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肿瘤表观基因组学:让组蛋白赖氨酸甲基化发挥作用。

Oncoepigenomics: making histone lysine methylation count.

机构信息

Department of Pharmaceutical Sciences, University of Connecticut, 69 N Eagleville Rd., Unit 3092, Storrs, CT 06269-3092, USA.

出版信息

Eur J Med Chem. 2012 Oct;56:179-94. doi: 10.1016/j.ejmech.2012.08.010. Epub 2012 Aug 11.

Abstract

Increasing studies show that methylation of histone lysine residues is implicated in the development and progression of varying disease states such as schizophrenia, diabetes, and multiple human cancers. Targeting the specific enzymes responsible for these processes has fueled global investigation into the understanding and correction of epigenetic pathology. This review aims to assemble a timely account of the current progress against chromatin-modifying histone lysine methyltransferases (KMTs) and demethylases (KDMs) to inform ongoing and future efforts into this promising field. In particular, we report on their role in tumor growth and progression and the development of small molecules that modulate these enzymes.

摘要

越来越多的研究表明,组蛋白赖氨酸残基的甲基化与各种疾病状态的发展和进展有关,如精神分裂症、糖尿病和多种人类癌症。针对这些过程中负责的特定酶的靶向治疗激发了全球对表观遗传病理学的理解和纠正的研究。本综述旨在及时总结针对染色质修饰组蛋白赖氨酸甲基转移酶(KMT)和去甲基化酶(KDM)的最新进展,为该有前途的领域的当前和未来的研究提供信息。特别是,我们报告了它们在肿瘤生长和进展以及调节这些酶的小分子开发中的作用。

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