QUANTITATIVE RANKING OF TRANSIENT LIGAND BINDING TO TARGET BIOMOLECULES BY USE OF NUCLEAR MAGNETIC RESONANCE

摘要

The present invention relates to a new use of NMR for quantitatively ranking transient ligand binding to target biomolecules. The present invention also relates to a new method to identify ligand site obeying two-state and more complex binding behavior in a transient complex of a ligand with a target molecule, still with the use of NMR. There is also provided an efficient method to quantitate fast dissociation rates of ligands containing at least one magnetic nuclei by performing NMR relaxation dispersion experiments at different protein concentrations, enabling the evaluation of populations and exchange rates, and extending the practical applicability of the NMR relaxation dispersion experiments.