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Target intelligence / Profile preview
Lysophosphatidic Acid Receptor 1 (LPA1R)
- Target
- LPA1R
- Molecular classification
- G protein-coupled receptor, GPCR, Class A GPCR, Rhodopsin-like GPCR, Lysophospholipid receptor
01
Overview
Lysophosphatidic acid receptor 1 (LPA1R) is a G protein-coupled receptor that binds lysophosphatidic acid (LPA), a bioactive phospholipid. Upon ligand binding, LPA1R activates Gαi, Gαq, and Gα12/13 signaling pathways, regulating cell migration, proliferation, differentiation, cytoskeleton dynamics, and inflammation. LPA1R plays roles in neural development, enteric nervous system function, platelet aggregation, smooth muscle contraction, and wound healing. It is implicated in diseases such as pulmonary fibrosis, cancer, and neurodevelopmental disorders. Selective antagonists are under investigation for fibrotic diseases.
- Other names
- LPA₁LPAR₁EDG₂
02
Mechanism of action
Selective antagonism of LPA1R
03
Biological functions
Cell migrationCell proliferationNeurogenesisWound healingSignal transductionCytoskeleton dynamicsPlatelet aggregationSmooth muscle contraction
04
Disease associations
Pulmonary fibrosisCancerNeurodevelopmental disorders
05
Safety considerations
Potential cross-reactivity with phosphorylated endocannabinoids
06
Interacting drugs
ONO‑9780307
07
Biomarkers
LPAR1 overexpression in HPV-positive neoplastic keratinocytes
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