Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease.
Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease.
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DOI：
10.1038/s41573-020-00108-x
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发表时间：
2021-04
期刊：
影响因子：
--
通讯作者：
Gozani O
中科院分区：
文献类型：
--
作者：
Bhat KP;Ümit Kaniskan H;Jin J;Gozani O
蛋白质赖氨酸甲基化是一种重要的翻译后修饰，调节组蛋白和非组蛋白的功能。蛋白质赖氨酸甲基化的酶或“作家”赖氨酸甲基转移酶（KMT）的失调涉及许多疾病的原因，包括癌症、精神健康障碍和发育障碍。在过去的十年中，在开发靶向参与组蛋白甲基化和表观遗传调控的KMT的药物方面取得了重大进展。这些抑制剂中的第一种，tazemetostat，最近被批准用于治疗上皮样肉瘤和滤泡性淋巴瘤，还有几种正在进行临床和临床前评估。除了染色质之外，许多调节蛋白质合成和其他基本生物过程的KMT正在成为药物开发的有希望的新靶点，以治疗各种疾病。
Protein lysine methylation is a crucial post-translational modification that regulates the functions of both histone and non-histone proteins. Deregulation of the enzymes or’writers’ of protein lysine methylation, lysine methyltransferases (KMTs), is implicated in the cause of many diseases, including cancer, mental health disorders and developmental disorders. Over the past decade, significant advances have been made in developing drugs to target KMTs that are involved in histone methylation and epigenetic regulation. The first of these inhibitors, tazemetostat, was recently approved for the treatment of epithelioid sarcoma and follicular lymphoma, and several more are in clinical and preclinical evaluation. Beyond chromatin, the many KMTs that regulate protein synthesis and other fundamental biological processes are emerging as promising new targets for drug development to treat diverse diseases.
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