Paramagnetic relaxation enhancement for protein-observed 19 F NMR as an enabling approach for efficient fragment screening

RSC Advances
Laura M L HawkWilliam C K Pomerantz

Abstract

Protein-observed 19F (PrOF) NMR is an emerging tool for ligand discovery. To optimize the efficiency of PrOF NMR experiments, paramagnetic relaxation enhancement through the addition of chelated Ni(II) was used to shorten longitudinal relaxation time without causing significant line broadening. Thus enhancing relaxation time leads to shorter experiments without perturbing the binding of low- or high-affinity ligands. This method allows for time-efficient screening of potential ligands for a wide variety of proteins in the growing field of fragment-based ligand discovery.

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Citations

Dec 14, 2017·Beilstein Journal of Organic Chemistry·Vladimir Kubyshkin, Nediljko Budisa
Nov 25, 2019·Journal of Biomolecular NMR·Peter D YcasWilliam C K Pomerantz
Apr 30, 2020·Biophysical Journal·Samantha S StadmillerGary J Pielak
Mar 12, 2018·ACS Omega·Luiz F PintoEduardo Fernandez-Megia
Nov 14, 2019·Accounts of Chemical Research·Anand DivakaranWilliam C K Pomerantz

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