选择性PI3K抑制剂的研究进展  

Research progress of selective PI3K inhibitors

作　　者：吴成军[1] 赵金龙[1] 周志旭[1] 杜磊[1] 柳蓓蓓[1] 孙铁民[1] 

机构地区：[1]沈阳药科大学创新药物研究与设计教育部重点实验室,沈阳110016

出　　处：《中南药学》2014年第4期305-310,384,共7页Central South Pharmacy

基　　金：教育部创新团队发展计划;辽宁省高校创新团队支持资助

摘　　要：磷脂酰肌醇3-激酶(PI3K)是细胞内重要的信号转导分子,在细胞存活、增殖和分化过程中起重要调节作用。PI3K是PI3K/AKT/mT0R信号转导通路中的关键节点蛋白,调控着重要的生命活动。现已证实磷脂酰肌醇3-激酶(PI3Ks)是潜力巨大的药物治疗靶点,特别是PI3Kα现己成为抗肿瘤治疗的重要靶点之一。目前己有多种针对PI3Ks的抑制剂进入临床研究。然而现有抑制剂的化学类型不多且选择性不高、临床应用受局限。因此积极研究和开发结构新颖的PI3K选择性抑制剂对于疾病的靶向治疗具有重要意义。本文将对选择性PI3K抑制剂在抗肿瘤方面的研究进展作一综述。Phosphatidylinositol 3-kinase is an important signal transduction molecule in cells, which plays an important regulatory rolein the process of cell survival, proliferation and differentiation. PI3K is a key node regulating the PI3K/AKT/mTOR signaling transduction pathway of several essential biological processes. It has been proved that PI3Ks are potential targets for chemical therapy, especially PI3Kα as one of the most important targets of anti-tumors. Many PI3K inhibitors have been in early clinic development currently. However, they are limited for the lack of selectivity as well as chemical types. It＇s important to develop novel isoform-specific inhibitors targeting at PI3Ks. This article will review the selective PI3K inhibitors and summarize the antitumor progress.

关 键 词：磷脂酰肌醇3-激酶 选择性PI3K抑制剂 抗肿瘤 

分 类 号：R979.1[医药卫生—药品]