EZH2 是一种重要的表观遗传调控因子，与 SUZ12、EED 和 RbAp46/48 一起形成 PRC2 复合物。作为 PRC2 的关键催化亚基，EZH2 调节着组蛋白 H3K27 的三甲基化，从而促进染色质浓缩并抑制相关靶基因的转录。EZH2 的过度表达和突变严重影响肿瘤的增殖、侵袭和转移。目前，已经研制出了大量高度特异性的 EZH2 抑制剂，其中一些已经开始临床试验。本综述旨在提供 EZH2 抑制剂的分子机制概述，并突出反映近年来发表的专利文献中的研究进展，检索了 Web of Science、SCIFinder、WIPO、USPTO、EPO 和 CNIPA 数据库中的 EZH2 抑制剂和降解剂文献和专利。近年来，已经发现了多种结构差异性较大的 EZH2 抑制剂，包括 EZH2 可逆抑制剂、EZH2 不可逆抑制剂、基于 EZH2 的双重抑制剂和 EZH2 降解剂。尽管面临多重挑战，EZ的抑制剂为各种疾病的治疗，如癌症，提供了有前途的潜力。

EZH2 is an important epigenetic regulator that forms the PRC2 complex with SUZ12, EED and RbAp46/48. As the key catalytic subunit of PRC2, EZH2 regulates the trimethylation of histone H3K27, which in turn promotes chromatin condensation and represses the transcription of relevant target genes. EZH2 overexpression and mutations are strictly related to tumor proliferation, invasion and metastasis. Currently, a large number of highly specific EZH2 inhibitors have been developed and some have already been in clinical trials.The aim of the present review is to provide an overview of the molecular mechanisms of EZH2 inhibitors and to highlight the research advances in the patent literature published from 2017 to date. A search of the literature and patents for EZH2 inhibitors and degraders was performed using the Web of Science, SCIFinder, WIPO, USPTO, EPO and CNIPA databases.In recent years, a great number of structurally diverse EZH2 inhibitors have been identified, including EZH2 reversible inhibitors, EZH2 irreversible inhibitors, EZH2-based dual inhibitors and EZH2 degraders. Despite the multiple challenges, EZH2 inhibitors offer promising potential for the treatment of various diseases, such as cancers.