Xu Mengfei, Xu Chunyan, Wang Rui, Tang Qing, Zhou Qichun, Wu Wanyin, Wan Xinliang, Mo Handan, Pan Jun, Wang Sumei
The Second Clinical Medical College, Guangzhou University of Chinese Medicine, Guangzhou, Guangdong 510120, China.
Department of Oncology, Clinical and Basic Research Team of TCM Prevention and Treatment of NSCLC, Guangdong Provincial Hospital of Chinese Medicine, The Second Clinical College of Guangzhou University of Chinese Medicine, Guangdong Provincial Key Laboratory of Clinical Research on Traditional Chinese Medicine Syndrome, State Key Laboratory of Dampness Syndrome of Chinese Medicine, Guangzhou, Guangdong 510120, China.
Genes Dis. 2024 Apr 25;12(3):101313. doi: 10.1016/j.gendis.2024.101313. eCollection 2025 May.
Enhancer of zeste homolog 2 (EZH2), an epigenetic regulator that primarily inhibits downstream gene expression by tri-methylating histone H3, which is usually overexpressed in tumors and participates in many processes such as tumor occurrence and development, invasion, migration, drug resistance, and anti-tumor immunity as an oncogene, making it an important biomarker in cancer therapy. Collectively, several transcription factors and RNAs cooperate to facilitate the elevated expression of EZH2 in cancer. Although the significance of blocking EZH2 in cancer for inhibiting cancer progression is widely recognized, the clinical application of EZH2 inhibitors continues to encounter numerous challenges. In this review, drawing upon our comprehensive understanding of the factual underpinnings of EZH2's role in cancer, we aim to clarify the crucial importance of targeting EZH2 in cancer treatment. Furthermore, we summarize the current research landscape surrounding targeted EZH2 inhibitors and offer insights into potential future applications of these inhibitors.
zeste同源物2增强子（EZH2）是一种表观遗传调控因子，主要通过对组蛋白H3进行三甲基化来抑制下游基因表达。它通常在肿瘤中过度表达，并作为一种癌基因参与肿瘤发生发展、侵袭、迁移、耐药及抗肿瘤免疫等许多过程，使其成为癌症治疗中的重要生物标志物。总的来说，几种转录因子和RNA协同作用促进了EZH2在癌症中的高表达。尽管阻断EZH2在癌症中对抑制癌症进展的重要性已得到广泛认可，但EZH2抑制剂的临床应用仍面临诸多挑战。在本综述中，基于我们对EZH2在癌症中作用的事实基础的全面理解，我们旨在阐明在癌症治疗中靶向EZH2的至关重要性。此外，我们总结了目前围绕靶向EZH2抑制剂的研究现状，并对这些抑制剂未来的潜在应用提供见解。
