Target intelligence / Profile preview

Phosphatidylinositol 3-Kinase Gamma Subunit (PI3Kγ)

Target
PI3Kγ
Molecular classification
Lipid Kinase, Phosphoinositide 3-Kinase (PI3K), Enzyme
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Overview

Phosphatidylinositol 3-kinase gamma (PI3Kγ) is a lipid kinase and the only member of class IB PI3Ks. It plays a crucial role in immune cell signaling, regulating chemotaxis, cytokine release, and ROS generation. PI3Kγ exists as a heterodimer, composed of a catalytic subunit (p110γ) and a regulatory subunit (p101 or p84/p87). It is activated downstream of GPCRs and other receptor types, making it a key therapeutic target for inflammatory diseases and cancer.

Other names
PI3K gammaPIK3CGp110γp101/p110γ complexp84/p110γ complexp87/p110γ complex
02

Mechanism of action

PI3Kγ phosphorylates phosphatidylinositol 4,5-bisphosphate [PI(4,5)P₂] to generate phosphatidylinositol 3,4,5-trisphosphate [PIP₃], a key second messenger in cell signaling. Inhibitors block this phosphorylation.

03

Biological functions

Signal transductionImmune responseCell migrationCytokine productionReactive oxygen species (ROS) generationRegulation of cardiac electrophysiology
04

Disease associations

Inflammatory diseasesCancerAutoimmunityCardiovascular disease
05

Safety considerations

Potential for immunosuppressionOff-target effects due to PI3K family homology

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