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

[Image: see text] A ligand-observed (1)H 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 involvi...

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Autores principales: Moschen, Thomas, Grutsch, Sarina, Juen, Michael A., Wunderlich, Christoph H., Kreutz, Christoph, Tollinger, Martin
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5150660/
https://www.ncbi.nlm.nih.gov/pubmed/27933946
http://dx.doi.org/10.1021/acs.jmedchem.6b01110
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author Moschen, Thomas
Grutsch, Sarina
Juen, Michael A.
Wunderlich, Christoph H.
Kreutz, Christoph
Tollinger, Martin
author_facet Moschen, Thomas
Grutsch, Sarina
Juen, Michael A.
Wunderlich, Christoph H.
Kreutz, Christoph
Tollinger, Martin
author_sort Moschen, Thomas
collection PubMed
description [Image: see text] A ligand-observed (1)H 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.
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spelling pubmed-51506602016-12-14 Measurement of Ligand–Target Residence Times by (1)H Relaxation Dispersion NMR Spectroscopy Moschen, Thomas Grutsch, Sarina Juen, Michael A. Wunderlich, Christoph H. Kreutz, Christoph Tollinger, Martin J Med Chem [Image: see text] A ligand-observed (1)H 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. American Chemical Society 2016-11-14 2016-12-08 /pmc/articles/PMC5150660/ /pubmed/27933946 http://dx.doi.org/10.1021/acs.jmedchem.6b01110 Text en Copyright © 2016 American Chemical Society This is an open access article published under a Creative Commons Attribution (CC-BY) License (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) , which permits unrestricted use, distribution and reproduction in any medium, provided the author and source are cited.
spellingShingle Moschen, Thomas
Grutsch, Sarina
Juen, Michael A.
Wunderlich, Christoph H.
Kreutz, Christoph
Tollinger, Martin
Measurement of Ligand–Target Residence Times by (1)H Relaxation Dispersion NMR Spectroscopy
title Measurement of Ligand–Target Residence Times by (1)H Relaxation Dispersion NMR Spectroscopy
title_full Measurement of Ligand–Target Residence Times by (1)H Relaxation Dispersion NMR Spectroscopy
title_fullStr Measurement of Ligand–Target Residence Times by (1)H Relaxation Dispersion NMR Spectroscopy
title_full_unstemmed Measurement of Ligand–Target Residence Times by (1)H Relaxation Dispersion NMR Spectroscopy
title_short Measurement of Ligand–Target Residence Times by (1)H Relaxation Dispersion NMR Spectroscopy
title_sort measurement of ligand–target residence times by (1)h relaxation dispersion nmr spectroscopy
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5150660/
https://www.ncbi.nlm.nih.gov/pubmed/27933946
http://dx.doi.org/10.1021/acs.jmedchem.6b01110
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