[NMR paper] Protein methylation characterization using NMR without isotopic labeling
Protein methylation characterization using NMR without isotopic labeling
Protein methylation is crucial in epigenetics, and targeting the involved methyltransferases shows great potential for therapeutic intervention with several inhibitors in clinical trials for oncology indications. Therefore, characterization of protein methylation is essential for understanding the methyltransferase function and discovering chemical inhibitors and antagonists. While NMR has been used to measure methylation rates, isotopic labeling of protein or methyl donors can be costly and...
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Efficiently driving protein-based fragment screening and lead discovery using two-dimensional NMR
Efficiently driving protein-based fragment screening and lead discovery using two-dimensional NMR
Abstract
Fragment-based drug discovery (FBDD) and validation of small molecule binders using NMR spectroscopy is an established and widely used method in the early stages of drug discovery. Starting from a library of small compounds, ligand- or protein-observed NMR methods are employed to detect binders, typically weak, that become the starting points for structureâ??activity relationships (SAR) by NMR. Unlike the more frequently used ligand-observed 1D...
[NMR paper] Recent applications of isotopic labeling for protein NMR in drug discovery.
Recent applications of isotopic labeling for protein NMR in drug discovery.
Related Articles Recent applications of isotopic labeling for protein NMR in drug discovery.
Expert Opin Drug Discov. 2013 Mar 12;
Authors: Hiroaki H
Abstract
Introduction: Nuclear magnetic resonance (NMR) applications in drug discovery are classified into two categories: ligand-based methods and protein-based methods. The latter is based on the observation of the (1)H-(15)N HSQC spectra of a protein with and without lead compounds. However, in order to take this...
Beyond Isotopic Labeling: Expanding the Reach of Protein-Detect NMR in Lead Discovery - ACS Publications
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