表观遗传相关药物对癌症的治疗

Epigenetic Related Drugs in Cancer Therapy

表观遗传变化是指核酸序列不发生变化的情况下发生的可遗传变化。表观遗传变化在癌症发生和恶性转移的过程中发挥着重要的作用。目前,已有数种表观药物通过FDA认证并用于癌症的治疗,主要为DNA甲基转移酶抑制剂和组蛋白去乙酰化酶抑制剂;还有许多的新型表观药物处于实验室或者临床试验阶段,包括组蛋白乙酰化酶、组蛋白甲基化酶、组蛋白去甲基化酶以及表观解读蛋白的小分子抑制剂,它们都表现出显著的抗肿瘤活性。该文对这些表观修饰小分子抑制剂的最新进展和将来的应用前景进行了整理、总结。

Epigenetic changes refers to heritable changes without DNA sequence alteration. Epigenetic changes play important roles in carcinogenesis, and FDA has approved several epigenetics-related drugs for cancertherapy, mostly inhibitors of DNMT and HDAC. Moreover, a large number of epigenetic drugs are current under clinical studies for cancer therapy, including inhibitors of HATs, HMTs, HDMTs and epigenetic readers, which all have shown strong antitumor activity. This review will summarize the latest advance and future applications of these inhibitors.