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Target intelligence / Profile preview
Phosphoinositide 3-kinase alpha (PI3Kα)
- Target
- PI3Kα
- Molecular classification
- Enzyme, Lipid Kinase, Phosphoinositide 3-Kinase, Class I Phosphoinositide 3-Kinases
01
Overview
Phosphoinositide 3-kinase alpha (PI3Kα) is a lipid kinase involved in key cellular processes such as growth, proliferation, survival, and metabolism. It is a heterodimer consisting of a catalytic subunit p110α (encoded by the PIK3CA gene) and a regulatory subunit p85. PI3Kα phosphorylates PIP2 to produce PIP3, leading to AKT activation and downstream signaling. Aberrant activation or mutation of PI3Kα is frequently observed in various cancers, making it an important therapeutic target.
- Other names
- PI3K alphaPI3KCAp110α
02
Mechanism of action
Inhibition of PI3Kα kinase activity
03
Biological functions
Cell growthCell proliferationCell survivalMetabolismSignal transductionPhosphorylation of membrane lipidsGeneration of second messengers
04
Disease associations
Cancer
05
Safety considerations
Resistance to inhibitorsLack of selectivity between wild-type and mutant forms
06
Interacting drugs
Alpelisib
1 more in the full profile.
07
Biomarkers
PIK3CA mutations
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