摘要
蛋白降解靶向嵌合体(proteolytic targeting chimera,PROTAC)是一类能够通过诱导靶蛋白的多聚泛素化而导致靶蛋白降解的化合物。PROTAC作为双功能分子,具有非常广泛的应用与发展空间。PROTAC是药物研发领域的一个新兴方向,通过降解靶蛋白来调控体内蛋白含量的策略极大地拓展了潜在药物靶标的范围。本文主要简介PROTAC的结构、作用机制、最新研究成果、技术优势以及目前存在的问题。
Proteolysis targeting chimera(PROTAC)are a class of compounds which can induce the poly-ubiquitination of the target proteins and promote their degradation.As a bifunctional molecule,RPOTAC has a wide range of space for application and development.PROTAC is a new direction in the field of drug discovery,and the strategy of regulating protein content in vivo by degrading target proteins greatly expands the range of potential drug targets.In this paper,the structure,mechanism,latest research results,technical advantages and disadvantages of PROTAC were introduced.
作者
王瑞峰
杨博文
赵冬梅
程卯生
WANG Rui-feng;YANG Bo-wen;ZHAO Dong-mei;CHENG Mao-sheng(Key Laboratory of Structure-Based Drug Design & Discovery(Shenyang Pharmaceutical University),Ministry of Education,Shenyang 110016,China)
出处
《中国药物化学杂志》
CAS
CSCD
北大核心
2019年第3期234-240,共7页
Chinese Journal of Medicinal Chemistry
基金
教育部创新团队发展计划
辽宁省高校创新团队支持计划资助
关键词
蛋白降解靶向嵌合体
泛素化
双功能分子
作用机制
proteolysis targeting chimera
ubiquitization
bifunctional molecule
mechanism
