Department of Oncology, People's Hospital, Henan Province, Zhengzhou, China.
Curr Cancer Drug Targets. 2010 Aug;10(5):539-45. doi: 10.2174/156800910791517217.
DNA methylation and histone acetylation are two most studied epigenetic markers. Aberrant methylation of gene promoter regions and histone tail lysine residue modification through acetylation and methylation play a key role in malignant disorders. Two DNA methyltransferase inhibitors, azacitidine and decitabine, have been licensed for clinical therapy for patients with myelodysplastic syndrome. New hypomethylating agents, zebularine and isothiocyanates, are in various stages of development for cancer therapy. In this review we summarize recent clinical developments on novel hypomethylating agents and new regimens from clinical trials for epigenetic therapy of cancer.
DNA 甲基化和组蛋白乙酰化是两种研究最多的表观遗传标记物。通过乙酰化和甲基化修饰基因启动子区域的异常甲基化和组蛋白尾部赖氨酸残基修饰在恶性疾病中起着关键作用。两种 DNA 甲基转移酶抑制剂，阿扎胞苷和地西他滨，已被批准用于治疗骨髓增生异常综合征患者的临床治疗。新型低甲基化剂，佐布利津和异硫氰酸盐，处于癌症治疗的各个开发阶段。在这篇综述中，我们总结了癌症表观遗传治疗的新型低甲基化剂和临床试验中新方案的最新临床进展。
