Screening and profiling assays for HDACs and sirtuins.
Screening and profiling assays for HDACs and sirtuins.
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DOI：
10.1016/j.ddtec.2015.10.008
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发表时间：
2015-11-01
期刊：
影响因子：
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通讯作者：
Howitz, Konrad T
中科院分区：
文献类型：
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作者：
Howitz, Konrad T
表观遗传因子是赋予、去除或识别染色质DNA或蛋白质的共价修饰的酶或蛋白质。他们可以分为三大类，通常被称为“作家”，“橡皮擦”和“读者”。HDAC和sirtuins从蛋白质赖氨酸残基的β-氨基上去除乙酰基，属于“橡皮擦”类别。由于它们对基因表达的重要作用和参与各种疾病状态，近年来这些酶一直是许多测定开发工作的主题。常用的技术包括质谱法、基于抗体的方法和使用荧光肽底物的蛋白酶偶联测定。最近的进展包括合成底物的发展，用于测定各种新发现的非乙酰基去酰化活性的sirtuins。
Epigenetic factors are enzymes or proteins that confer, remove or recognize covalent modifications to chromatin DNA or proteins. They can be divided into three broad groups, commonly referred to as the 'writers', 'erasers' and 'readers'. The HDACs and sirtuins, which remove acetyl groups from the É›-amino of protein lysine residues, fall into the 'eraser' category. Due to their important effects on gene expression and involvement in various disease states, these enzymes have been the subjects of many assay development efforts in recent years. Commonly used techniques include mass spectrometry, antibody-based methods and protease-coupled assays with fluorogenic peptide substrates. Recent advances include the development of synthetic substrates for the assay of various newly discovered non-acetyl deacylation activities among the sirtuins.