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靶向组蛋白去甲基化酶作为一种潜在的癌症治疗方法(综述)。

Targeting histone demethylases as a potential cancer therapy (Review).

机构信息

Department of Gastrointestinal Surgery, Department of General Surgery, Guangdong Provincial People's Hospital, Guangdong Academy of Medical Sciences, Guangzhou, Guangdong 510080, P.R. China.

Research Center of Medical Sciences, Guangdong Provincial People's Hospital, Guangdong Academy of Medical Sciences, Guangzhou, Guangdong 510080, P.R. China.

出版信息

Int J Oncol. 2022 Sep;61(3). doi: 10.3892/ijo.2022.5393. Epub 2022 Jul 8.

Abstract

Post‑translational modifications of histones by histone demethylases have an important role in the regulation of gene transcription and are implicated in cancers. Recently, the family of lysine (K)‑specific demethylase (KDM) proteins, referring to histone demethylases that dynamically regulate histone methylation, were indicated to be involved in various pathways related to cancer development. To date, numerous studies have been conducted to explore the effects of KDMs on cancer growth, metastasis and drug resistance, and a majority of KDMs have been indicated to be oncogenes in both leukemia and solid tumors. In addition, certain KDM inhibitors have been developed and have become the subject of clinical trials to explore their safety and efficacy in cancer therapy. However, most of them focus on hematopoietic malignancy. This review summarizes the effects of KDMs on tumor growth, drug resistance and the current status of KDM inhibitors in clinical trials.

摘要

组蛋白去甲基化酶对组蛋白的翻译后修饰在基因转录调控中起重要作用,并与癌症有关。最近,赖氨酸(K)特异性去甲基酶(KDM)蛋白家族,指的是动态调节组蛋白甲基化的组蛋白去甲基酶,被认为参与了与癌症发展相关的各种途径。迄今为止,已经进行了大量研究来探讨 KDM 对癌症生长、转移和耐药性的影响,大多数 KDM 在白血病和实体瘤中均被认为是癌基因。此外,已经开发了某些 KDM 抑制剂,并已成为临床试验的主题,以探索它们在癌症治疗中的安全性和有效性。然而,它们大多数都集中在血液恶性肿瘤上。本综述总结了 KDM 对肿瘤生长、耐药性的影响以及 KDM 抑制剂在临床试验中的现状。

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