Design of small molecule epigenetic modulators.

Design of small molecule epigenetic modulators.
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DOI:
10.1016/j.bmcl.2013.11.001
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发表时间:
2014-01-01
影响因子:
2.7
通讯作者:
Woster, Patrick M.
Woster, Patrick M.
中科院分区:
医学4区
文献类型:
--
作者:
Pachaiyappan, Boobalan;Woster, Patrick M.

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表观遗传学领域已经迅速扩大,揭示了药物发现的多个新靶点。表观基因组机制的功能元件可分为书写器、擦除器和读取器,这些元件共同控制细胞基因表达和稳态。越来越清楚的是,表观基因组的畸变可能是多种疾病的基础,因此发现以特定方式调节表观基因组的小分子是发现新治疗剂的可行方法。在这篇摘要中,将简要概述表观遗传控制基因表达的组成部分,并将描述识别调节表观遗传过程的小分子的努力。
The field of epigenetics has expanded rapidly to reveal multiple new targets for drug discovery. The functional elements of the epigenomic machinery can be catagorized as writers, erasers and readers, and together these elements control cellular gene expression and homeostasis. It is increasingly clear that aberrations in the epigenome can underly a variety of diseases, and thus discovery of small molecules that modulate the epigenome in a specific manner is a viable approach to the discovery of new therapeutic agents. In this Digest, the components of epigenetic control of gene expression will be briefly summarized, and efforts to identify small molecules that modulate epigenetic processes will be described.
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