利用双链解旋测定法鉴定 RNA 解旋酶抑制剂。
Identifying RNA Helicase Inhibitors Using Duplex Unwinding Assays.
机构信息
Department of Biochemistry and Molecular Biology, University of Arkansas for Medical Sciences, Little Rock, AR, USA.
出版信息
Methods Mol Biol. 2021;2209:53-72. doi: 10.1007/978-1-0716-0935-4_4.
RNA helicases are responsible for virtually all of RNA metabolism. Viral and bacterial pathogens typically encode their own RNA helicases. Hence, this family of enzymes is increasingly recognized as potential targets for treatment of a variety of diseases. However, the conserved structural similarities among helicase families present an obstacle to the idea of developing specific inhibitors. In order to identify potential modulators of RNA helicase activity, rapid screening approaches are needed. This has been accomplished by optimizing and adapting standard helicase assays to function in high-throughput modalities. These optimized assays have enabled the application of rapid screening approaches to be applied toward discovering helicase inhibitors. This chapter provides detailed protocols for utilizing a medium to high-throughput approach for inhibitor discovery.
RNA 解旋酶几乎负责所有的 RNA 代谢。病毒和细菌病原体通常会编码自己的 RNA 解旋酶。因此，这些酶家族越来越被认为是治疗各种疾病的潜在靶点。然而，解旋酶家族之间的保守结构相似性给开发特异性抑制剂的想法带来了障碍。为了识别 RNA 解旋酶活性的潜在调节剂，需要快速筛选方法。这是通过优化和改编标准解旋酶测定法以在高通量模式下发挥作用来实现的。这些优化的测定法使快速筛选方法能够应用于发现解旋酶抑制剂。本章提供了利用中高通量方法进行抑制剂发现的详细方案。
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