Shapiro M J, Wareing J R
Department of Analytics, Preclinical Research, Novartis Institute for Biomedical Research, Summit, NJ 07901, USA.
Curr Opin Drug Discov Devel. 1999 Jul;2(4):396-400.
High resolution NMR spectroscopy has provided a versatile tool for assessing ligand/receptor interactions. NMR-based methods are currently being investigated which may prove valuable for compound screening. These techniques include the use of chemical shift perturbations, the monitoring of translational diffusion and the observation of NOEs. Novel experiments like TROSY and NOE pumping will play significant roles in looking at proteins larger than 30 kDa. New probe technology such as the Cryoprobe could have a significant impact on NMR-based screening for drug discovery by lowering the necessary amount of (15)N-labled protein.
高分辨率核磁共振光谱法为评估配体/受体相互作用提供了一种通用工具。目前正在研究基于核磁共振的方法,这些方法可能对化合物筛选具有重要价值。这些技术包括利用化学位移扰动、监测平移扩散以及观察核Overhauser效应(NOE)。像横向弛豫优化谱(TROSY)和NOE泵浦这样的新实验,在研究大于30 kDa的蛋白质时将发挥重要作用。诸如低温探头之类的新型探头技术,通过减少所需的(15)N标记蛋白质的量,可能会对基于核磁共振的药物发现筛选产生重大影响。