靶向抑制CDK4/6的肿瘤治疗基础研究与临床应用进展  

Progress in basic research and clinical application of CDK4/6 inhibitor in tumor therapy

作　　者：吴丽梅 程丽艳[1] 郑晓亮[1] 王孝举[1] WU Limei;CHENG Liyan;ZHENG Xiaoliang;WANG Xiaoju(Center for Molecular Medicine,Zhejiang Academy of Medical Sciences,Hangzhou 310013,Zhejiang,China)

机构地区：[1]浙江省医学科学院分子医学中心

出　　处：《中国临床药理学与治疗学》2019年第9期1065-1069,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家自然科学基金(81773626);浙江省自然科学基金(LQY19H160001)

摘　　要：周期蛋白依赖性激酶4/6(cyclin-dependent kinase 4/6,CDK4/6)是一类丝氨酸/苏氨酸激酶,通过与细胞周期蛋白D(cyclin D)结合,调节视网膜母细胞瘤蛋白(Rb)的磷酸化状态,Rb磷酸化后与E2F转录因子分离,释放的E2F可以自由激活一系列基因表达,参与DNA复制和细胞分裂,从而介导细胞G 1/S期转换,影响细胞周期的进程。近年研究发现CDK4/6在多种肿瘤发生和发展过程中起着核心作用,已成为临床多种肿瘤治疗的重要分子靶点。本文将对CDK4/6与肿瘤的关系以及CDK4/6抑制剂临床应用的最新研究进展做一综述。Cyclin-dependent kinase 4/6(CDK4/6)is a serine/threonine kinase that regulates the phosphorylation state of retinoblastoma protein(Rb)by binding to cyclin D.Phosphorylated Rb releases E2F that freely activates a series of gene expression to participate in DNA replication and cell division,which mediates cell G 1/S phase transition,affects the progression of the cell cycle.Recent studies have found that CDK4/6 plays a central role in tumorigenesis and development,and has become an important molecular target for clinical treatment of various tumors.This article will review the latest research progress in the relationship between CDK4/6 and tumors and the clinical application of CDK4/6 inhibitors.

关 键 词：细胞周期依赖性激酶4/6 细胞周期蛋白D CDK4/6抑制剂 肿瘤靶向治疗 

分 类 号：R73[医药卫生—肿瘤]