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Target intelligence / Profile preview
Phosphatidylinositol 3-kinase alpha isoform (PI3Kα)
- Target
- PI3Kα
- Molecular classification
- Enzyme, Lipid kinase, PI3K family member
01
Overview
Phosphatidylinositol 3-kinase alpha isoform (PI3Kα) is a lipid kinase that plays a crucial role in cell growth, proliferation, survival, and metabolism. It functions as a heterodimer composed of a catalytic subunit (p110α) and a regulatory subunit (p85α). PI3Kα catalyzes the phosphorylation of phosphatidylinositol-(4,5)-bisphosphate [PIP₂] to generate phosphatidylinositol-(3,4,5)-trisphosphate [PIP₃], activating downstream signaling cascades involving AKT and mTOR pathways. Aberrant activation of PI3Kα, often due to PIK3CA gene mutations, is implicated in various cancers, particularly breast cancer, making it a key target for cancer therapy. Several small-molecule inhibitors, such as BYL719/alpelisib, target PI3Kα, aiming to block its activity and disrupt the signaling pathways that drive tumor growth.
- Other names
- PIK3CAp110α/p85α complex
02
Mechanism of action
Inhibition of PI3Kα activity
03
Biological functions
Phosphorylation of PIP₂ to PIP₃Activation of AKT/mTOR pathwayCell growthCell proliferationCell survivalMetabolism
04
Disease associations
Cancer
05
Safety considerations
Potential for off-target effectsResistance development
06
Interacting drugs
BYL719
1 more in the full profile.
07
Biomarkers
PIK3CA mutations (e.g., E542K, E545K, H1047R)
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