Rapid acquisition of 1H and 19F NMR experiments for direct and competition ligand-based screening
Rapid acquisition of 1H and 19F NMR experiments for direct and competition ligand-based screening
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DOI：
10.1002/mrc.2733
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发表时间：
2011-04-01
影响因子：
2
通讯作者：
Piotto, Martial
中科院分区：
文献类型：
--
作者：
Dalvit, Claudio;Gossert, Alvar D.;Piotto, Martial
由于 NMR 对蛋白质结合事件的相对敏感性较高，直接和基于竞争配体的 NMR 实验通常用于针对蛋白质靶标筛选化学片段库。为此目的，已经提出了大量的核磁共振方法。其中两项技术是 F-19 T-2 滤波器和 H-1 选择性 T-2 滤波器实验。这些实验的脉冲序列的修改导致实验时间减少了近 2 倍，从而提高了筛选通量，并使 NMR 成为筛选大型化合物集合的有吸引力的技术。版权所有 (C) 2011 John Wiley & Sons, Ltd.
Direct and competition ligand-based NMR experiments are often used in the screening of chemical fragment libraries against a protein target due to the high relative sensitivity of NMR for protein-binding events. A plethora of NMR methods has been proposed for this purpose. Two of these techniques are the F-19 T-2 filter and the H-1 selective T-2 filter experiments. Modifications of the pulse sequences of these experiments have resulted in a similar to 2-fold reduction in the experiment time thus allowing an increase in the screening throughput and making NMR an attractive technique for screening large compound collections. Copyright (C) 2011 John Wiley & Sons, Ltd.