癌症被认为是一种表观遗传疾病。表观遗传异常改变导致参与细胞正常生长的关键基因失活，促进癌症发生和发展，这使得对癌症治疗上可采取一些主动性表观遗传调节。DNA去甲基化药物通过化学逆转重新激活高甲基化的肿瘤抑制基因，已成为一个令人兴奋的癌症治疗方法。其作用机制主要有：抑制DNA甲基转移酶，干扰甲基转移反应途径和影响三羧酸循环途径。介绍了近年来DNA去甲基化药物作用机制的研究进展。

Cancer was regarded as an epigenetic disease in recent years. Aberrant epigenetic changes which lead to inactivation of pivotal genes were involved in correct cell growth, contributing to cancer development and progression, which had resulted in several initiatives implementing epigenetics in cancer treatment. DNA demethylating agents reactivating hypermethylated tumor suppressor genes, which caused chemical reversal of them, had become an exciting approach for cancer treatment. Three aspects of action mechanism mainly include:the inhibition of DNA methyltransferase, interference of the methyl transfer reaction pathway, and the influence of the tricarboxylic acid cycle. In this review, recent advances in the research of DNA demethylating agents are described according to their mechanism of action.

骨干院校建设重点科研项目（XJ1305）；福建省中青年教师教育科研项目（JAT160852）；泉州市科技计划项目（2013Z52）