Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

表观遗传学 染色质 组蛋白 计算生物学 生物 DNA甲基化 化学空间 后生 癌症表观遗传学 癌症 遗传学 生物信息学 药物发现 DNA 基因表达 基因 组蛋白甲基转移酶
作者
Subhankar Biswas,C. Mallikarjuna Rao
出处
期刊:European Journal of Pharmacology [Elsevier]
卷期号:837: 8-24 被引量:297
标识
DOI:10.1016/j.ejphar.2018.08.021
摘要

Addition of chemical tags on the DNA and modification of histone proteins impart a distinct feature on chromatin architecture. With the advancement in scientific research, the key players underlying these changes have been identified as epigenetic modifiers of the chromatin. Indeed, the plethora of enzymes catalyzing these modifications, portray the diversity of epigenetic space and the intricacy in regulating gene expression. These epigenetic players are categorized as writers: that introduce various chemical modifications on DNA and histones, readers: the specialized domain containing proteins that identify and interpret those modifications and erasers: the dedicated group of enzymes proficient in removing these chemical tags. Research over the past few decades has established that these epigenetic tools are associated with numerous disease conditions especially cancer. Besides, with the involvement of epigenetics in cancer, these enzymes and protein domains provide new targets for cancer drug development. This is certain from the volume of epigenetic research conducted in universities and R&D sector of pharmaceutical industry. Here we have highlighted the different types of epigenetic enzymes and protein domains with an emphasis on methylation and acetylation. This review also deals with the recent developments in small molecule inhibitors as potential anti-cancer drugs targeting the epigenetic space.
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