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Phosphoinositide 3-kinase catalytic subunit alpha isoform (PI3Kα)
- Target
- PI3Kα
- Molecular classification
- Enzyme, Lipid Kinase, Phosphoinositide 3-Kinase, Class IA Phosphoinositide 3-Kinase
01
Overview
Phosphoinositide 3-kinase catalytic subunit alpha isoform (PI3Kα) is a lipid kinase that plays a crucial role in cell signaling pathways involved in growth, proliferation, survival, metabolism, and motility. It catalyzes the conversion of PI(4,5)P₂ to PI(3,4,5)P₃, a key second messenger that activates downstream effectors like AKT. PI3Kα is frequently mutated or aberrantly activated in various cancers, making it a significant therapeutic target.
- Other names
- PIK3CAp110alpha
02
Mechanism of action
Small molecule inhibitors bind to the ATP-binding pocket of PI3Kα, preventing its kinase activity and downstream signaling.
03
Biological functions
Cell growthCell proliferationCell survivalApoptosis resistanceMetabolismCell migrationCell motilitySignal transduction
04
Disease associations
Cancer
05
Safety considerations
HyperglycemiaDiarrheaRashOther mechanism-based toxicities
06
Interacting drugs
PI3K inhibitors (specific examples to be populated as data becomes readily available and confirmed)
07
Biomarkers
PIK3CA mutations (predictive biomarker for response to PI3Kα inhibitors)PIP3 levels
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