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Phosphatidylinositol 4,5-bisphosphate 3-Kinase Catalytic Subunit Alpha (PI3Kα)
- Target
- PI3Kα
- Molecular classification
- Lipid kinase, Enzyme
01
Overview
Phosphatidylinositol 3-kinase alpha (PI3Kα) is a lipid kinase that phosphorylates phosphatidylinositol lipids, primarily converting phosphatidylinositol 4,5-bisphosphate [PtdIns(4,5)P2] to phosphatidylinositol 3,4,5-trisphosphate [PIP₃]. It consists of a catalytic subunit p110α (encoded by PIK3CA) and a regulatory subunit, typically p85α. PI3Kα plays a central role in cellular signaling, regulating cell growth, proliferation, survival, motility, and metabolism. Aberrant activation of PI3Kα, particularly through mutations in PIK3CA, is implicated in many cancers, making it an important anticancer therapeutic target. Inhibitors like alpelisib are used to target its activity in specific cancer types.
- Other names
- PI3K alphaPIK3CAp110-alpha
02
Mechanism of action
Inhibition of PI3Kα
03
Biological functions
Cell growthProliferationSurvival/apoptosis resistanceMotility/migrationCell cycle progressionMetabolismProtein synthesisSignal transduction
04
Disease associations
Cancer
05
Interacting drugs
Alpelisib (BYL719)
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