EZH1/2作为癌症治疗的靶点
EZH1/2 as targets for cancer therapy
原文发布日期:2022-11-11
英文摘要:
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The enhancer of zeste homolog 2 (EZH2) and its highly related homolog EZH1 are considered to be epigenetic silencing factors, and they play key roles in the growth and differentiation of cells as the core components of polycomb repressive complex 2 (PRC2). EZH1 and EZH2 are known to have a role in human malignancies, and alterations in these two genes have been implicated in transformation of human malignancies. Inhibition of EZH1/2 has been shown to result in tumor regression in humans and has been studied and evaluated in the preclinical setting and in multiple clinical trials at various levels. Our work thus contributes to the understanding of the relationship between regulatory molecules associated with EZH1/2 proteins and tumor progression, and may provide new insights for mechanism-based EZH1/2-targeted therapy in tumors.
zeste同源基因增强子2(EZH2)及其高度同源物EZH1被视为表观遗传沉默因子,作为多梳抑制复合体2(PRC2)的核心组成部分,在细胞生长与分化中起关键作用。已知EZH1和EZH2在人类恶性肿瘤中发挥作用,这两种基因的改变与恶性肿瘤的转化密切相关。研究表明,抑制EZH1/2可导致人体内肿瘤消退,这一效应已在临床前环境及多个不同阶段的临床试验中得到验证与评估。我们的工作由此深化了对EZH1/2相关调控分子与肿瘤进展关系的理解,或可为基于机制的EZH1/2靶向肿瘤治疗提供新见解。
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