Beijing Key Laboratory of Gene Resource and Molecular Development, Beijing Normal University, Beijing, China.
Med Oncol. 2023 May 6;40(6):167. doi: 10.1007/s12032-023-02025-6.
The enhancer of zeste homolog 2 (EZH2) is encoded by the Enhancer of zeste 2 polycomb repressive complex 2 subunit gene. EZH2 is involved in the cell cycle, DNA damage repair, cell differentiation, autophagy, apoptosis, and immunological modulation. The main function of EZH2 is to catalyze the methylation of H3 histone of H3K27Me3, which inhibits the transcription of target genes, such as tumor suppressor genes. EZH2 also forms complexes with transcriptions factors or directly binds to the promoters of target genes, leading to regulate gene transcriptions. EZH2 has been as a prominent target for cancer therapy and a growing number of potential targeting medicines have been developed. This review summarized the mechanisms that EZH2 regulates gene transcription and the interactions between EZH2 and important intracellular signaling molecules (Wnt, Notch, MEK, Akt) and as well the clinical applications of EZH2-targeted drugs.
EZH2 是由 Enhancer of zeste 2 polycomb repressive complex 2 亚基基因编码的。EZH2 参与细胞周期、DNA 损伤修复、细胞分化、自噬、凋亡和免疫调节。EZH2 的主要功能是催化 H3 组蛋白 H3K27Me3 的甲基化，从而抑制靶基因的转录，如肿瘤抑制基因。EZH2 还与转录因子形成复合物或直接结合到靶基因的启动子上，从而调节基因转录。EZH2 已成为癌症治疗的一个突出靶点，越来越多的潜在靶向药物已经被开发出来。本文综述了 EZH2 调节基因转录的机制，以及 EZH2 与重要的细胞内信号分子（Wnt、Notch、MEK、Akt）之间的相互作用，以及 EZH2 靶向药物的临床应用。
