Hawk Laura M L, Gee Clifford T, Urick Andrew K, Hu Haitao, Pomerantz William C K
Department of Chemistry, University of Minnesota, 207 Pleasant St. SE, Minneapolis, MN 55455, United States.
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, United States.
RSC Adv. 2016;6(98):95715-95721. doi: 10.1039/C6RA21226C. Epub 2016 Sep 29.
Protein-observed F (PrOF) NMR is an emerging tool for ligand discovery. To optimize the efficiency of PrOF NMR experiments, paramagnetic relaxation enhancement through the addition of chelated Ni(II) was used to shorten longitudinal relaxation time without causing significant line broadening. Thus enhancing relaxation time leads to shorter experiments without perturbing the binding of low- or high-affinity ligands. This method allows for time-efficient screening of potential ligands for a wide variety of proteins in the growing field of fragment-based ligand discovery.
蛋白质观测F（PrOF）核磁共振是一种新兴的配体发现工具。为了优化PrOF核磁共振实验的效率，通过添加螯合的Ni(II)来实现顺磁弛豫增强，以缩短纵向弛豫时间，同时不会导致明显的谱线展宽。因此，增强弛豫时间可使实验时间缩短，而不会干扰低亲和力或高亲和力配体的结合。这种方法能够在基于片段的配体发现这一不断发展的领域中，对多种蛋白质的潜在配体进行高效的时间筛选。
