GSK-3β活性调节与肿瘤治疗

被引：20

作者：

陶丽 ^{[1
]}

盛晓波 ^{[1
]}

刘玉萍 ^{[1
]}

韦忠红 ^{[1
]}

王爱云 ^{[1
,2
]}

陆茵 ^{[1
,2
]}

机构：

[1] 南京中医药大学药学院

[2] 南京中医药大学江苏省中药药效与安全性评价重点实验室

来源：

中国药理学通报 | 2014年 / 06期

关键词：

糖原合成酶激酶3β; Wnt/β-catenin信号通路; 绝缘机制; 药物设计; 底物竞争性抑制剂; 肿瘤治疗;

D O I：

暂无

中图分类号：

R730.5 [肿瘤治疗学];

学科分类号：

100214 [肿瘤学];

摘要：

糖原合成酶激酶3β(glycogen synthase kinase 3β,GSK-3β)作为细胞内主要的丝氨酸/苏氨酸家族激酶,其活性异常与多种疾病的发生发展密切相关。值得关注的是,GSK-3β对肿瘤进程的调节是双向的,当扮演"促瘤因子"角色的GSK-3β被抑制时,不可避免阻断了其"抑瘤因子"的功能,使得Wnt/β-catenin信号通路的激活,成为目前靶向肿瘤GSK-3β引起治疗矛盾的焦点。事实上,生物学的绝缘机制可以使GSK-3β在广泛参与细胞内众多信号通路的调节中互不干扰,从而决定了细胞命运。因此,深入了解GSK-3β在不同信号系统中活性调节的具体机制,或者设计底物特异的竞争性抑制剂,对于在靶向GSK-3β的肿瘤治疗中采取选择性的权衡策略具有重大意义。

引用

页码：741 / 744

页数：4

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