.3x10-7 M) [37]
amitriptyline Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist ~6.2 pIC50 39
⤷ pIC50 ~6.2 (IC50 ~6x10-7 M) [39]
syn-BrP-LPA Small molecule or natural product Hs Antagonist 6.2 pIC50 54
⤷ pIC50 6.2 (IC50 6.48x10-7 M) [54]
AM095 Small molecule or natural product Mm Antagonist 6.1 pIC50 46
⤷ pIC50 6.1 (IC50 7.78x10-7 M) [46]
AM095 Small molecule or natural product Primary target of this compound Hs Antagonist 6.0 – 6.1 pIC50 46
⤷ pIC50 6.0 – 6.1 [46]
anti-BrP-LPA Small molecule or natural product Hs Antagonist 5.7 pIC50 54
⤷ pIC50 5.7 (IC50 2.079x10-6 M) [54]
BrP-LPA Small molecule or natural product Hs Antagonist 5.3 pIC50 54
⤷ pIC50 5.3 (IC50 4.52x10-6 M) [54]
VPC32179 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - - 24
⤷ [24]
View species-specific antagonist tables
Antagonist Comments
The IC50 for AM966 [47] and SAR100842 [32] were determined by the LPA-stimulated intracellular calcium release from CHO cells expressing hLPA1 receptors. AM966 inhibited LPA-induced chemotaxis (pIC50 = 6.7) of human IMR-90 lung fibroblasts [47]. SAR100842 inhibited LPA-induced secretion of IL-6, CCL2 and CXCL1 (IC50 ~50 nM) in systemic sclerosis dermal fibroblasts [32].

pKi of AM966 in presence of following LPA species [44]:
LPA sp.pKi
18:17.85 ± 0.03
16:07.73 ± 0.05
17:07.77 ± 0.02
18:27.86 ± 0.02
C18:1 7.78 ± 0.02
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family
Gq/G11 family
G12/G13 family 		Adenylyl cyclase inhibition
Phospholipase C stimulation
Phospholipase A2 stimulation
Other - See Comments
Comments:  In general LPA1 is known to induce many responses including cell proliferation and survival, cell migration, and cytoskeletal changes; altered cell-cell contact through serum-response element activation, Ca2+ mobilization, and adenylyl cyclase inhibition; and activation of mitogen-activated protein kinase, phospholipase C, Akt, and Rho pathways. For a detailed review please see [7].
References:  18,29
Tissue Distribution Click here for help
Brain, uterus, testis, lung, small intestine, heart, stomach, kidney, spleen, thymus, placenta, and skeletal muscle
Species:  Human
Technique:  Northern blot
References:  4
Kidney,spleen, thymus (not in liver)
Expression level:  Low
Species:  Mouse
Technique:  Northern Blot
References:  52
Embryonic cerebral dorsal telencephalon (cortical ventricular zone (VZ))
Expression level:  High
Species:  Mouse
Technique:  In situ hybridisation and RT-PCR, Western Blot
References:  12,25
Brain, heart, lung, and testis
Expression level:  High
Species:  Mouse
Technique:  Northern blot
References:  52
Brain, uterus, testis, lung, small intestine, heart, stomach, kidney, spleen, thymus, placenta, and skeletal muscle, embryonic brain, embryonic dorsal olfactory bulb, embryonic limb buds, embryonic craniofacial region, embryonic somites, and embryonic genital tubercle
Species:  Mouse
Technique:  In situ hybridisation, Northern blot
References:  10,25,38
Abdominal/thoracic aortic vascular smooth muscle cell
Expression level:  High
Species:  Mouse
Technique:  qRT-PCR
References:  11
In the postnatal murine nervous system: oligodendrocytes and Schwann cells, the myelinating cells of the central and peripheral nervous systems
Species:  Rat
Technique:  In situ hybridisation, histochemistry, immunocytochemistry, Northern blot
References:  3
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Actin rearrangement, stress fibre formation, and cell rounding
Species:  Rat
Tissue:  Neuroblastoma (B103 cell line)
Response measured:  Cell rounding upon receptor stimulation by LPA ligand
References:  18,29
Physiological Functions Click here for help
Increased cell proliferation and/or survival
Species:  Mouse
Tissue:  Schwann cells
References:  31,50
Increase in neuronal differentiation
Species:  Mouse
Tissue:  Brain
References:  19,31
Actin rearrangement and alteration of cortical neuroblast morphology in vitro and in vivo
Species:  Mouse
Tissue:  Neuroprogenitors, Schwann cells
References:  17,20-21,51
Cell migration
Species:  Mouse
Tissue:  Cortical neuroprogenitor
References:  21
Inhibition of adipocyte differentiation
Species:  Mouse
Tissue:  Adipose
References:  45
Contraction
Species:  Mouse
Tissue:  Aortic vascular smooth muscle.
References:  11
Physiological Consequences of Altering Gene Expression Click here for help
Phenotypes include: (50%) neonatal lethality; impaired suckling in neonatal pups; smaller size pups; craniofacial dysmorphism; increased apoptosis. Alterations in signaling characteristics are also observed.
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  10
Mice with receptor knockout develop 50% perinatal lethality due to defective olfaction and impaired suckling behavior, decreased body size, craniofacial dysmorphism with blunted snouts, and increased apoptosis in sciatic nerve Schwann cells.
Species:  Mouse
Tissue:  Brain
Technique:  Gene knockouts
References:  10,25
Malaga receptor knockout have negligible perinatal lethality, reduced NPC proliferation, increased cerebral cortical apoptosis, decreased cortical size, and premature expression of neuronal markers, reduced neurogenesis in dentate gyrus, inhibition of fear extinction.
Species:  Mouse
Tissue:  Brain
Technique:  Gene knockouts
References:  15,35,40
Partial sciatic nerve ligation (PSNL)‐induced neuropathic pain was diminished in KO mice.
Species:  Mouse
Tissue:  Partial sciatic nerve
Technique:  Gene knockout
References:  43
LPA-induced hydrocephalus was blocked in LPA1 and LPA3 KO mice.
Species:  Mouse
Tissue:  Brain
Technique:  Gene knockout
References:  34,53
Bone mineralization and osteocyte function was reduced in osteoblast-specific LPA1 KO mice.
Species:  Mouse
Tissue:  Osteoblastic cell lineage
Technique:  Gene knockout.
References:  2
Diabetic neuropathic pain was blocked in LPA1 and LPA3 KO mice.
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  49
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0005332 abnormal amino acid level PMID: 14697676 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0000428 abnormal craniofacial morphology PMID: 14697676 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0001106 abnormal Schwann cell morphology PMID: 11087877 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0002651 abnormal sciatic nerve PMID: 11087877 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0005322 abnormal serotonin concentration PMID: 14697676 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0001436 abnormal suckling behavior PMID: 11087877 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0001255 decreased body height PMID: 14697676 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0006086 decreased body mass index PMID: 14697676 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0001265 decreased body size PMID: 11087877 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0009142 decreased prepulse inhibition PMID: 14697676 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0001107 decreased Schwann cell number PMID: 11087877 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0010025 decreased total body fat amount PMID: 11087877 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0000914 exencephaly PMID: 11087877 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0001914 hemorrhage PMID: 11087877 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0001402 hypoactivity PMID: 14697676 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0001906 increased dopamine level PMID: 14697676 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0004831 long incisors PMID: 14697676 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0002058 neonatal lethality PMID: 11087877 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0001300 ocular hypertelorism PMID: 11087877 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0001300 ocular hypertelorism PMID: 14697676 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0002081 perinatal lethality PMID: 14697676 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0001732 postnatal growth retardation PMID: 11087877 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0002082 postnatal lethality PMID: 11087877 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0002082 postnatal lethality PMID: 14697676 
Lpar1tm1Jch Lpar1tm1Jch/Lpar1tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6J		 MGI:108429  MP:0000445 short snout PMID: 11087877 
Lpar1tm1Mcox Lpar1tm1Mcox/Lpar1tm1Mcox
B6.129P2-Lpar1		 MGI:108429  MP:0000445 short snout PMID: 14697676 
Gene Expression and Pathophysiology Comments
Mouse models indicate that overactivation of LPA1 during fetal development initiates hydrocephalus in vivo [53], and can cause prenatal intracerebral hemorrhage leading to schizophrenia-like brain and behavioral changes [36]. Also in mice, fetal hypoxia activates LPA1 signaling, inhibition of which reduces hypoxia-induced brain injury. These findings may point to potential treatments for fetal hypoxia-induced CNS disorders or for other forms of hypoxic brain injury [27].
Biologically Significant Variant Comments
There is a splice variant (mrec 1.3) that results in an 18-amino acid deletion of the N terminus, but its biological significance is unknown [9].

References

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1. Akasaka H, Tanaka T, Sano FK, Matsuzaki Y, Shihoya W, Nureki O. (2022) Structure of the active Gi-coupled human lysophosphatidic acid receptor 1 complexed with a potent agonist. Nat Commun, 13 (1): 5417. [PMID:36109516]

2. Alioli CA, Demesmay L, Laurencin-Dalacieux S, Beton N, Farlay D, Follet H, Saber A, Duboeuf F, Chun J, Rivera R et al.. (2020) Expression of the type 1 lysophosphatidic acid receptor in osteoblastic cell lineage controls both bone mineralization and osteocyte specification. Biochim Biophys Acta Mol Cell Biol Lipids, 1865 (8): 158715. [PMID:32330664]

3. Allard J, Barrón S, Diaz J, Lubetzki C, Zalc B, Schwartz JC, Sokoloff P. (1998) A rat G protein-coupled receptor selectively expressed in myelin-forming cells. Eur J Neurosci, 10 (3): 1045-53. [PMID:9753172]

4. An S, Bleu T, Hallmark OG, Goetzl EJ. (1998) Characterization of a novel subtype of human G protein-coupled receptor for lysophosphatidic acid. J Biol Chem, 273 (14): 7906-10. [PMID:9525886]

5. Bandoh K, Aoki J, Taira A, Tsujimoto M, Arai H, Inoue K. (2000) Lysophosphatidic acid (LPA) receptors of the EDG family are differentially activated by LPA species. Structure-activity relationship of cloned LPA receptors. FEBS Lett, 478 (1-2): 159-65. [PMID:10922489]

6. Cheng PTW, Kaltenbach 3rd RF, Zhang H, Shi J, Tao S, Li J, Kennedy LJ, Walker SJ, Shi Y, Wang Y et al.. (2021) Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases. J Med Chem, 64 (21): 15549-15581. [PMID:34709814]

7. Choi JW, Herr DR, Noguchi K, Yung YC, Lee CW, Mutoh T, Lin ME, Teo ST, Park KE, Mosley AN, Chun J. (2010) LPA receptors: subtypes and biological actions. Annu Rev Pharmacol Toxicol, 50: 157-86. [PMID:20055701]

8. Chrencik JE, Roth CB, Terakado M, Kurata H, Omi R, Kihara Y, Warshaviak D, Nakade S, Asmar-Rovira G, Mileni M et al.. (2015) Crystal Structure of Antagonist Bound Human Lysophosphatidic Acid Receptor 1. Cell, 161 (7): 1633-43. [PMID:26091040]

9. Contos JJ, Chun J. (1998) Complete cDNA sequence, genomic structure, and chromosomal localization of the LPA receptor gene, lpA1/vzg-1/Gpcr26. Genomics, 51 (3): 364-78. [PMID:9721207]

10. Contos JJ, Fukushima N, Weiner JA, Kaushal D, Chun J. (2000) Requirement for the lpA1 lysophosphatidic acid receptor gene in normal suckling behavior. Proc Natl Acad Sci USA, 97 (24): 13384-9. [PMID:11087877]

11. Dancs PT, Ruisanchez É, Balogh A, Panta CR, Miklós Z, Nüsing RM, Aoki J, Chun J, Offermanns S, Tigyi G et al.. (2017) LPA1 receptor-mediated thromboxane A2 release is responsible for lysophosphatidic acid-induced vascular smooth muscle contraction. FASEB J, 31 (4): 1547-1555. [PMID:28069828]

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