College of Marine Science, Shandong University, Weihai 264209, China.
Curr Drug Targets. 2020;21(11):1068-1083. doi: 10.2174/1389450121666200325093104.
Epigenetic modifications ensure the maintenance of normal cellular functions, and their dysregulation is frequently found in many disease states, including cancer. Nowadays, the most studied epigenetic dysregulation associated with tumorigenesis, cancer progression and metastasis refers to the variations in DNA methylation, histone modification and chromatin structure. The development of novel agents targeting these processes has enabled us to open up new pathways for anti-cancer strategies. To date, many small molecules have been designed to target epigenetic modifiers, and some of them are currently in clinical trials for patients with haematologic malignancies and solid tumours. With this in mind, we elaborate on basic information on epigenetic modifications and potential epigenetic therapies for cancer treatment.
表观遗传修饰可确保正常细胞功能的维持，其失调在许多疾病状态中经常出现，包括癌症。如今，与肿瘤发生、癌症进展和转移最相关的研究最多的表观遗传失调是指 DNA 甲基化、组蛋白修饰和染色质结构的变化。针对这些过程的新型药物的开发使我们能够为抗癌策略开辟新途径。迄今为止，已经设计了许多小分子来靶向表观遗传修饰物，其中一些目前正在针对血液恶性肿瘤和实体瘤患者进行临床试验。有鉴于此，我们详细阐述了有关癌症治疗的表观遗传修饰和潜在表观遗传疗法的基本知识。
