Phosphatidylinositol 3-kinase alpha (mutant) (PI3Kα (mutant))

Phosphatidylinositol 3-kinase alpha (PI3Kα) is a lipid kinase that plays a central role in cellular signaling pathways regulating cell growth, survival, proliferation, motility, metabolism, and angiogenesis. The enzyme is a heterodimer composed of a catalytic subunit (p110α), encoded by the PIK3CA gene, and a regulatory subunit (p85α). Mutations in the PIK3CA gene are among the most frequent oncogenic alterations found in human cancers. Common oncogenic mutations include H1047R, E542K, and E545K, which lead to constitutive activation of the PI3Kα pathway and drive oncogenesis. PIK3CA mutant forms are validated drug targets, and specific inhibitors targeting mutant PI3Kα isoforms have been developed.

Inhibition of mutant PI3Kα activity