DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge.
DNA Methylation Targeting: The DNMT/HMT Crosstalk Challenge.
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DOI：
10.3390/biom7010003
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发表时间：
2017-01-05
期刊：
影响因子：
5.5
通讯作者：
Goossens L
中科院分区：
文献类型：
--
作者：
Castillo-Aguilera O;Depreux P;Halby L;Arimondo PB;Goossens L
染色质可以采取与基因转录相关的解凝聚状态（常染色质）和与转录抑制相关的凝聚状态（异染色质）。这些状态由表观遗传调节剂控制，表观遗传调节剂在DNA或组蛋白上是活跃的，并且彼此紧密相关。DNA和组蛋白的甲基化参与基因的激活或沉默及其串扰。由于DNA/组蛋白甲基化模式在癌症中改变，靶向这些修饰的分子是有趣的治疗工具。我们在此提出了一个巨大的面板的DNA甲基转移酶抑制剂分类，根据其机制，以及选定的组蛋白甲基转移酶抑制剂共享一个共同的作用模式。
Chromatin can adopt a decondensed state linked to gene transcription (euchromatin) and a condensed state linked to transcriptional repression (heterochromatin). These states are controlled by epigenetic modulators that are active on either the DNA or the histones and are tightly associated to each other. Methylation of both DNA and histones is involved in either the activation or silencing of genes and their crosstalk. Since DNA/histone methylation patterns are altered in cancers, molecules that target these modifications are interesting therapeutic tools. We present herein a vast panel of DNA methyltransferase inhibitors classified according to their mechanism, as well as selected histone methyltransferase inhibitors sharing a common mode of action.