Zhang Zhixiong, Wang Guan, Li Yuyan, Lei Dongsheng, Xiang Jin, Ouyang Liang, Wang Yanyan, Yang Jinliang
State Key Laboratory of Biotherapy and Cancer Center, National Clinical Research Center for Geriatrics, Innovation Center of Nursing Research, West China Hospital, and Collaborative Innovation Center of Biotherapy, Sichuan University, Chengdu, China.
Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, China.
Front Pharmacol. 2022 Dec 16;13:1072651. doi: 10.3389/fphar.2022.1072651. eCollection 2022.
DNA methylation mediated by DNA methyltransferase is an important epigenetic process that regulates gene expression in mammals, which plays a key role in silencing certain genes, such as tumor suppressor genes, in cancer, and it has become a promising therapeutic target for cancer treatment. Similar to other epigenetic targets, DNA methyltransferase can also be modulated by chemical agents. Four agents have already been approved to treat hematological cancers. In order to promote the development of a DNA methyltransferase inhibitor as an anti-tumor agent, in the current review, we discuss the relationship between DNA methylation and tumor, the anti-tumor mechanism, the research progress and pharmacological properties of DNA methyltransferase inhibitors, and the future research trend of DNA methyltransferase inhibitors.
由DNA甲基转移酶介导的DNA甲基化是一种重要的表观遗传过程，可调节哺乳动物的基因表达，在癌症中使某些基因（如肿瘤抑制基因）沉默方面发挥关键作用，并且它已成为癌症治疗中一个有前景的治疗靶点。与其他表观遗传靶点类似，DNA甲基转移酶也可被化学试剂调节。已有四种试剂被批准用于治疗血液系统癌症。为了推动DNA甲基转移酶抑制剂作为抗肿瘤药物的发展，在当前综述中，我们讨论了DNA甲基化与肿瘤之间的关系、抗肿瘤机制、DNA甲基转移酶抑制剂的研究进展和药理学特性，以及DNA甲基转移酶抑制剂的未来研究趋势。
