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

Autor:	Moschen, Thomas, Grutsch, Sarina, Juen, Michael A., Wunderlich, Christoph H., Kreutz, Christoph, Tollinger, Martin
Jazyk:	angličtina
Rok vydání:	2016
Předmět:	Molecular Weight Kinetics Structure-Activity Relationship Time Factors Brief Article Dose-Response Relationship Drug Molecular Structure Proton Magnetic Resonance Spectroscopy Ligands
Zdroj:	Journal of Medicinal Chemistry
ISSN:	1520-4804 0022-2623
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::95938acb4bf389230b612438fc6f9f31 http://europepmc.org/articles/PMC5150660 Zobrazit plný text záznamu