Target intelligence / Profile preview

Phosphatidylinositol 3-Kinase Activity (PI3K Activity)

Target
PI3K Activity
Molecular classification
Enzyme, Lipid Kinase
01

Overview

Phosphatidylinositol 3-kinase (PI3K) activity refers to the enzymatic function of a family of lipid kinases that phosphorylate the 3′-hydroxyl group of the inositol ring in phosphoinositides. This modification generates key signaling lipids, most notably phosphatidylinositol (3,4,5)-trisphosphate (PIP3), which act as second messengers in numerous cellular processes. PI3K activity is central to cell growth, proliferation, survival/apoptosis regulation, metabolism, motility/migration, and intracellular vesicle trafficking. Dysregulation or mutation-induced hyperactivation of the PI3K pathway occurs frequently in cancer (~one-third of tumors). Several small-molecule inhibitors targeting specific isoforms have been developed for cancer therapy.

Other names
PI3K enzymatic activityPhosphoinositide 3-kinase activityPI3K signaling pathway
02

Mechanism of action

Inhibition of phosphatidylinositol 3-kinase activity, leading to decreased PIP3 production and downstream signaling.

03

Biological functions

Signal transductionCell growthCell proliferationSurvival/apoptosis regulationMetabolismMotility/migrationIntracellular vesicle trafficking
04

Disease associations

CancerDiabetesAging-related diseasesInflammation
05

Safety considerations

HyperglycemiaImmune-related adverse eventsElevated liver enzymes
06

Interacting drugs

Idelalisib

1 more in the full profile.

07

Biomarkers

PIK3CA mutationsPTEN loss

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