PDF(Pubmed)
Abstract：
Histone methylation plays a crucial role in tumorigenesis. Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase that regulates chromatin structure and gene expression. EZH2 inhibitors (EZH2is) have been shown to be effective in treating hematologic malignancies, while their effectiveness in solid tumors remains limited. One of the major challenges in the treatment of solid tumors is their hypoxic tumor microenvironment. Hypoxia-inducible factor 1-alpha (HIF-1α) is a key hypoxia responder that interacts with EZH2 to promote tumor progression. Here we discuss the implications of the relationship between EZH2 and hypoxia for expanding the application of EZH2is in solid tumors.
摘要：
组蛋白甲基化在肿瘤发生中起着至关重要的作用。zeste同源物2（EZH2）的增强子是调节染色质结构和基因表达的组蛋白甲基转移酶。EZH2抑制剂（EZH2is）已被证明可有效治疗血液系统恶性肿瘤，而它们在实体瘤中的有效性仍然有限。实体肿瘤治疗的主要挑战之一是它们的低氧肿瘤微环境。缺氧诱导因子1-α（HIF-1α）是与EZH2相互作用以促进肿瘤进展的关键缺氧反应者。在这里，我们讨论了EZH2与缺氧之间的关系对扩大EZH2is在实体瘤中的应用的意义。
