靶向突变p53的小分子药物研究进展  

Advances in small molecular drugs targeted mutant p53

作　　者：王玉玲 苏永南 暴亚锋 杨志宽 牟汉川 张继虹 

机构地区：[1]昆明理工大学医学院衰老与肿瘤分子遗传学实验室,云南昆明650500

出　　处：《中国药理学通报》2018年第3期321-324,共4页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No 8156130180)

摘　　要：肿瘤抑制因子p53蛋白可以调节靶基因转录,控制细胞凋亡、衰老等生命活动,但其容易发生突变,失去抑癌功能,促进肿瘤发生发展。目前p53蛋白已成为治疗肿瘤的热门靶点之一,该文主要介绍以突变p53为靶点恢复构象活性的小分子化合物结构及作用机制。Tumor suppressor p53 protein can regulate the transcription of target genes,to control cell apoptosis,aging and other life activities,but mutant p53 is prone to losing antitumor function,thus promoting tumor development. At present,p53 protein has become one of the hot targets for the treatment of cancer. This article mainly introduces the structure and mechanism of small molecular compounds with restoring activity of mutant p53 as the target.

关 键 词：突变P53 靶点 构象 药物设计 机制 

分 类 号：R-05[医药卫生] R341