Fuhrmann Jakob, Thompson Paul R
Department of Chemistry, The Scripps Research Institute , 130 Scripps Way, Jupiter, Florida 33458, United States.
Department of Biochemistry and Molecular Pharmacology, UMass Medical School , 364 Plantation Street, Worcester, Massachusetts 01605, United States.
ACS Chem Biol. 2016 Mar 18;11(3):654-68. doi: 10.1021/acschembio.5b00942. Epub 2015 Dec 31.
The post-translational modification of arginine residues represents a key mechanism for the epigenetic control of gene expression. Aberrant levels of histone arginine modifications have been linked to the development of several diseases including cancer. In recent years, great progress has been made in understanding the physiological role of individual arginine modifications and their effects on chromatin function. The present review aims to summarize the structural and functional aspects of histone arginine modifying enzymes and their impact on gene transcription. We will discuss the potential for targeting these proteins with small molecules in a variety of disease states.
精氨酸残基的翻译后修饰是基因表达表观遗传控制的关键机制。组蛋白精氨酸修饰水平异常与包括癌症在内的多种疾病的发生发展有关。近年来,在理解单个精氨酸修饰的生理作用及其对染色质功能的影响方面取得了巨大进展。本综述旨在总结组蛋白精氨酸修饰酶的结构和功能方面及其对基因转录的影响。我们将讨论在各种疾病状态下用小分子靶向这些蛋白质的潜力。