Emerging epigenetic targets and therapies in cancer medicine.
Emerging epigenetic targets and therapies in cancer medicine.
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DOI：
10.1158/2159-8290.cd-12-0076
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发表时间：
2012-05
期刊：
影响因子：
28.2
通讯作者：
Licht JD
中科院分区：
文献类型：
--
作者：
Popovic R;Licht JD
染色质结构和功能的表观遗传调控异常可导致基因表达异常和癌症发展。因此，表观遗传疗法旨在通过抑制表观遗传机制的各种组分来恢复正常的染色质修饰模式。组蛋白去乙酰化酶和DNA甲基转移酶抑制剂代表了第一种推定的表观遗传疗法，然而这些药物具有多效性作用，并且仍然不清楚它们如何导致治疗反应。最近，抑制组蛋白甲基转移酶的药物被开发出来，可能代表了更具体的药物。在这里，我们回顾了癌症中新兴的表观遗传靶点，并介绍了最近有希望的表观遗传疗法模型。
Abnormalities in the epigenetic regulation of chromatin structure and function can lead to aberrant gene expression and cancer development. Consequently, epigenetic therapies aim to restore normal chromatin modification patterns through the inhibition of various components of the epigenetic machinery. Histone deacetylase and DNA methyltransferase inhibitors represent the first putative epigenetic therapies, however these agents have pleiotropic effects and it remains unclear how they lead to therapeutic responses. More recently, drugs that inhibit histone methyltransferases were developed, perhaps representing more specific agents. Here we review emerging epigenetic targets in cancer and present recent models of promising epigenetic therapies.