摘要DNA甲基转移酶(DNMT)在多种肿瘤细胞中呈表达上调,异常表达的DNMT通过催化肿瘤抑制基因启动子区域CpG岛甲基化,引起抑癌基因甲基化失活,从而促进正常细胞向肿瘤细胞转化.研究表明,DNMT在消化道肿瘤、乳腺癌、肺癌等肿瘤细胞中呈表达丰度异常,且与肿瘤的发生呈明显相关性,并影响肿瘤预后.药物及靶向干扰可抑制DNMT的活性,可使甲基化的基因去甲基化复活,进而抑制肿瘤细胞生长,促进细胞凋亡.

abstractsOverexpression of DNA methyltransferases(DNMTs)is observed in many tumors. Overexpressed DNMTs silence tumor suppressor genes by catalyzing the methylation of CpG islands within the promoter regions, and therefore promote the neoplastic transformation of normal cells. Highly elevated DNMT activities have been observed in cancers including gastrointestinal cancers, breast cancer, and lung cancer and have been associated with cancer development and prognosis. Drugs and targeted therapies that inhibit DNMT activities can reactivate methylated tumor suppressor genes, promote apoptosis, and thus inhibit tumor growth.