Frontiers in Pharmacology (Dec 2022)

Recent progress in DNA methyltransferase inhibitors as anticancer agents

  • Zhixiong Zhang,
  • Zhixiong Zhang,
  • Guan Wang,
  • Yuyan Li,
  • Yuyan Li,
  • Dongsheng Lei,
  • Jin Xiang,
  • Liang Ouyang,
  • Liang Ouyang,
  • Yanyan Wang,
  • Yanyan Wang,
  • Jinliang Yang

DOI
https://doi.org/10.3389/fphar.2022.1072651
Journal volume & issue
Vol. 13

Abstract

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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.

Keywords