磷脂酰肌醇3-激酶(PI3Ks)蛋白家族介导的PI3K-Akt-mTOR信号传导通路涉及人体众多细胞功能的调节,是近年来抗肿瘤药物研究的重要靶标。Ⅰ型PI3K具有PI3Kα、PI3Kβ、PI3Kδ和PI3Kγ4种关键亚型,这4种亚型各自介导不同的生命活动,因此设计亚型选择性抗肿瘤药物能够增加治疗的选择性,减少毒副作用。本文对于近期PI3K关键亚型抑制剂,特别是PI3Kα和PI3Kδ抑制剂,以及它们在PI3K-Akt-mTOR信号传导通路中的作用进行综述。
Phosphoinositide 3-kinases(PI3Ks) family,consisted in the PI3K-Akt-mTOR signaling pathway,are important oncology targets in research of antitumor drugs and regulate various cellular processes.Among the different PI3 K subtypes,PI3 K class Ⅰ(PI3Kα,PI3Kβ,PI3Kδ and PI3Kγ) plays a key role in the biology of human cancer.Isoform-specific inhibitors will increase the selectivity of therapy and reduce toxicity and side effects.Therefore,In this article,we introduced the selective inhibitors of the class Ⅰ PI3 K isoforms,especially PI3Kα and PI3Kδ inhibitors,and the function in the PI3 K signaling pathway.