Measurement of Ligand–Target Residence Times by 1H Relaxation Dispersion NMR Spectroscopy
详细信息 查看全文
- 作者：Thomas Moschen ; Sarina Grutsch ; Michael A. Juen ; Christoph H. Wunderlich ; Christoph Kreutz ; Martin Tollinger
- 刊名：Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：December 8, 2016
- 年：2016
- 卷：59
- 期：23
- 页码：10788-10793
- 全文大小：468K
- ISSN：1520-4804
文摘
A ligand-observed 1H NMR relaxation experiment is introduced for measuring the binding kinetics of low-molecular-weight compounds to their biomolecular targets. We show that this approach, which does not require any isotope labeling, is applicable to ligand–target systems involving proteins and nucleic acids of variable molecular size. The experiment is particularly useful for the systematic investigation of low affinity molecules with residence times in the micro- to millisecond time regime.