EZH2在肿瘤中的作用及其抑制剂的研究进展
Research advances in role of EZH2 in tumors and its inhibitors
顾馨集 1黄韵晓 1于兵2
作者信息
- 1. 海军军医大学基础医学院,上海 200433
- 2. 海军军医大学基础医学院细胞生物学教研室,上海 200433
- 折叠
摘要
Zeste增强子同源物 2(enhancer of zeste homolog 2,EZH2)的高表达与肿瘤发生、发展、浸润、转移和临床不良预后密切相关.EZH2通过多梳抑制复合体 2(polycomb inhibition complex 2,PRC2)依赖的H3K27甲基化或非组蛋白甲基化、不依赖PRC2的非组蛋白甲基化、直接的蛋白-蛋白相互作用等多种机制激活下游基因,在肿瘤相关基因的转录抑制和肿瘤发生发展调控中起着至关重要的作用.因此,EZH2被认为是一个很有前景的肿瘤治疗靶点.目前,针对EZH2的小分子抑制剂的开发和临床试验已成为一个突出的研究领域.本文综述了EZH2的功能及其调控机制,并重点介绍了热点抑制剂的最新进展,旨在为EZH2及其抑制剂的进一步研究和应用于各种癌症治疗提供参考.
Abstract
The overexpression of of Zeste enhancer homolog 2(EZH2)is closely associated with tumor initiation,progression,invasion,metastasis,and unfavorable clinical prognosis.EZH2 plays a crucial role in the transcriptional repression of tumor-related genes and the regulation of tumorigenesis and development through various mechanisms,including PRC2-dependent H3K27 methylation or non-histone methylation,PRC2-independent non-histone methylation,direct protein-protein interactions,etc,to activate downstream genes.Therefore,EZH2 is considered to be a promising therapeutic target for tumor treatment.Currently,the development and clinical trials of small molecule inhibitors targeting EZH2 have emerged as a prominent area of research.This article reviews functions and regulatory mechanisms of EZH2 and highlights recent advancements in hotspot inhibitors,aiming to provide valuable insights for further research and application in diverse cancer treatments.
关键词
Zeste增强子同源物2/EZH2抑制剂/肿瘤/H3K27me3/表观遗传Key words
enhancer of zeste homolog 2/EZH2 inhibitors/neoplasms/H3K27me3/epigenetics引用本文复制引用
出版年
2024
国家科技期刊平台
NSTL
万方数据