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Target intelligence / Profile preview
Calcium-independent phospholipase A2 (iPLA2)
- Target
- iPLA2
- Molecular classification
- Enzyme, Phospholipase, PLA2, Group VI PLA2, Patatin-like phospholipases (PNPLAs)
01
Overview
Calcium-independent phospholipase A2 (iPLA2) is a member of the phospholipase A2 superfamily that does not require calcium ions for its catalytic activity. iPLA2 enzymes, also known as patatin-like phospholipases (PNPLAs), catalyze the hydrolysis of fatty acids from the sn-2 position of membrane phospholipids. They play a central role in phospholipid remodeling, fat catabolism, mitochondrial integrity, cell proliferation and differentiation, signal transduction pathways, and cell death mechanisms. Altered function/expression is implicated in metabolic disorders, neurodegenerative diseases and cardiovascular diseases. Inhibitors are being developed, but clinical translation remains under investigation due to the complexity of systemic effects when modulating these pathways.
- Other names
- PNPLA8Membrane-associated iPLA₂γPNPLA9Cytosolic-associated iPLA₂βpatatin-like phospholipasesPNPLAs
02
Mechanism of action
Inhibition of fatty acid hydrolysis from the sn-2 position of membrane phospholipids
03
Biological functions
Phospholipid remodelingFat catabolismMaintenance of mitochondrial integrityCell proliferationCell differentiationSignal transductionCell deathApoptosisNecrosisRegulation of membrane homeostasisGeneration of lipid mediatorsModulation of insulin secretion
04
Disease associations
Metabolic disordersObesity-related complicationsNeurodegenerative diseasesCardiovascular diseasesCancerCNS disordersInflammationDiabetes mellitus type II risk factors
05
Safety considerations
Complexity of systemic effects when modulating these pathways directlyBroad biological roles may lead to off-target effects
06
Interacting drugs
iPLA2 inhibitors
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