靶向p53-MDM2通路的相关抑制剂研究进展  

Progress on the research of related inhibitors target on p53-MDM2 pathway

作　　者：刘佳敏 付毅红 樊思莉 粱俸铭 谢德文 王贞超[1,2,3] 欧阳贵平 LIU Jiamin;FU Yihong;FAN Sili;LIANG Fengming;XIE Dewen;WANG Zhenchao;OUYANG Guiping(School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,Guizhou,China;State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medcial University,Guiyang 550014,Guizhou,China;Drug Synthetic Engineering Laboratory of Guizhou Province,Guiyang 550025,Guizhou,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025 [2]贵州医科大学药用植物功效与利用国家重点实验室,贵州贵阳550014 [3]贵州省合成药物工程实验室,贵州贵阳550025

出　　处：《化学研究》2020年第4期347-358,共12页Chemical Research

基　　金：药用植物功效与利用国家重点实验室资助项目(FAMP201801K,FAMP201707K);贵州省科技计划项目(黔科合基础[2018]1051)。

摘　　要：p53基因(也称为"基因卫士")是一种抑癌基因,该基因在细胞周期调控、DNA修复、细胞分化和凋亡等方面发挥着重要作用.p53蛋白能与MDM2蛋白形成负反馈调节机制,发挥p53依赖活性.p53-MDM2蛋白为抗肿瘤药物研究的靶点之一,可通过抑制MDM2蛋白或恢复野生型p53蛋白的肿瘤抑制功能,达到治疗人类癌症的目的.本文综述了具有抗肿瘤作用且与p53-MDM2通路相关的抑制剂的研究现状,以期为后续p53靶点药物的研发提供参考.The p53 gene(also called as the guardian of the genome),a well-known tumor suppressor gene,plays a crucial role in cell cycle regulation,DNA repair,cell differentiation,and apoptosis.MDM2 exerts p53-dependent activity mainly by binding to p53 protein to form MDM2-p53 negative feedback loop.The p53-MDM2 protein is one of the targets of antitumor drug.It can treat human cancer by inhibiting MDM2 protein or activating the tumor suppressing function of wild-type p53 protein.This review summarized the research status of inhibitors related to the p53-MDM2 pathway with antitumor effects,in order to lay a foundation for the discovery of antitumor agents targeting p53-MDM2.

关 键 词：P53 MDM2 肿瘤抑制剂 

分 类 号：O626.13[理学—有机化学]