Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes involved in various cellular functions, including cell growth, proliferation, differentiation, motility, survival, and intracellular trafficking. These enzymes play a crucial role in cellular signaling pathways and are implicated in cancer and other diseases .
Phosphoinositide 3-kinase alpha (PI3Kα) is a class I PI3K composed of a catalytic subunit (p110α) and a regulatory subunit (p85α). The p110α subunit is encoded by the PIK3CA gene, while the p85α subunit is encoded by the PIK3R1 gene . The catalytic subunit p110α uses ATP to phosphorylate phosphatidylinositols (PtdIns), PtdIns4P, and PtdIns(4,5)P2 .
The involvement of p110α in human cancer has been hypothesized since 1995. Genetic and functional studies have shown that common activating PIK3CA missense mutations are present in various human tumors . These mutations are particularly prevalent in breast cancers, with enrichment in the luminal and human epidermal growth factor receptor 2-positive subtypes (HER2+) . The three hotspot mutation positions (GLU542, GLU545, and HIS1047) have been widely reported .
Phosphoinositide 3-kinase alpha Bovine Recombinant is a glycosylated protein with a molecular weight of approximately 83.5 kDa for the p85α chain and 124.3 kDa for the p110α chain . This recombinant protein is used in various research applications to study the PI3K pathway and its role in cellular signaling and cancer.
Due to the association between p110α and cancer, it is considered an appropriate drug target. Pharmaceutical companies are designing and characterizing potential p110α isoform-specific inhibitors . The presence of PIK3CA mutations may also predict the response to certain therapies, such as aspirin therapy for colorectal cancer .