New approaches for NMR screening in drug discovery.
New approaches for NMR screening in drug discovery.
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DOI：
10.1016/j.ddtec.2004.10.003
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发表时间：
2004-12-01
期刊：
影响因子：
--
通讯作者：
Jahnke, Wolfgang
中科院分区：
文献类型：
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作者：
Fernandez, Cesar;Jahnke, Wolfgang
核磁共振波谱已成为药物研究中一个强大而通用的工具，特别是在蛋白质与配体相互作用的研究中。在过去的几年里，新的核磁共振筛选技术得到了发展。其中一些旨在提高灵敏度，这直接转化为更高的吞吐量和/或减少蛋白质消耗。其他方法引入了全新的筛选概念，并产生了质量不同的信息。本文简要介绍了几种新的核磁共振筛选技术在药物发现中的应用，并讨论了它们的主要优点和缺点。这些方法对药物设计做出了可观的贡献，导致发现了大量与生物相关的蛋白质靶点的高亲和力配体。
NMR spectroscopy has become a powerful and versatile tool in pharmaceutical research, particularly for studies of protein-ligand interactions. During the past few years, new NMR screening techniques have been developed. Some of them aim to increase sensitivity, which translates directly into higher throughput and/or decrease of protein consumption. Other approaches introduce completely new screening concepts and yield qualitatively different information. A brief description of some new NMR screening techniques applied to drug discovery is given in this review, and their principal advantages and drawbacks are discussed. These methods have made an appreciable contribution to drug design, leading to the discovery of a large number of high affinity ligands for biologically relevant protein targets.: