组蛋白甲基转移酶EZH2及其抑制剂在恶性肿瘤中作用及机制的研究进展

doi:10.3969/j.issn.1004-616x.2024.03.011

摘要/Abstract

摘要： Zeste增强子同源物2(EZH2)是一种组蛋白甲基转移酶，主要通过多梳抑制复合体2(PRC2)依赖的组蛋白H3中27位的赖氨酸三甲基化(H3K27me3)、PRC2依赖的非组蛋白甲基化、不依赖于PRC2的非组蛋白甲基化和不依赖于PRC2的转录激活4种途径调控基因表达。EZH2在多种恶性肿瘤中的表达水平明显上调，参与了肿瘤的发生与发展，与肿瘤的增殖、转移、侵袭、肿瘤分级、肿瘤耐药、不良预后等密切相关。多种EZH2抑制剂在恶性肿瘤生长方面表现出良好抑制效果，延缓了肿瘤的生长与转移，EZH2在恶性肿瘤治疗方面展现了广泛的应用前景。因此，本文对EZH2及其抑制剂在恶性肿瘤中的作用及机制的研究进展进行综述，从而为开发靶向EZH2的肿瘤治疗方法提供理论依据。

关键词: EZH2, Zeste增强子同源物, 肿瘤靶向治疗, 信号通路, 组蛋白甲基转移酶

中图分类号:

R730

黄韵晓, 顾馨集, 朱梦梅, 于兵. 组蛋白甲基转移酶EZH2及其抑制剂在恶性肿瘤中作用及机制的研究进展[J]. 癌变·畸变·突变, 2024, 36(3): 237-243.

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