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Inhibitors of Protein Methyltransferases and Demethylases
Chemical Reviews ( IF 51.4 ) Pub Date : 2017-03-24 00:00:00 , DOI: 10.1021/acs.chemrev.6b00801 H. Ümit Kaniskan 1 , Michael L. Martini 1 , Jian Jin 1
Chemical Reviews ( IF 51.4 ) Pub Date : 2017-03-24 00:00:00 , DOI: 10.1021/acs.chemrev.6b00801 H. Ümit Kaniskan 1 , Michael L. Martini 1 , Jian Jin 1
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Post-translational modifications of histones by protein methyltransferases (PMTs) and histone demethylases (KDMs) play an important role in the regulation of gene expression and transcription and are implicated in cancer and many other diseases. Many of these enzymes also target various nonhistone proteins impacting numerous crucial biological pathways. Given their key biological functions and implications in human diseases, there has been a growing interest in assessing these enzymes as potential therapeutic targets. Consequently, discovering and developing inhibitors of these enzymes has become a very active and fast-growing research area over the past decade. In this review, we cover the discovery, characterization, and biological application of inhibitors of PMTs and KDMs with emphasis on key advancements in the field. We also discuss challenges, opportunities, and future directions in this emerging, exciting research field.
中文翻译：
蛋白质甲基转移酶和脱甲基酶的抑制剂
蛋白甲基转移酶（PMT）和组蛋白脱甲基酶（KDM）对组蛋白的翻译后修饰在调节基因表达和转录中起重要作用，并与癌症和许多其他疾病有关。这些酶中的许多酶还靶向影响多种关键生物学途径的各种非组蛋白蛋白。考虑到它们在人类疾病中的关键生物学功能和意义，人们越来越有兴趣评估这些酶作为潜在的治疗靶标。因此，在过去的十年中，发现和开发这些酶的抑制剂已成为一个非常活跃和快速发展的研究领域。在这篇综述中，我们涵盖了PMT和KDM抑制剂的发现，表征和生物学应用，重点是该领域的关键进展。
更新日期：2017-06-28
中文翻译：
蛋白质甲基转移酶和脱甲基酶的抑制剂
蛋白甲基转移酶（PMT）和组蛋白脱甲基酶（KDM）对组蛋白的翻译后修饰在调节基因表达和转录中起重要作用，并与癌症和许多其他疾病有关。这些酶中的许多酶还靶向影响多种关键生物学途径的各种非组蛋白蛋白。考虑到它们在人类疾病中的关键生物学功能和意义，人们越来越有兴趣评估这些酶作为潜在的治疗靶标。因此，在过去的十年中，发现和开发这些酶的抑制剂已成为一个非常活跃和快速发展的研究领域。在这篇综述中，我们涵盖了PMT和KDM抑制剂的发现，表征和生物学应用，重点是该领域的关键进展。
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