新型肿瘤治疗靶点Cdc20的研究进展  

Progress in research on the novel cancer therapeutic target Cdc20

作　　者：乐祥阳 蒯梦妮 李乾斌 陈卓 LE Xiang-yang KUAI Meng-ni LI Qian-bin CHEN Zhuo(Xiang Ya School of Pharmaceutical Sciences, Central South University, Changsha 410013, China)

机构地区：[1]中南大学湘雅药学院,湖南长沙410013

出　　处：《药学学报》2017年第9期1366-1371,共6页Acta Pharmaceutica Sinica

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

摘　　要：细胞分裂后期促进复合物(APC)具有调节细胞周期进展的作用,经细胞分裂周期蛋白20(Cdc20)或Cdc20同系物1(Cdh1)活化后形成两种不同的E3泛素连接酶复合物APC^(Cdc20)或APC^(Cdh1)。Cdc20为促癌因子,Cdh1为抑癌因子,在肿瘤的发生及发展中发挥不同的作用。越来越多的研究表明,Cdc20对肿瘤的发生起促进作用,很多肿瘤中存在Cdc20的高表达。目前Cdc20抑制剂除了apcin外,大部分为非特异性抑制剂,不仅阻断Cdc20与APC的结合,也阻断Cdh1与APC的结合,选择性差。本文就Cdc20在肿瘤发生及发展过程中的作用及其抑制剂进行综述。The anaphase promoting complex（APC） regulates cell cycle progression by forming two functionally distinct E3 ubiquitin ligase complexes, APC^（Cdc20） activated by cell division cycle protein 20（Cdc20） and APC^（Cdh1） activated by Cdc20 homologue 1（Cdh1）, respectively. Cdc20 and Cdh1 have different functions in the occurrence and development of the tumor. Cdc20 is a cancer promoter while Cdh1 suppresses tumorigenesis. Emerging evidence has begun to reveal that Cdc20 has positive functions in tumorigenesis, the overexpression of Cdc20 has been observed in many cancers. Currently, Cdc20 inhibitors, mostly non-specific inhibitors except apcin, not only block the combination between Cdc20 and APC, also block the combination between Cdh1 and APC, which leads to a poor selectivity. In this paper, the Cdc20 role in the development and process of cancers and its inhibitors are reviewed.

关 键 词：肿瘤 细胞分裂周期蛋白20 E3泛素连接酶 抑制剂 

分 类 号：R914[医药卫生—药物化学]