PI3K-mTOR双重小分子抑制剂的研究进展  

Review of research on dual PI3K-mTOR small molecular inhibitors

作　　者：陈颖[1] 韩进松 宋云龙[1] 周永刚[2] 朱驹[1] 

机构地区：[1]第二军医大学药学院药物化学教研室,上海200433 [2]解放军81医院药剂科,江苏南京210002

出　　处：《药学实践杂志》2014年第5期332-336,359,共6页Journal of Pharmaceutical Practice

摘　　要：PI3K脂激酶家族介导的细胞信号转导通路,调节细胞增殖、分化、凋亡等一系列活动,已经成为治疗肿瘤、炎症等疾病的重要靶标。近来出现了多种结构类型的该通路抑制剂,笔者总结了近年内进入临床研究的具有PI3K-mTOR双重抑制活性的小分子化合物。Objective The phosphoinositide 3-kinase（ PI3K） constituted an important family of lipid kinase enzymes that control a range of cellular proliferation,differentiation and apoptosis through their regulation of a network of signal transduction pathways,which had emerged as important therapeutic targets in the context of cancer and inflammation. Considerable progress had been made in the discovery and development of small molecular inhibitors targeting PI3 K. Progress in dual PI3K-mTOR inhibitors,a number of which had entered early phase clinical trials over recent years was summarized.

关 键 词：磷脂酰肌醇3激酶-哺乳动物雷帕霉素靶蛋白 双重抑制剂 小分子 抗肿瘤 

分 类 号：R979.1[医药卫生—药品]