Histone deacetylases
Histone deacetylases
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DOI：
10.1016/s1471-4892(03)00084-5
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发表时间：
2003-08-01
影响因子：
4
通讯作者：
Richon, VM
中科院分区：
文献类型：
--
作者：
Marks, PA;Miller, T;Richon, VM
染色质历史的翻译后修饰在调节基因表达中具有重要作用。参与这些表观遗传事件的酶包括组蛋白脱乙酰酶（I类和II类），其可以被结构多样的小分子组抑制。这些组蛋白脱乙酰酶抑制剂在体外和体内诱导癌细胞的生长停滞、分化和/或凋亡。这些药物中的几种的临床试验结果表明，它们在具有抗肿瘤活性的剂量下耐受良好。
Post-translational modification of the histories of chromatin has a fundamental role in regulating gene expression. Enzymes involved in these epigenetic events include histone deacetylases (class I and class II), which can be inhibited by a structurally diverse group of small molecules. These histone deacetylase inhibitors induce growth arrest, differentiation and/or apoptosis of cancer cells in vitro and in vivo. Results of clinical trials with several of these agents have indicated that they are well tolerated at doses that have anti-tumour activity.