文章：

靶向抑制组蛋白赖氨酸去甲基化酶作为新型抗癌治疗策略的研究进展——近期证据更新

The Targeted Inhibition of Histone Lysine Demethylases as a Novel Promising Anti-Cancer Therapeutic Strategy—An Update on Recent Evidence

原文发布日期：27 August 2025

DOI: 10.3390/cancers17172798

类型: Article

开放获取: 是

英文摘要：

A growing body of evidence confirms that non-mutational epigenetic reprogramming constitutes an important hallmark of cancer, contributing to the heterogeneity and phenotypic plasticity observed in cancers. Among the many epigenetic modulators, histone lysine demethylases (KDMs) have emerged as promising targets for pharmacological inhibition in cancer treatment. KDMs were found to be frequently overexpressed and/or hyperactivated in cancer cells, and their inhibition was shown to result in the inhibition of cancer cell growth both in vitro and in vivo. The inhibition of Lysine-specific histone demethylase 1A (LSD1), KDM3, KDM4, KDM5, and KDM6 may affect cell survival, proliferation, motility, and apoptosis induction. Importantly, KDM inhibitors can be used as modulators of anti-cancer immune response and sensitivity to radiation and chemotherapy. This narrative review aims to present the most recent evidence documenting the anti-cancer potential of KDM inhibitors.

摘要翻译： 

越来越多的证据证实，非突变性表观遗传重编程是癌症的重要特征之一，这导致了癌症中观察到的异质性和表型可塑性。在众多表观遗传调节因子中，组蛋白赖氨酸去甲基化酶（KDMs）已成为癌症治疗中药物抑制的潜在靶点。研究发现，KDMs在癌细胞中常常过度表达和/或过度激活，而抑制这些酶在体外和体内均能抑制癌细胞的生长。抑制赖氨酸特异性组蛋白去甲基化酶1A（LSD1）、KDM3、KDM4、KDM5和KDM6可能影响细胞的存活、增殖、运动及凋亡诱导。重要的是，KDM抑制剂可作为抗癌免疫反应以及对放疗和化疗敏感性的调节剂。本文旨在综述记录KDM抑制剂抗癌潜力的最新证据。

原文链接：

The Targeted Inhibition of Histone Lysine Demethylases as a Novel Promising Anti-Cancer Therapeutic Strategy—An Update on Recent Evidence