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Target intelligence / Profile preview
Phosphatidylinositol 3-Kinase Alpha Subunit (PI3Kα)
- Target
- PI3Kα
- Molecular classification
- Lipid Kinase, Enzyme, PI3K, Serine/Threonine Kinase
01
Overview
Phosphatidylinositol 3-kinase alpha subunit (PI3Kα) is a lipid kinase that plays a central role in cellular signaling pathways regulating growth, proliferation, survival, and metabolism. It is a heterodimer composed of a catalytic subunit (p110α) and a regulatory subunit (p85α). PI3Kα phosphorylates phosphatidylinositol-(4,5)-bisphosphate (PIP₂) to generate phosphatidylinositol-(3,4,5)-trisphosphate (PIP₃), activating downstream signaling cascades such as AKT/mTOR. Aberrant activation of PI3Kα, often via gain-of-function mutations, is implicated in various cancers, making it an important therapeutic target. Inhibitors like BYL719 target PI3Kα to modulate its activity and inhibit cancer cell growth.
- Other names
- PI3K alphaPI3K-alphap110α/p85αPIK3CA
02
Mechanism of action
Inhibition of PI3Kα kinase activity
03
Biological functions
Signal transductionCell cycle progressionMetabolismGrowth factor responseCell growthCell survivalCell proliferationMigrationDifferentiationPhosphorylation
04
Disease associations
CancerTherapeutic resistance
05
Safety considerations
HyperglycemiaDiarrheaSkin rash
06
Interacting drugs
BYL719
07
Biomarkers
PIK3CA mutations
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