摘要
细胞周期是细胞生命活动的基本特征, 完整的细胞周期受多种蛋白酶的调控, 细胞周期调控失调与细胞癌变有着密切的关系. 细胞周期蛋白依赖性激酶抑制剂(cyclin-dependent kinase inhibitors, CDKI)是以细胞周期蛋白依赖性激酶(cyclin-dependent kinases, CDKs)为靶点, 通过阻断细胞周期控制细胞增殖, 从而达到抗肿瘤的目的. 简述了细胞周期、细胞周期蛋白依赖性激酶抑制剂、细胞周期调控机制与抗肿瘤作用之间的关系, 综述了近年来具有嘌呤骨架的细胞周期蛋白依赖性激酶抑制剂的研究进展, 并展望了其发展趋势.
Cell cycle is a basic characteristic of a cell that associates with its division and duplication. An entire cell cycle is regulated by a series of enzymes. The occurance of cell cycle disorder can lead to an excessive cell proliferation which may trigger cancer. However, the drugs that target cyclin-dependent kinases could spur the process of cancer cell apoptosis through interrupting the cell cycle. In this article, different kinds of cyclin-dependent kinases (CDKs), cyclins, the mechanism of cell cycle regulation and its relation with cancers are reviewed. The CDKs inhibitors with purine scaffold are introduced and their progresses in research and development are briefly discussed.
张京玉, 王清龙, 侯学会, 刘宏民. 具有嘌呤结构的细胞周期蛋白依赖性激酶抑制剂研究进展[J]. 有机化学, 2015, 35(5): 1022-1032
