Epigenetic changes associated with histone modifications play an important role in the emergence and maintenance of the phenotype of various cancer types. In contrast to direct mutations in the main DNA sequence, these changes are reversible, which makes the development of inhibitors of enzymes of post-translational histone modifications one of the most promising strategies for the creation of anticancer drugs. To date, a wide variety of histone modifications have been found that play an important role in the regulation of chromatin state, gene expression, and other nuclear events. This review examines the main features of the most common and studied epigenetic histone modifications with a proven role in the pathogenesis of a wide range of malignant neoplasms: acetylation / deacetylation and methylation / demethylation of histone proteins, as well as the role of enzymes of the HAT / HDAC and HMT / HDMT families in the development of oncological pathologies. The data on the relationship between histone modifications and certain types of cancer are presented and discussed. Special attention is devoted to the consideration of various strategies for the development of epigenetic inhibitors. The main directions of the development of inhibitors of histone modifications are analyzed and effective strategies for their creation are identified and discussed. The most promising strategy is the use of multitarget drugs, which will affect multiple molecular targets of cancer. A critical analysis of the current status of approved epigenetic anticancer drugs has also been performed.

与组蛋白修饰相关的表观遗传变化在各种癌症类型的表型的出现和维持中起重要作用。与主要 DNA 序列中的直接突变相比，这些变化是可逆的，这使得开发翻译后组蛋白修饰酶抑制剂成为创造抗癌药物的最有希望的策略之一。迄今为止，已发现多种组蛋白修饰在染色质状态、基因表达和其他核事件的调节中发挥重要作用。这篇综述检查了最常见和研究的表观遗传组蛋白修饰的主要特征，这些修饰在多种恶性肿瘤的发病机制中已被证实：组蛋白的乙酰化/去乙酰化和甲基化/去甲基化，以及 HAT / HDAC 和 HMT / HDMT 家族的酶在肿瘤病理学发展中的作用。介绍并讨论了有关组蛋白修饰与某些类型癌症之间关系的数据。特别注意考虑开发表观遗传抑制剂的各种策略。分析了组蛋白修饰抑制剂开发的主要方向，并确定并讨论了其产生的有效策略。最有希望的策略是使用多靶点药物，这将影响癌症的多个分子靶点。还对已批准的表观遗传抗癌药物的现状进行了批判性分析。介绍并讨论了有关组蛋白修饰与某些类型癌症之间关系的数据。特别注意考虑开发表观遗传抑制剂的各种策略。分析了组蛋白修饰抑制剂开发的主要方向，并确定并讨论了其产生的有效策略。最有希望的策略是使用多靶点药物，这将影响癌症的多个分子靶点。还对已批准的表观遗传抗癌药物的现状进行了批判性分析。介绍并讨论了有关组蛋白修饰与某些类型癌症之间关系的数据。特别注意考虑开发表观遗传抑制剂的各种策略。分析了组蛋白修饰抑制剂开发的主要方向，并确定并讨论了其产生的有效策略。最有希望的策略是使用多靶点药物，这将影响癌症的多个分子靶点。还对已批准的表观遗传抗癌药物的现状进行了批判性分析。分析了组蛋白修饰抑制剂开发的主要方向，并确定并讨论了其产生的有效策略。最有希望的策略是使用多靶点药物，这将影响癌症的多个分子靶点。还对已批准的表观遗传抗癌药物的现状进行了批判性分析。分析了组蛋白修饰抑制剂开发的主要方向，并确定并讨论了其产生的有效策略。最有希望的策略是使用多靶点药物，这将影响癌症的多个分子靶点。还对已批准的表观遗传抗癌药物的现状进行了批判性分析。