Target intelligence / Profile preview

Phosphoinositide 3-kinase gamma (PI3Kγ)

Target
PI3Kγ
Molecular classification
Enzyme, Lipid Kinase, Phosphoinositide 3-Kinase, Class IB PI3K
01

Overview

Phosphoinositide 3-kinase gamma (PI3Kγ) is a lipid kinase and the sole member of the class IB PI3K family. It is primarily activated downstream of G protein–coupled receptors (GPCRs) via Gβγ subunits and plays a crucial role in immune system regulation, particularly in myeloid cells. PI3Kγ regulates chemotaxis, cytokine release, and reactive oxygen species production, key processes in both innate and adaptive immunity. It is implicated as a drug target for cancer and inflammatory diseases due to its central role in immune signaling pathways. It also functions in cell growth, proliferation, metabolism, and acts as a scaffold protein for PKA regulating cAMP levels.

02

Mechanism of action

Inhibition of PI3Kγ kinase activity, preventing PIP3 production and downstream signaling.

03

Biological functions

Immune regulationChemotaxisCytokine releaseReactive oxygen species productionCell growthCell proliferationCell differentiationTissue morphogenesisMetabolismSignal transductioncAMP regulation
04

Disease associations

CancerInflammation

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