癌癥被認為是一種表觀遺傳疾病。表觀遺傳異常改變導(dǎo)致參與細胞正常生長的關(guān)鍵基因失活，促進癌癥發(fā)生和發(fā)展，這使得對癌癥治療上可采取一些主動性表觀遺傳調(diào)節(jié)。DNA去甲基化藥物通過化學(xué)逆轉(zhuǎn)重新激活高甲基化的腫瘤抑制基因，已成為一個令人興奮的癌癥治療方法。其作用機制主要有：抑制DNA甲基轉(zhuǎn)移酶，干擾甲基轉(zhuǎn)移反應(yīng)途徑和影響三羧酸循環(huán)途徑。介紹了近年來DNA去甲基化藥物作用機制的研究進展。

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.

骨干院校建設(shè)重點科研項目（XJ1305）；福建省中青年教師教育科研項目（JAT160852）；泉州市科技計劃項目（2013Z52）