表观遗传学是一种可遗传且可逆的修饰，其发生独立于原始 DNA 序列的改变，但显着影响基因表达。在癌症进展中经常观察到异常的表观遗传调节因子，不仅影响肿瘤细胞的行为，还影响肿瘤相关的微环境（TME）。越来越多的证据表明它们作为生物标志物来预测临床结果和化疗耐药性的巨大潜力。因此，针对放松管制的表观遗传调节因子将是癌症治疗的一个引人注目的策略。迄今为止，当前的表观遗传药物在癌症的临床前试验和临床治疗中都显示出良好的疗效，这鼓励了从天然化合物或人工合成中开发新型表观遗传抑制剂的研究发现。但获得FDA批准的仅有少数，相关研究还需投入更多精力。本章将更新表观遗传抑制剂在癌症治疗中的应用和最新进展，并为表观遗传药物的未来发展提供展望。版权所有©2024。出版者：Elsevier Inc.

Epigenetics is a heritable and reversible modification that occurs independent of the alteration of primary DNA sequence but remarkably affects genetic expression. Aberrant epigenetic regulators are frequently observed in cancer progression not only influencing the behavior of tumor cells but also the tumor-associated microenvironment (TME). Increasing evidence has shown their great potential as biomarkers to predict clinical outcomes and chemoresistance. Hence, targeting the deregulated epigenetic regulators would be a compelling strategy for cancer treatment. So far, current epigenetic drugs have shown promising efficacy in both preclinical trials and clinical treatment of cancer, which encourages research discoveries on the development of novel epigenetic inhibitors either from natural compounds or artificial synthesis. However, only a few have been approved by the FDA, and more effort needs to be put into the related research. This chapter will update the applications and latest progress of epigenetic inhibitors in cancer treatment and provide prospects for the future development of epigenetic drugs.Copyright © 2024. Published by Elsevier Inc.