Target intelligence / Profile preview

Lysophosphatidic acid receptor signaling pathway (LPA signaling pathway)

Target
LPA signaling pathway
Molecular classification
Other
01

Overview

The lysophosphatidic acid (LPA) signaling pathway refers to a group of extracellular signaling events mediated principally through G protein-coupled receptors (GPCRs) known as LPA receptors (LPA1–6), upon binding the bioactive lipid lysophosphatidic acid. This pathway regulates a wide range of biological functions, including cellular survival, proliferation, differentiation, migration, and adhesion, impacting diverse physiological processes such as nervous system development, vasculature formation, immune regulation, and tissue repair. LPA signaling has been implicated in several pathological processes, including cancer progression, fibrosis, inflammation, neurodegeneration, and cardiovascular disease. Drug candidates target this pathway by modulating receptor activity (agonists and antagonists) or by inhibiting LPA production, notably via autotaxin inhibition. Pathway targeting is challenged by pathway complexity, receptor subtype redundancy, and pleiotropy, making it difficult to fully separate beneficial from adverse effects.

Other names
LPA pathwayLPA receptor signalinglysophosphatidic acid signalingLPA signaling
02

Mechanism of action

LPA receptor antagonism, LPA receptor agonism, Enzyme inhibition (e.g., autotaxin inhibitors)

03

Biological functions

Signal transductionCell proliferationCell migrationCell survivalDifferentiationAdhesion
04

Disease associations

CancerFibrosisNeurodegenerative diseaseCardiovascular diseaseInflammation
05

Safety considerations

On-target effects on wound healing, immunity, vascular permeabilityOff-target effects in tissues expressing LPA receptorsTherapeutic challenge of pathway redundancy
06

Interacting drugs

AM966

5 more in the full profile.

07

Biomarkers

Lysophosphatidic acid (LPA) plasma levelsAutotaxin activity

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