Liu Pengcheng, Yang Fan, Zhang Lizhi, Hu Ying, Chen Bangjie, Wang Jianpeng, Su Lei, Wu Mingyue, Chen Wenjian
Department of Human Resources, The First Affiliated Hospital of Anhui Medical University, Hefei, China.
The First Clinical Medical College, Anhui Medical University, Hefei, China.
Front Pharmacol. 2022 Aug 25;13:958146. doi: 10.3389/fphar.2022.958146. eCollection 2022.
DNA methylation is one of the most essential epigenetic mechanisms to regulate gene expression. DNA methyltransferases (DNMTs) play a vital role in DNA methylation in the genome. In mammals, DNMTs act with some elements to regulate the dynamic DNA methylation patterns of embryonic and adult cells. Conversely, the aberrant function of DNMTs is frequently the hallmark in judging cancer, including total hypomethylation and partial hypermethylation of tumor suppressor genes (TSGs), which improve the malignancy of tumors, aggravate the ailment for patients, and significantly exacerbate the difficulty of cancer therapy. Since DNA methylation is reversible, currently, DNMTs are viewed as an important epigenetic target for drug development. However, the impression of DNMTs on cancers is still controversial, and therapeutic methods targeting DNMTs remain under exploration. This review mainly summarizes the relationship between the main DNMTs and cancers as well as regulatory mechanisms and clinical applications of DNMTs in cancer and highlights several forthcoming strategies for targeting DNMTs.
DNA甲基化是调控基因表达的最重要的表观遗传机制之一。DNA甲基转移酶（DNMTs）在基因组DNA甲基化过程中发挥着至关重要的作用。在哺乳动物中，DNMTs与一些元件共同作用，调控胚胎细胞和成年细胞动态的DNA甲基化模式。相反，DNMTs的异常功能常常是判断癌症的标志，包括肿瘤抑制基因（TSGs）的整体低甲基化和部分高甲基化，这会提高肿瘤的恶性程度，加重患者病情，并显著增加癌症治疗的难度。由于DNA甲基化是可逆的，目前，DNMTs被视为药物研发的重要表观遗传靶点。然而，DNMTs对癌症的影响仍存在争议，针对DNMTs的治疗方法仍在探索中。本综述主要总结了主要DNMTs与癌症之间的关系以及DNMTs在癌症中的调控机制和临床应用，并重点介绍了几种即将出现的靶向DNMTs的策略。
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