In vitro assays for the determination of histone deacetylase activity
In vitro assays for the determination of histone deacetylase activity
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DOI：
10.1016/j.ymeth.2005.03.003
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发表时间：
2005-08-01
期刊：
影响因子：
4.8
通讯作者：
Jung, M
中科院分区：
文献类型：
--
作者：
Heltweg, B;Trapp, J;Jung, M
组蛋白去乙酰化酶是重要的转录调节因子，也是抗癌药物的新靶点。我们提出了一个概述，包括放射性标记的组蛋白，寡肽和小分子作为底物的各种检测格式。各种格式的优点和缺点，例如，底物的可用性，生产量或亚型的选择性进行了讨论。详细的程序，可用于不同的问题，如库筛选或荧光抑制剂测试，各种检测类型。我们提出了一个新的协议，一个简单的高通量检测NAD（+）依赖性（III类）组蛋白脱乙酰酶，也称为sirtuins。(c)2005年爱思唯尔公司All rights reserved.
Histone deacetylases are important regulators of transcription and an emerging target for anticancer drugs. We present an overview over various assay formats that include radiolabelled histones, oligopeptides, and small molecules as substrates. The advantages and disadvantages of the various formats in terms of, e.g., substrate availability, throughput or subtype selectivity are discussed. Detailed procedures for various assay types that can be used for different problems, such as library screening or fluorescent inhibitor testing, are given. We present a new protocol for a simple high-throughput assay for NAD(+)-dependent (class III) histone deacetylases, also termed sirtuins. (c) 2005 Elsevier Inc. All rights reserved.