蛋白激酶B/Akt抑制剂

磷脂酰肌醇-3-激酶(phosphatidylinositol 3-kinase,PI3K)/蛋白激酶B(protein kinase B,PKB/Akt)信号通路在细胞生长与存活中起着关键作用,PI3K/Akt通路的过度激活在多种肿瘤中常见。Akt激酶本身以及Akt激酶上游调节分子,例如PTEN和PI3K,在超过50%的人类肿瘤中均有异常变化。因此Akt成为肿瘤预防和肿瘤靶向治疗的热点之一。许多小分子化合物通过不同机制抑制Akt活性,根据小分子抑制剂与激酶的结合部位和化学结构不同,主要分为ATP竞争性抑制剂、Akt变构抑制剂和磷脂酰肌醇类似物抑制剂。本文综述了PI3K/Akt通路与肿瘤的关系和Akt抑制剂的研究现状,为新型抗癌药物的设计研究提供参考。

Research progress of protein kinase B/Akt inhibitors

PI3K(phosphatidylinositol 3-kinase)/Akt(protein kinase B,PKB) signaling pathway plays a key role in cell growth and survival.Excessive activation of PI3K/Akt pathway has been found in many tumors.In more than 50% of human tumors,Akt or/and its upstream regulatory molecules(such as PTEN and PI3K) changes abnormally.So Akt has become a hot target for cancer prevention and therapy.Recently,many effective small-molecule Akt inhibitors with different mechanisms have been found.According to the binding site and/o...