General Information of the Protein
Protein ID |
PT03925
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Protein Name |
Lysophosphatidic acid receptor 1
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Secondarily Protein Name |
Lysophosphatidic acid receptor Edg-2
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Gene Name |
LPAR1
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Secondarily Gene Name |
EDG2
LPA1
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Sequence |
MAAISTSIPVISQPQFTAMNEPQCFYNESIAFFYNRSGKHLATEWNTVSKLVMGLGITVCIFIMLANLLVMVAIYVNRRFHFPIYYLMANLAAADFFAGLAYFYLMFNTGPNTRRLTVSTWLLRQGLIDTSLTASVANLLAIAIERHITVFRMQLHTRMSNRRVVVVIVVIWTMAIVMGAIPSVGWNCICDIENCSNMAPLYSDSYLVFWAIFNLVTFVVMVVLYAHIFGYVRQRTMRMSRHSSGPRRNRDTMMSLLKTVVIVLGAFIICWTPGLVLLLLDVCCPQCDVLAYEKFFLLLAEFNSAMNPIIYSYRDKEMSATFRQILCCQRSENPTGPTEGSDRSASSLNHTILAGVHSNDHSVV
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Organism |
Homo sapiens, Human
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Protein Classification |
Membrane receptor
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Family A G protein-coupled receptor
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Small molecule receptor (family A GPCR)
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Lipid-like ligand receptor (family A GPCR)
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EDG receptor
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Function |
Receptor for lysophosphatidic acid (LPA) (PubMed:9070858, PubMed:19306925, PubMed:25025571, PubMed:26091040). 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 (PubMed:26091040). Signaling triggers an increase of cytoplasmic Ca(2+) levels (PubMed:19656035, PubMed:19733258, PubMed:26091040). Activates RALA; this leads to the activation of phospholipase C (PLC) and the formation of inositol 1,4,5-trisphosphate (PubMed:19306925). Signaling mediates activation of down-stream MAP kinases (By similarity). Contributes to the regulation of cell shape. Promotes Rho-dependent reorganization of the actin cytoskeleton in neuronal cells and neurite retraction (PubMed:26091040). Promotes the activation of Rho and the formation of actin stress fibers (PubMed:26091040). Promotes formation of lamellipodia at the leading edge of migrating cells via activation of RAC1 (By similarity). Through its function as LPA receptor, plays a role in chemotaxis and cell migration, including responses to injury and wounding (PubMed:18066075, PubMed:19656035, PubMed:19733258). Plays a role in triggering inflammation in response to bacterial lipopolysaccharide (LPS) via its interaction with CD14. Promotes cell proliferation in response to LPA (By similarity). Inhibits the intracellular ciliogenesis pathway in response to LPA and through AKT1 activation (PubMed:31204173). 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 (By similarity).
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Uniprot ID |
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HGNC ID | |||||
Subcellular Location |
Cell surface
Cell membrane
Endosome
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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 |
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Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000026 , CHO-K1
Cell Line ID: CL000064 , Chem-1
Cell Line ID: CL000011 , CHO
Cell Line ID: CL000389 , CHO-DXB11
Cell Line ID: CL000025 , HEK-293T
Cell Line ID: CL000466 , McA-RH7777
Cell Line ID: CL001056 , MEF-1 [Mouse fibroblast]
Biochemical Assays
Clinical Information about the Protein
Target 1 ( Lysophosphatidic acid receptor 1 (LPAR1) )
Target Type | Clinical trial Target | ||||
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Disease | 2 Target-related Diseases | 2 | |||
1 | Pulmonary fibrosis [ICD-11: CB03.4] | ||||
2 | Scleroderma [ICD-11: 4A42] | ||||
Clinical Trial Drug(s) | 2 Clinical Trial Drugs | 2 | |||
1 | BMS-986278 | Phase 2 | |||
2 | BMS-986020 | Phase 2 |