摘要
表观遗传学研究最近已经成为生命科学和药物设计领域的研究热点之一。DNA甲基化和组蛋白甲基化在影响基因表达和基因组功能方面起到关键作用。对于治疗包括癌症在内的许多疾病,抑制DNA和组蛋白甲基转移酶(DNMTs and HMTs)是一种有希望的方案。本文就甲基转移酶晶体结构解析和具有生物活性抑制剂的筛选的最新研究成果进行了综述。为了阐释包括内部和外部的甲基转移酶与抑制剂的相互作用如何发生,我们 不仅讨论了DNA和HMT的结构特点,而且也讨论了转移酶抑制剂的机制与结构-功能的关系。本研究对DNA/组蛋白甲基转移酶的生物学功能及其抑制剂的发现和开发进行了简略综述。
关键词: DNA甲基转移酶,药物研发,表观遗传治疗,组蛋白甲基转移酶,抑制剂
Current Medicinal Chemistry
Title:Interaction Between DNA/histone Methyltransferases and their Inhibitors
Volume: 22 Issue: 3
Author(s): J. Hu, S. Chen, X. Kong, K. Zhu, S. Cheng, M. Zheng, H. Jiang and C. Luo
Affiliation:
关键词: DNA甲基转移酶,药物研发,表观遗传治疗,组蛋白甲基转移酶,抑制剂
摘要: Epigenetic research has recently become one of the hotspots in the field of bioscience and drug design. DNA methylation and histone methylation serve a critical function in influencing gene expression and genome function. The inhibition of DNA and histone methyltransferases (DNMTs and HMTs) is a promising approach for the therapeutic treatment of numerous diseases, including cancer. This work reviews the recent achievements in methyltransferase crystallographic structure resolution and bioactive inhibitor screening. We discuss the features of DNA and HMT structures, as well as the mechanism and structure–function relationship of transferase inhibitors, to elucidate how methyltransferase and inhibitor interactions occur both internally and externally. This study briefly reviews the biological function, as well as the inhibitor discovery and development, of DNA/histone methyltransferases.
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Hu J., Chen S., Kong X., Zhu K., Cheng S., Zheng M., Jiang H. and Luo C., Interaction Between DNA/histone Methyltransferases and their Inhibitors, Current Medicinal Chemistry 2015; 22 (3) . https://dx.doi.org/10.2174/0929867321666141106114538
DOI https://dx.doi.org/10.2174/0929867321666141106114538 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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