Target intelligence / Profile preview

Lysophosphatidic acid receptor 2 (LPAR2)

Target
LPAR2
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

Lysophosphatidic acid receptor 2 (LPAR2) is a class A, G protein-coupled receptor encoded by the LPAR2 gene in humans, mediating cellular responses to the lipid mediator lysophosphatidic acid (LPA). LPAR2 couples predominantly with Gi and Gq proteins, triggering downstream signaling responsible for calcium mobilization, cytoskeletal changes, cell proliferation, anti-apoptosis, and DNA repair. It is highly expressed in immune cells and reproductive organs, with moderate expression in various adult tissues. LPAR2 has significant roles in cancer biology, inflammation, and tissue injury, including mucosal protection from NSAID-induced damage through promoting prostaglandin E production. Several selective agonists (e.g., DBIBB, GRI977143) have been developed, aiming for cytoprotection and tissue repair. It is considered a promising therapeutic target, but safety and specificity concerns persist due to its widespread physiological and pathological roles.

Other names
Edg4Pbx4pre-B-cell leukemia transcription factor 4endothelial differentiation gene 4lysophosphatidic acid G-protein-coupled receptor 4
02

Mechanism of action

Selective agonism of LPAR2 (promoting mucosal integrity, cytoprotection via prostaglandin E upregulation, facilitating cell survival/proliferation, and mitigation of apoptosis and tissue injury)

03

Biological functions

Signal transductionCell proliferationCell migrationCell survivalCa2+ mobilizationAnti-apoptosisDNA damage repairImmune response
04

Disease associations

CancerInflammationNeurodegenerative diseaseCardiovascular diseaseLiver diseaseMetabolic diseaseGastrointestinal injury (e.g., NSAID-induced enteropathy)
05

Safety considerations

Potential impact on multiple physiological processes (inflammation, fibrosis, proliferation)non-specificity of early agonistspossible unintended effects on mucosal barrier or proliferation-linked pathologies
06

Interacting drugs

DBIBB (2-[[[4-(1,3-dioxo-1H-benz[de]isoquinolin-2(3H)-yl)butyl]amino]sulfonyl]-benzoic acid)

4 more in the full profile.

07

Biomarkers

Expression of LPAR2 in leukocytestestiskidneyprostatespleenthymuspancreasand various cancers (as tumor biomarker or for stratification based on receptor status)

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