DNA甲基化是調(diào)節(jié)基因表達(dá)而不改變DNA堿基序列的表觀遺傳修飾，通過沉默腫瘤抑制基因在癌癥發(fā)展中發(fā)揮關(guān)鍵作用。DNA去甲基化藥物在臨床上已經(jīng)顯示出療效，然而，高效性和特異性的DNA去甲基化藥物尚未出現(xiàn)。目前，在市場上已有2種藥物阿扎胞苷和地西他濱用于治療骨髓增生異常綜合征。尋找直接結(jié)合靶點新的抑制劑是未來的方向。從抗腫瘤活性和臨床研究方面介紹了DNA去甲基化藥物的研究進(jìn)展。

DNA methylation is an epigenetic modification that modulates gene expression without altering the DNA base sequence, which plays a crucial role in cancer by silencing tumor suppressor genes. DNA demethylating agents have shown efficacy in clinics. However, highly efficient and specific DNA demethylating agents have not yet been found. At present, two drugs, azacitidine and decitabine are on the market for the treatment of myelodysplastic syndrome. Improving methods will certainly lead to the prediction of novel directly binding inhibitors in the future. This article reviewed the progress on antitumor activities and clinical studies of DNA demethylating agents.

中國博士后基金資助項目（2016M591399）；福建省中青年教師教育科研項目（JAT160852）；天津市自然科學(xué)基金重點項目（16JCZDJC32600）