Measurement of Ligand–Target Residence Times by 1H Relaxation Dispersion NMR Spectroscopy

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 nucl...

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Published inJournal of medicinal chemistry Vol. 59; no. 23; pp. 10788 - 10793
Main Authors Moschen, Thomas, Grutsch, Sarina, Juen, Michael A, Wunderlich, Christoph H, Kreutz, Christoph, Tollinger, Martin
Format Journal Article
LanguageEnglish
Published American Chemical Society 08.12.2016
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.6b01110