表观遗传药物在疾病中的应用综述。

Genetics and Epigenetics Pub Date : 2014-05-27 eCollection Date: 2014-01-01 DOI:10.4137/GEG.S12270
Sarah Heerboth, Karolina Lapinska, Nicole Snyder, Meghan Leary, Sarah Rollinson, Sibaji Sarkar
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引用次数: 246

摘要

表观遗传变化,如DNA甲基化、组蛋白甲基化和乙酰化,通过上调、下调或完全沉默基因,在转录水平上改变基因表达。表观遗传事件的失调可能是病理性的,导致心血管疾病、神经系统疾病、代谢疾病和癌症的发展。因此,确定抑制这些表观遗传变化的药物具有重要的临床意义。在这篇综述中,我们总结了与不同疾病和疾病相关的表观遗传事件,包括心血管疾病、神经系统疾病、代谢疾病和癌症。了解与这些类型的疾病相关的特定表观遗传变化有助于开发特异性抑制剂,这些抑制剂可以用作表观遗传药物。在这篇综述中,我们讨论了目前使用的主要类型的表观遗传药物,如DNA甲基化抑制药物、溴结构域抑制剂、组蛋白乙酰转移酶抑制剂、组蛋白去乙酰化酶抑制剂、蛋白质甲基转移酶抑制剂和组蛋白甲基化抑制剂,以及它们在逆转表观遗传变化和治疗疾病中的作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Use of epigenetic drugs in disease: an overview.

Use of epigenetic drugs in disease: an overview.

Use of epigenetic drugs in disease: an overview.

Use of epigenetic drugs in disease: an overview.

Epigenetic changes such as DNA methylation and histone methylation and acetylation alter gene expression at the level of transcription by upregulating, downregulating, or silencing genes completely. Dysregulation of epigenetic events can be pathological, leading to cardiovascular disease, neurological disorders, metabolic disorders, and cancer development. Therefore, identifying drugs that inhibit these epigenetic changes are of great clinical interest. In this review, we summarize the epigenetic events associated with different disorders and diseases including cardiovascular, neurological, and metabolic disorders, and cancer. Knowledge of the specific epigenetic changes associated with these types of diseases facilitates the development of specific inhibitors, which can be used as epigenetic drugs. In this review, we discuss the major classes of epigenetic drugs currently in use, such as DNA methylation inhibiting drugs, bromodomain inhibitors, histone acetyl transferase inhibitors, histone deacetylase inhibitors, protein methyltransferase inhibitors, and histone methylation inhibitors and their role in reversing epigenetic changes and treating disease.

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