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Histone lysine methyltransferases in biology and disease.
Nature Structural & Molecular Biology ( IF 12.5 ) Pub Date : 2019-10-03 , DOI: 10.1038/s41594-019-0298-7 Dylan Husmann 1 , Or Gozani 1
Nature Structural & Molecular Biology ( IF 12.5 ) Pub Date : 2019-10-03 , DOI: 10.1038/s41594-019-0298-7 Dylan Husmann 1 , Or Gozani 1
Affiliation
The precise temporal and spatial coordination of histone lysine methylation dynamics across the epigenome regulates virtually all DNA-templated processes. A large number of histone lysine methyltransferase (KMT) enzymes catalyze the various lysine methylation events decorating the core histone proteins. Mutations, genetic translocations and altered gene expression involving these KMTs are frequently observed in cancer, developmental disorders and other pathologies. Therapeutic compounds targeting specific KMTs are currently being tested in the clinic, although overall drug discovery in the field is relatively underdeveloped. Here we review the biochemical and biological activities of histone KMTs and their connections to human diseases, focusing on cancer. We also discuss the scientific and clinical challenges and opportunities in studying KMTs.
中文翻译:
组蛋白赖氨酸甲基转移酶在生物学和疾病中的作用。
整个表观基因组中组蛋白赖氨酸甲基化动力学的精确时间和空间协调实际上调节了所有以DNA为模板的过程。大量的组蛋白赖氨酸甲基转移酶(KMT)酶催化装饰核心组蛋白的各种赖氨酸甲基化事件。涉及这些KMT的突变,遗传易位和基因表达改变通常在癌症,发育障碍和其他病理中观察到。尽管针对该领域的整体药物研发还相对欠发达,但目前正在临床中测试靶向特定KMT的治疗性化合物。在这里,我们回顾了组蛋白KMT的生化和生物学活性及其与人类疾病的联系,重点是癌症。我们还将讨论研究KMT的科学和临床挑战与机遇。
更新日期:2019-10-03
中文翻译:
组蛋白赖氨酸甲基转移酶在生物学和疾病中的作用。
整个表观基因组中组蛋白赖氨酸甲基化动力学的精确时间和空间协调实际上调节了所有以DNA为模板的过程。大量的组蛋白赖氨酸甲基转移酶(KMT)酶催化装饰核心组蛋白的各种赖氨酸甲基化事件。涉及这些KMT的突变,遗传易位和基因表达改变通常在癌症,发育障碍和其他病理中观察到。尽管针对该领域的整体药物研发还相对欠发达,但目前正在临床中测试靶向特定KMT的治疗性化合物。在这里,我们回顾了组蛋白KMT的生化和生物学活性及其与人类疾病的联系,重点是癌症。我们还将讨论研究KMT的科学和临床挑战与机遇。