组蛋白去乙酰化酶抑制剂:最新进展、趋势和前景。

Oscar Moradei, Christiane R Maroun, Isabelle Paquin, Arkadii Vaisburg
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引用次数: 73

摘要

组蛋白去乙酰化酶(hdac)和组蛋白乙酰转移酶(HATs)是催化位于组蛋白和非组蛋白NH(2)末端尾部赖氨酸残基去乙酰化和乙酰化的酶。在人类癌症中经常观察到这种平衡的扰动,抑制hdac已成为一种新的抗癌治疗策略。迄今为止,超过30个学术和工业团体参与了与这些目标酶相关的研究。在过去的一年里,数十篇描述新的HDAC抑制剂的研究论文和专利申请已经公开,这些抑制剂属于不同的结构类别。本文综述了HDAC抑制剂的设计和合成的最新进展,这是一种潜在的抗癌药物。
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Histone deacetylase inhibitors: latest developments, trends and prospects.

Histone deacetylases (HDACs) and histone acetyltransferases (HATs) are enzymes that catalyze the deacetylation and acetylation of lysine residues located in the NH(2) terminal tails of histones and non-histone proteins. Perturbation of this balance is often observed in human cancers and inhibition of HDACs has emerged as a novel therapeutic strategy against cancer. To date, more that 30 groups, academic and industrial, are involved in research related to these target enzymes. Over the past year, dozens of research papers and patent applications describing new HDAC inhibitors belonging to different structural classes have been disclosed. The present review highlights the latest developments in design and synthesis of HDAC inhibitors -- potential anti-cancer drugs.

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