title: Measurement of Ligand-Target Residence Times by1H Relaxation Dispersion NMR Spectroscopy.
abstract: A ligand-observed1H 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.
authors.affiliation: Institute of Organic Chemistry and Centre for Molecular Biosciences (CMBI), University of Innsbruck , Innsbruck 6020, Austria.
authors.forename: Thomas
authors.initials: T
authors.lastname: Moschen
authors.affiliation: Institute of Organic Chemistry and Centre for Molecular Biosciences (CMBI), University of Innsbruck , Innsbruck 6020, Austria.
authors.forename: Sarina
authors.initials: S
authors.lastname: Grutsch
authors.affiliation: Institute of Organic Chemistry and Centre for Molecular Biosciences (CMBI), University of Innsbruck , Innsbruck 6020, Austria.
authors.forename: Michael A
authors.initials: MA
authors.lastname: Juen
authors.affiliation: Institute of Organic Chemistry and Centre for Molecular Biosciences (CMBI), University of Innsbruck , Innsbruck 6020, Austria.
authors.forename: Christoph H
authors.initials: CH
authors.lastname: Wunderlich
authors.affiliation: Institute of Organic Chemistry and Centre for Molecular Biosciences (CMBI), University of Innsbruck , Innsbruck 6020, Austria.
authors.forename: Christoph
authors.initials: C
authors.lastname: Kreutz
authors.affiliation: Institute of Organic Chemistry and Centre for Molecular Biosciences (CMBI), University of Innsbruck , Innsbruck 6020, Austria.
authors.forename: Martin
authors.initials: M
authors.lastname: Tollinger
mesh_terms: D004305:Dose-Response Relationship, Drug; D007700:Kinetics; D008024:Ligands; D015394:Molecular Structure; D008970:Molecular Weight; D066244:Proton Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship; D013997:Time Factors
chemical_list: D008024:Ligands