The Wistar Institute, Philadelphia, PA 19104, USA.
Faculty of Science and Engineering/Cell Biology, University of Turku and Åbo Akademi University, Turku 20500, Finland.
Oncol Rep. 2023 Mar;49(3). doi: 10.3892/or.2023.8496. Epub 2023 Feb 17.
Cancer is a global public health concern. Alterations in epigenetic processes are among the earliest genomic aberrations occurring during cancer development and are closely related to progression. Unlike genetic mutations, aberrations in epigenetic processes are reversible, which opens the possibility for novel pharmacological treatments. Non‑coding RNAs (ncRNAs) represent an essential epigenetic mechanism, and emerging evidence links ncRNAs to carcinogenesis. Epigenetic drugs (epidrugs) are a group of promising target therapies for cancer treatment acting as coadjuvants to reverse drug resistance in cancer. The present review describes central epigenetic aberrations during malignant transformation and explains how epidrugs target DNA methylation, histone modifications and ncRNAs. Furthermore, clinical trials focused on evaluating the effect of these epidrugs alone or in combination with other anticancer therapies and other ncRNA‑based therapies are discussed. The use of epidrugs promises to be an effective tool for reversing drug resistance in some patients with cancer.
癌症是一个全球性的公共卫生关注点。表观遗传过程的改变是癌症发生过程中最早出现的基因组异常之一，与癌症的进展密切相关。与遗传突变不同，表观遗传过程的改变是可逆的，这为新型药物治疗开辟了可能性。非编码 RNA（ncRNA）代表了一种重要的表观遗传机制，越来越多的证据将 ncRNA 与致癌作用联系起来。表观遗传药物（epidrugs）是一组有前途的癌症治疗靶向治疗药物，可作为辅助药物逆转癌症的耐药性。本综述描述了恶性转化过程中的主要表观遗传异常，并解释了 epidrugs 如何靶向 DNA 甲基化、组蛋白修饰和 ncRNA。此外，还讨论了专注于评估这些 epidrugs 单独或与其他抗癌疗法和其他基于 ncRNA 的疗法联合使用的临床试验。使用 epidrugs 有望成为某些癌症患者逆转耐药性的有效工具。
