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Phosphoinositide 3-kinase alpha (for PI3Kα, encoded by the PIK3CA gene) and Phosphoinositide 3-kinase delta (for PI3Kδ, encoded by the PIK3CD gene) (PI3Kα (p110α) and PI3Kδ (p110δ))
- Target
- PI3Kα (p110α) and PI3Kδ (p110δ)
- Molecular classification
- Enzyme (Lipid kinase), Class I phosphoinositide 3-kinase
01
Overview
Phosphoinositide 3-kinases alpha and delta are members of the Class I PI3K family of lipid kinases, which catalyze the phosphorylation of phosphatidylinositol lipids, generating PIP3 and activating key intracellular signaling pathways involved in cell survival, proliferation, and metabolism. PI3Kα is predominantly expressed in many tissues and is often activated by mutations in cancer; PI3Kδ is mainly expressed in leukocytes and plays a crucial role in immune cell function, making it a therapeutic target in both hematologic malignancies and inflammatory diseases. Pharmaceutical inhibition of these isoforms is clinically validated but associated with isoform-specific safety risks, such as metabolic and immunological disturbances.
- Other names
- PI3K alpha (PI3Kα)PI3K delta (PI3Kδ)p110α (for PI3Kα)p110δ (for PI3Kδ)PIK3CA (gene for PI3Kα)PIK3CD (gene for PI3Kδ)
02
Mechanism of action
Small molecule inhibitors block kinase activity, preventing phosphorylation of phosphatidylinositol (4,5)-bisphosphate (PIP2) to PIP3, inhibiting downstream signaling (AKT, mTOR, etc.), resulting in reduced cell growth/survival
03
Biological functions
Signal transduction (PI3K/AKT pathway)Cell proliferationCell survivalMetabolism regulationImmune responseCell growthApoptosis inhibitionMotility
04
Disease associations
Cancer (mutations, activation)InflammationImmunodeficiencyAutoimmune diseaseOther proliferative disorders
05
Safety considerations
Hyperglycemia (PI3Kα inhibition disrupts insulin signaling)Immune suppression/infections (PI3Kδ inhibition impairs B-cell and T-cell function)Diarrhea, rash, hepatotoxicity (class-related)Possible cardiovascular toxicity
06
Interacting drugs
Alpelisib (BYL-719, selective PI3Kα inhibitor)
4 more in the full profile.
07
Biomarkers
PIK3CA mutation status (PI3Kα)PIK3CD gene expression (PI3Kδ)PIP3 cellular levelsActivated/phosphorylated AKTTumor genotype (especially for patient stratification in cancer therapy)
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