Target intelligence / Profile preview

Phospholipase A2 group IB (PLA2G1B)

Target
PLA2G1B
Molecular classification
Enzyme, Secreted phospholipase A2, Lipolytic enzyme, Hydrolase
01

Overview

Phospholipase A2 group IB (PLA2G1B) is a secreted, pancreatic enzyme of the phospholipase A2 family, primarily responsible for catalyzing the hydrolysis of the sn-2 position of glycerophospholipids in dietary and endogenous membranes to release fatty acids (including arachidonic acid) and lysophospholipids. This reaction is calcium-dependent and represents a key step in lipid digestion and in the production of bioactive lipid mediators (such as prostaglandins and leukotrienes), which play diverse roles in inflammation, immune regulation, and cellular signaling[1][2][3]. PLA2G1B is synthesized by pancreatic acinar cells and is also implicated in the modulation of immune cell signaling and in certain pathologies including chronic pancreatitis, cancer, obesity, and infectious disease. It has been studied as a potential therapeutic target due to its central role in lipid mediator biosynthesis and inflammation, although therapeutic inhibition poses challenges due to widespread physiological functions and lack of selective inhibitors[1][2][3].

Other names
Phospholipase A2, group IB (pancreas)PLA2PLA2APPLA2Group IB phospholipase A2Phosphatidylcholine 2-acylhydrolase 1BSecretory phospholipase A2 group IBPancreatic sPLA2
02

Mechanism of action

Inhibitors block hydrolysis of the sn-2 ester bond in phospholipids, reducing production of arachidonic acid and downstream eicosanoids - Some inhibitors block calcium binding, essential for enzymatic activity

03

Biological functions

Lipid metabolismHydrolysis of membrane phospholipidsRelease of arachidonic acid and lysophospholipidsImmune and inflammatory responseRegulation of cell contractionModulation of cell proliferationEnergy metabolism (via N-acyl ethanolamines)Eicosanoid biosynthesis
04

Disease associations

InflammationChronic pancreatitisCancer (tumor invasiveness, signaling)Obesity and metabolic disordersInfection (modulation of immune responses, anti-helminth activity)Retinal and neuronal function
05

Safety considerations

Widespread biological roles may lead to off-target effects when inhibiting PLA2G1B, including gastrointestinal, metabolic, or immunological disturbancesLack of selectivity: Many available inhibitors also inhibit other PLA2 isoforms[2]Disruption of lipid and eicosanoid homeostasis may have pro- or anti-inflammatory consequences depending on the context
06

Interacting drugs

Indole analogs (experimental inhibitors)

3 more in the full profile.

07

Biomarkers

PLA2G1B enzymatic levels in serum or tissue (as a marker for pancreatic and inflammatory diseases)[3]Downstream metabolites (e.g., arachidonic acid, lysophospholipids, eicosanoids) as indirect pharmacodynamic markers

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