Jin Ning, George Tiffany L, Otterson Gregory A, Verschraegen Claire, Wen Haitao, Carbone David, Herman James, Bertino Erin M, He Kai
The Ohio State University Comprehensive Cancer Center - Arthur G. James Cancer Hospital and Richard J. Solove Research Institute, Columbus, OH, USA.
Department of Microbial Infection and Immunity, The Ohio State University, Columbus, OH, USA.
Clin Epigenetics. 2021 Apr 20;13(1):83. doi: 10.1186/s13148-021-01069-7.
Epigenetic ("above genetics") modifications can alter the gene expression without altering the DNA sequence. Aberrant epigenetic regulations in cancer include DNA methylation, histone methylation, histone acetylation, non-coding RNA, and mRNA methylation. Epigenetic-targeted agents have demonstrated clinical activities in hematological malignancies and therapeutic potential in solid tumors. In this review, we describe mechanisms of various epigenetic modifications, discuss the Food and Drug Administration-approved epigenetic agents, and focus on the current clinical investigations of novel epigenetic monotherapies and combination therapies in solid tumors.
表观遗传（“遗传学之上”）修饰可在不改变DNA序列的情况下改变基因表达。癌症中异常的表观遗传调控包括DNA甲基化、组蛋白甲基化、组蛋白乙酰化、非编码RNA和mRNA甲基化。表观遗传靶向药物已在血液系统恶性肿瘤中展现出临床活性，并在实体瘤中具有治疗潜力。在本综述中，我们描述了各种表观遗传修饰的机制，讨论了美国食品药品监督管理局批准的表观遗传药物，并重点关注实体瘤中新型表观遗传单药疗法和联合疗法的当前临床研究。
