Target intelligence / Profile preview

Lysophosphatidic acid pathway (LPA pathway)

Target
LPA pathway
Molecular classification
G protein-coupled receptor (for LPA receptors such as LPA₁–LPA₆), Enzyme (for autotaxin, which generates LPA), Lipid mediator pathway
01

Overview

The **lysophosphatidic acid pathway** involves signaling by lysophosphatidic acid, a bioactive phospholipid, through a family of G protein-coupled receptors (LPA₁–LPA₆) and key biosynthetic enzymes such as autotaxin. This pathway controls a range of cellular functions including proliferation, survival, migration, and angiogenesis, and contributes to pathological processes like cancer progression, fibrosis, and inflammation. Therapeutic interest centers on antagonists of LPA receptors and inhibitors of autotaxin for the treatment of oncology, fibrotic, and inflammatory diseases[1][2][3][4].

Other names
Lysophosphatidic acid signaling pathwayLPA signaling
02

Mechanism of action

Antagonism of LPA receptors to inhibit downstream GPCR signaling; Inhibition of autotaxin enzymatic activity to reduce LPA production

03

Biological functions

Signal transductionCell proliferationCell migration/invasionCell survival/anti-apoptosisAngiogenesisFibrosis/tissue repair
04

Disease associations

Cancer (including ovarian, hepatocellular, and others)Fibrosis (lung, hepatic, radiation-induced)InflammationNeurodegenerative diseaseCardiovascular disease
05

Safety considerations

Off-target effects due to wide physiological roles of LPA and its receptorsPotential for impaired tissue repair and wound healingRisk of affecting normal vascular and immune processes
06

Interacting drugs

SAR100842 (LPA₁ antagonist, for systemic sclerosis)

5 more in the full profile.

07

Biomarkers

Elevated plasma LPA level (prognostic for ovarian cancer)LPA receptor expression levels (e.g., LPA₁, LPA₂, LPA₃, LPA₆ in tissues)mRNA expression of LPA receptors in tumors as prognostic indicators

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