摘要
溴结构域与超末端结构域(BET)在调控细胞周期和介导基因转录中发挥重要作用,与多种疾病关系密切,是表观遗传学的靶点之一。目前已有许多不同结构的BET溴结构域抑制剂被报道,其中多个抑制剂已进入临床试验阶段。本文介绍BET溴结构域的结构和生物学功能,并对选择性和非选择性的BET溴结构域抑制剂作一综述,期望能为科研工作者设计和开发高活性和高选择性的BET溴结构域抑制剂提供新思路。
BET(bromodomain and extra-terminal domain)plays an important role in controlling cell cycle progression and gene transcription.It is involved in kinds of diseases and considered as one of targets in epigenetics.To date,a number of structurally diversified BET bromodomain inhibitors have been reported,w ith quite a few having entered clinical trials.In this review,w e introduced structure and function of BET bromodomain,and especially analyzed and summarized selective and non-selective BET bromodomain inhibitors so as to provide new ideas for scientists of designing and discovering BET bromodomain inhibitors w ith high activity and selectivity.
作者
曹冉
李煜
朱启华
徐云根
CAO Ran;LI Yu;ZHU Qi-hua;XU Yun-gen(Department of Medical Chemistry,China Pharmaceutical University,Nanjing 211198)
出处
《中国药物化学杂志》
CAS
CSCD
北大核心
2020年第6期347-358,共12页
Chinese Journal of Medicinal Chemistry
基金
江苏高等学校优秀科技创新团队项目(2015)
