细胞外信号调节激酶及其抑制剂的研究进展

被引:19
作者
艾俊涛
胡高云
王靓
李代洪
谢欣
李乾斌
机构
[1] 中南大学药学院药物化学系
基金
高等学校博士学科点专项科研基金;
关键词
细胞外信号调节激酶; 抑制剂; 构效关系; 信号通路;
D O I
暂无
中图分类号
R96 [药理学];
学科分类号
100706 [药理学];
摘要
细胞外信号调节激酶(ERK)是一个多功能的丝氨酸/苏氨酸蛋白激酶,是MAPK家族的重要成员,在MAPK信号通路中起着重要的作用。ERK通过磷酸化多种底物蛋白来调节细胞多种生理过程,如细胞生长、分裂、增殖、凋亡等,已成为抗癌药物研发的重要靶点。近年来,基于结构的药物设计策略在ERK抑制剂的研究中已得到广泛的应用。本文对ERK的分子结构、作用机制及直接作用于ERK蛋白的ATP竞争性和非竞争性抑制剂的设计思路、化学结构及构效关系做一综述。
引用
收藏
页码:43 / 52
页数:10
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