摘要
细胞周期是维持细胞正常生命活动的基本特征。一个完整的细胞周期受到多种蛋白酶的调控。研究表明,几乎所有肿瘤的发生都与细胞周期调控机制紊乱所导致的细胞生长分化受阻及凋亡异常有关。细胞周期蛋白依赖性激酶(CDK)是细胞周期调控的核心,CDK与相应的细胞周期蛋白结合形复合物,并通过细胞周期蛋白的周期性表达和降解,推动细胞周期各时相的有序进行。因此,以CDK为靶点的药物可以阻断细胞周期,控制细胞增长,从而达到抗肿瘤的目的。本文就CDK的结构和功能,及其抑制剂的化学结构类型及构效关系进行综述。
Cell cycle is the basic process of cell life activities. A complete cell cycle is regulated by a series of proteases.Researches show that almost all tumors relate to abnormal cell growth, differentiation and apotosis which are caused by cell cycle regulation disorder.Cyclin-dependent kinases （CDK） are the core of cell cycle regulation, which are essential for initiating and processing the cell cycle as they interact with their cyclin partners. CDK contribute to well-organized cell cycle by facilitating periodic expression and degradation of cyclins. Therefore the drugs that target CDK could spur the process of cancer cell apoptosis through interrupting the cell cycle. In this article, we provide an introduction of the structure and function of CDK, the CDK inhibitors in various chemical structures and their structure-activity relationship.
出处
《国际药学研究杂志》
CAS
CSCD
2014年第1期37-44,56,共9页
Journal of International Pharmaceutical Research
基金
南充市科技计划资助项目(13A0033)
关键词
细胞周期蛋白依赖性激酶
抑制剂
抗肿瘤
构效关系
eyclin-dependent kinases
inhibitors
antitumor
structural-activity relationship
