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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Kα)
- Target
- PI3Kα
- Molecular classification
- Enzyme, Lipid Kinase, Kinase
01
Overview
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3Kα or p110α) is the catalytic subunit of class IA phosphoinositide 3-kinases (PI3Ks). It phosphorylates phosphatidylinositol 4,5-bisphosphate [PI(4,5)P₂] to generate phosphatidylinositol 3,4,5-trisphosphate [PI(3,4,5)P₃], a key regulator of cell growth, proliferation, survival, metabolism, and motility. Aberrant activation or mutation of PIK3CA/PI3Kα is strongly linked to cancer, making it an important therapeutic target.
- Other names
- p110αPIK3CA
02
Mechanism of action
Inhibition of PI3Kα kinase activity, either by competitive binding at the ATP-binding site or by stabilizing inactive conformations.
03
Biological functions
Signal transductionCell growthCell proliferationCell survivalMetabolism regulationInositol phosphate metabolismImmune response
04
Disease associations
Cancer
05
Safety considerations
HyperglycemiaRashDiarrheaDrug resistance
06
Interacting drugs
Alpelisib
4 more in the full profile.
07
Biomarkers
PIK3CA mutationsPIP3 levelsAKT phosphorylation
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