Division of Hematology & Oncology, Department of Medicine, University of Florida Health Cancer Center, University of Florida, Gainesville, Florida 32606, USA; email:
Annu Rev Pharmacol Toxicol. 2018 Jan 6;58:187-207. doi: 10.1146/annurev-pharmtox-010716-105106. Epub 2017 Oct 6.
Alterations of genes regulating epigenetic processes are frequently found as cancer drivers and may cause widespread alterations of DNA methylation, histone modification patterns, or chromatin structure that disrupt normal patterns of gene expression. Because of the inherent reversibility of epigenetic changes, inhibitors targeting these processes are promising anticancer strategies. Small molecules targeting epigenetic regulators have been developed recently, and clinical trials of these agents are under way for hematologic malignancies and solid tumors. In this review, we describe how the writers, readers, and erasers of epigenetic marks are dysregulated in cancer and summarize the development of therapies targeting these mechanisms.
基因调控表观遗传过程的改变通常被发现是癌症的驱动因素，可能导致 DNA 甲基化、组蛋白修饰模式或染色质结构的广泛改变，从而破坏正常的基因表达模式。由于表观遗传变化具有固有的可逆性，针对这些过程的抑制剂是很有前途的抗癌策略。最近已经开发出针对表观遗传调节剂的小分子，并且针对血液恶性肿瘤和实体瘤的这些药物的临床试验正在进行中。在这篇综述中，我们描述了表观遗传标记的写入器、读取器和擦除器在癌症中是如何失调的，并总结了针对这些机制的治疗方法的发展。
