Target intelligence / Profile preview

Phospholipase A2 group IB (PLA2G1B) (PLA2G1B)

Target
PLA2G1B
Molecular classification
Enzyme, Hydrolase, Phospholipase, Secretory phospholipase A2
01

Overview

Phospholipase A2 group IB (PLA2G1B) is a calcium-dependent secretory enzyme primarily synthesized in the pancreas as an inactive zymogen and activated by trypsin in the duodenum (UniProt P04054). Its primary physiological role is the digestion of dietary phospholipids into lysophospholipids and free fatty acids, facilitating lipid absorption (PMID: 22561061). Beyond digestion, PLA2G1B acts as a ligand for the phospholipase A2 receptor (PLA2R1), influencing cell proliferation, migration, and hormone release (PMID: 11035015). Pathologically, elevated levels are associated with acute pancreatitis and chronic metabolic conditions; research indicates that PLA2G1B deficiency or inhibition can protect against diet-induced obesity and insulin resistance (PMID: 25624355). In the context of drug development, it is targeted to manage inflammatory cascades and metabolic disorders, though achieving isoform specificity remains a significant challenge (PubChem CID 155160).

Other names
Secretory phospholipase A2 group IBPancreatic phospholipase A2Phosphatidylcholine 2-acylhydrolase 1BsPLA2-IBPLA2G1B
02

Mechanism of action

Inhibition of the enzymatic hydrolysis of the sn-2 ester bond of phospholipids, preventing the release of free fatty acids and lysophospholipids (PMID: 11035015).

03

Biological functions

Lipid metabolismDigestionCell signalingPhospholipid hydrolysisCell proliferation
04

Disease associations

PancreatitisObesityDiabetes mellitusInflammationHyperlipidemia
05

Safety considerations

Potential for gastrointestinal malabsorption of lipidsOff-target inhibition of other sPLA2 isoformsSystemic inflammatory response modulation
06

Interacting drugs

Varespladib

1 more in the full profile.

07

Biomarkers

Serum sPLA2 activityPLA2G1B protein levelsLysophosphatidylcholine levels

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