MEK抑制剂的研究进展  

Research Progress of MEK Inhibitors

作　　者：蒯梦妮 乐祥阳 李乾斌 胡高云 KUAI Mengni;LE Xiangyang;LI Qianbin;HU Gaoyun(Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, Hunan, 410013, China)

机构地区：[1]中南大学湘雅药学院,湖南长沙410013

出　　处：《肿瘤药学》2017年第5期513-522,共10页Anti-Tumor Pharmacy

基　　金：国家自然科学基金资助项目(81573287);湖南省自然科学基金(2016JJ2162)

摘　　要：RAF-MEK-ERK通路的激活在癌细胞的增殖、分化、侵袭和转移等过程中发挥着重要作用,已成为抗肺癌药物研究的重要通路。目前,虽然对于MEK抑制剂的基础研究得到了较大进展,但临床疗效不足和耐药现象等限制了其进一步发展。因此,对于新型MEK抑制剂和双通路或多通路抑制剂的需求成为了科研工作者新的研究方向,对联合用药和个体化用药也提出了更高的要求。本文介绍了早期MEK抑制剂,总结了MEK抑制剂的耐药机制,并对其最新研究进展进行综述。RAF-MEK-ERK pathway plays a pivotal role in the process of tumor proliferation,differentiation,invasion and metastasis.They are now considered as significant targets for anticancer drug discovery.The purpose of this paper is to expound the MEK inhibitors,latest research progress and future development direction of MEK inhibitors.This article firstly introduced the early MEK inhibitors,followedby the introduction to MEK inhibitors of drug resistance mechanism,finally discussed the newfound MEK inhibitors.At present,although theexploring of MEK inhibitors gets much achievement,we still need further development of MEK inhibitors to provide research direction in theface of the lack of clinical curative effect and drug resistance.As for the new type of MEK inhibitors,more double channel pathway inhibitorneed,more scientific research workers,the combination and individualized medication use is also up to higher requirements.

关 键 词：MEK抑制剂 癌症 耐药性 

分 类 号：R979.1[医药卫生—药品]