Drug Discovery and Development, Italian Institute of Technology, Genova, Italy.
Magn Reson Chem. 2011 Apr;49(4):199-202. doi: 10.1002/mrc.2733. Epub 2011 Mar 9.
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 (19)F T(2) filter and the (1)H selective T(2) filter experiments. Modifications of the pulse sequences of these experiments have resulted in a ∼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.
由于 NMR 对蛋白质结合事件具有较高的相对灵敏度,因此在筛选针对蛋白质靶标的化学片段文库时,通常使用直接竞争配体的 NMR 实验。为此提出了许多 NMR 方法。其中两种技术是(19)F T(2)滤波器和(1)H 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约 2 倍,从而增加了筛选通量,使 NMR 成为筛选大型化合物库的有吸引力的技术。