General Information of the Protein
Protein ID
PT04593
Protein Name
Lysophosphatidic acid receptor 1
Secondarily
Protein Name
Lysophosphatidic acid receptor Edg-2
Gene Name
LPAR1
Secondarily
Gene Name
Edg2
Gpcr91
Lpa1
Sequence
MAAASTSSPVISQPQFTAMNEQQCFYNESIAFFYNRSGKYLATEWNTVSKLVMGLGITVCVFIMLANLLVMVAIYVNRRFHFPIYYLMANLAAADFFAGLAYFYLMFNTGPNTRRLTVSTWLLRQGLIDTSLTASVANLLAIAIERHITVFRMQLHTRMSNRRVVVVIVVIWTMAIVMGAIPSVGWNCICDIDHCSNMAPLYSDSYLVFWAIFNLVTFVVMVVLYAHIFGYVRQRTMRMSRHSSGPRRNRDTMMSLLKTVVIVLGAFIVCWTPGLVLLLLDVCCPQCDVLAYEKFFLLLAEFNSAMNPIIYSYRDKEMSATFRQILCCQRNENPNGPTEGSDRSASSLNHTILAGVHSNDHSVV
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Organism
Rattus norvegicus, Rat
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Lipid-like ligand receptor (family A GPCR)
>
EDG receptor
Function
Receptor for lysophosphatidic acid (LPA). Plays a role in the reorganization of the actin cytoskeleton, cell migration, differentiation and proliferation, and thereby contributes to the responses to tissue damage and infectious agents. Activates downstream signaling cascades via the G(i)/G(o), G(12)/G(13), and G(q) families of heteromeric G proteins. Signaling inhibits adenylyl cyclase activity and decreases cellular cAMP levels. Signaling triggers an increase of cytoplasmic Ca(2+) levels. Activates RALA; this leads to the activation of phospholipase C (PLC) and the formation of inositol 1,4,5-trisphosphate. Signaling mediates activation of down-stream MAP kinases. Contributes to the regulation of cell shape. Promotes Rho-dependent reorganization of the actin cytoskeleton in neuronal cells and neurite retraction. Promotes the activation of Rho and the formation of actin stress fibers. Promotes formation of lamellipodia at the leading edge of migrating cells via activation of RAC1. Through its function as LPA receptor, plays a role in chemotaxis and cell migration, including responses to injury and wounding. Plays a role in triggering inflammation in response to bacterial lipopolysaccharide (LPS) via its interaction with CD14. Promotes cell proliferation in response to LPA. Inhibits the intracellular ciliogenesis pathway in response to LPA and through AKT1 activation (By similarity). Required for normal skeleton development. May play a role in osteoblast differentiation. Required for normal brain development. Required for normal proliferation, survival and maturation of newly formed neurons in the adult dentate gyrus. Plays a role in pain perception and in the initiation of neuropathic pain.
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Uniprot ID
Primary ID:
P61794

Secondarily ID:
O88584
P56487
P70420
Q5FWS2
Q61130
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Subcellular Location
Cell surface
Cell membrane
Endosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000466 , McA-RH7777
Compound ID Compound Name Compound Formula
CP0784921
potassium O-(2-(heptadec-9-enyl)-1,3-dioxolan-4-yl)methyl O-hydrogenphosphorothioate
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C21H40KO5PS
 1
1
EC50 = 981 nM
   TI
   LI
   LO
   TS
CP0717184
potassium O-((2R,4R)-2-(heptadec-9-enyl)-1,3-dioxolan-4-yl)methyl O-hydrogenphosphorothioate
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C21H40KO5PS
 1
1
EC50 = 1410 nM
   TI
   LI
   LO
   TS
CP0717182
potassium O-((2S,4S)-2-(heptadec-9-enyl)-1,3-dioxolan-4-yl)methyl O-hydrogenphosphorothioate
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C21H40KO5PS
 1
1
EC50 = 1560 nM
   TI
   LI
   LO
   TS
CP0655525
potassium O-((2S,4R)-2-(heptadec-9-enyl)-1,3-dioxolan-4-yl)methyl O-hydrogenphosphorothioate
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C21H40KO5PS
 1
1
EC50 = 1580 nM
   TI
   LI
   LO
   TS
CP0737794
potassium O-((2R,4S)-2-(heptadec-9-enyl)-1,3-dioxolan-4-yl)methyl O-hydrogenphosphorothioate
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C21H40KO5PS
 1
1
EC50 = 2260 nM
   TI
   LI
   LO
   TS
CP0764192
potassium (2-(heptadeca-9,12,15-trienyl)-1,3-dioxolan-4-yl)methyl hydrogenphosphate
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C21H36KO6P
 1
1
EC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0720720
potassium ((2R,4S)-2-(heptadec-9-enyl)-1,3-dioxolan-4-yl)methyl hydrogenphosphate
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C21H40KO6P
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0655527
potassium (2-(heptadec-9-enyl)-1,3-dioxolan-4-yl)methyl hydrogenphosphate
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C21H40KO6P
 2
1
IC50 = 915 nM
   TI
   LI
   LO
   TS
2
Ki = 497 nM
   TI
   LI
   LO
   TS
CP0711336
potassium (2-dodecyl-1,3-dioxolan-4-yl)methyl hydrogenphosphate
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C16H32KO6P
 2
1
IC50 = 1110 nM
   TI
   LI
   LO
   TS
2
Ki = 652 nM
   TI
   LI
   LO
   TS
CP0656066
potassium (2-(6-(4-octylphenyl)hexyl)-1,3-dioxolan-4-yl)methyl hydrogenphosphate
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C24H40KO6P
 2
1
IC50 = 4660 nM
   TI
   LI
   LO
   TS
2
Ki = 1930 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
100% Identity
Protein ID Protein Name Protein Organism
PT06891 Lysophosphatidic acid receptor 1 Mus musculus, Mouse