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磷脂酰肌醇3-激酶(phosphatidylinositol-3 kinase,PI3K)是细胞内重要的信号分子,它具有调节细胞增殖、分化、代谢、凋亡等功能。PI3K的基因易发生突变和扩增,从而导致PI3K被激活,与肿瘤的形成和发展密切相关。IA型的PI3K及其下游的信号分子组成的通路参与调节肿瘤细胞的增殖、存活、黏附、迁移等活动。综述了IA型PI3K——PI3Kα、PI3Kβ和PI3Kδ与肿瘤发生、发展的关系,列举了20个具有代表性的IA型PI3K抑制剂,并讨论了它们的分子抑制机制。
Phosphatidylinositol 3-kinase (PI3K) is an intracellular signaling molecule that regulates cell proliferation, differentiation, metabolism and apoptosis. PI3K gene prone to mutation and amplification, resulting in PI3K is activated, and tumor formation and development are closely related. IA-type PI3K and its downstream signal pathways constitute the pathway involved in regulating tumor cell proliferation, survival, adhesion, migration and other activities. This review summarizes the relationship between type IA PI3K - PI3Kα, PI3Kβ and PI3Kδ and tumorigenesis and progression. Twenty typical PI3K inhibitors of IA type are listed and their molecular inhibition mechanisms are discussed.