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Target intelligence / Profile preview
Phosphatidylinositol 3-Kinase Alpha Catalytic Subunit (PI3Kα)
- Target
- PI3Kα
- Molecular classification
- Enzyme, Lipid Kinase, Phosphatidylinositol 3-Kinase, Kinase
01
Overview
PI3Kα is a lipid kinase that phosphorylates PIP2 to produce PIP3, a key second messenger involved in cell growth, proliferation, survival, and metabolism. It is a heterodimer consisting of a catalytic p110α subunit and a regulatory p85 subunit. PI3Kα is frequently mutated in cancer, particularly in breast cancer, and is a target for small molecule inhibitors like BYL719 (alpelisib).
- Other names
- PI3K alphaPIK3CAp110alpha
02
Mechanism of action
ATP-competitive inhibition of PI3Kα kinase activity.
03
Biological functions
Signal transductionCell growthCell proliferationCell survivalMetabolismCell migrationPhospholipid phosphorylation
04
Disease associations
CancerBreast CancerColon CancerEndometrial CarcinomaMetabolic DisordersInsulin Resistance
05
Safety considerations
HyperglycemiaRashDiarrhea
06
Interacting drugs
BYL719
1 more in the full profile.
07
Biomarkers
PIK3CA mutations (e.g., E542K, E545K, H1047R)
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