小分子PI3K/mTOR双重抑制剂研究进展  

Developments of Small Molecule PI3K/mTOR Dual Inhibitors

作　　者：孙成钰[1,2] 周勇[1] 周红英[1] 朱五福[2] 

机构地区：[1]重庆三峡医药高等专科学校附属医院,重庆万州404000 [2]江西科技师范大学药学院,江西南昌330013

出　　处：《江西科技师范大学学报》2016年第6期61-69,共9页Journal of Jiangxi Science & Technology Normal University

基　　金：国家自然科学基金项目(81460527)

摘　　要：PI3K-Akt-mTOR信号通路是细胞内的重要传导通路,且研究发现该通路在肿瘤细胞中高度表达,与肿瘤形成有着密切的联系,抑制该信号通路已经成为肿瘤预防和肿瘤靶向治疗的研究热点。PI3K-Akt-mTOR通路抑制剂主要分为四类:PI3K抑制剂、Akt抑制剂、mTOR抑制剂和PI3K/mTOR双重抑制剂。其中,与单一靶点小分子抑制剂相比,同时作用于PI3K和mTOR双靶点的双重抑制剂以其独特的优势受到了越来越多的关注。本文阐述了近年来小分子PI3K/mTOR双重抑制剂的研究进展。PI3K-Akt-mTOR signaling pathway is an important pathway in cells. The researchers found that PI3K- Akt-mTOR signal pathway is highly expressed in tumor ceils, which shows that it is closely related with tumor formation. And inhibition of this signaling pathway has been one of the research hotspots. PI3K-Akt-mTOR pathway inhibitors include four categories： PI3K inhibitors, Akt inhibitors, mTOR inhibitors and PI3K/mTOR dual inhibitors. Among them, the PI3K/ roTOR dual inhibitors because of its unique advantages attracted more and more attention.This paper systemaiically summarizes the development of smallmolecule PI3K/mTOR dual inhibitors.

关 键 词：P13K-Akt-mTOR信号通路 PI3K/mTOR双重抑制剂 肿瘤 靶向治疗 

分 类 号：R914.1[医药卫生—药物化学]