摘要
细胞周期蛋白依赖性激酶9(cyclin-dependent kinase 9,CDK9)是CDK家族的一员,属于丝氨酸/苏氨酸蛋白激酶。与其他CDK不同,CDK9在细胞周期调节中不发挥作用,而是主要参与基因的转录延伸过程。CDK9能与相应的细胞周期蛋白结合形成正转录延伸因子b(positive transcription elongation factor b,P-TEFb),激活RNA聚合酶Ⅱ并使转录因子磷酸化,从而促进基因转录延伸。研究表明,CDK9在肿瘤的发病机制中发挥至关重要的作用,使其成为治疗干预的潜在靶标。近年来,CDK9抑制剂相关研究被广泛报道,部分抑制剂已进入临床试验研究。本文探讨了CDK9的结构、功能及其与肿瘤的关系,并综述了近年来CDK9抑制剂研究的最新进展。
Cyclin-dependent kinase 9(CDK9)is a member of the CDK family and belongs to the serine/threonine protein kinases.Unlike other CDK,CDK9 does not play a role in cell cycle regulation but is primarily involved in the process of gene transcription elongation.It can form the P-TEFb complex by binding to the corresponding cyclin,activating RNA polymeraseⅡ,and phosphorylating transcription factors,thereby promoting gene transcription elongation.Research has shown that CDK9 plays a crucial role in the pathogenesis of tumors,making it a potential therapeutic target for intervention.In recent years,the study of CDK9 inhibitors has been widely reported,and some inhibitors have entered clinical trials.This article introduces the structure,function,and relationship of CDK9 with tumors,and reviews the latest development in CDK9 inhibitor research.
作者
曹志豪
曾扬杰
李文欣
张瑞
王举波
任晓东
CAO Zhi-hao;ZENG Yang-jie;LI Wen-xin;ZHANG Rui;WANG Ju-bo;REN Xiao-dong(Medical College,Guizhou University,Guiyang 550025,China;School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2024年第20期2119-2130,共12页
Chinese Journal of New Drugs
基金
贵州省科技计划项目(黔科合基础-ZK[2021]一般556)
贵州大学引进人才科研项目(贵大人基合字(2020)76号)。
