0000000000466240

AUTHOR

Roberto Buratto

showing 1 related works from this author

Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR

2014

International audience; : Transverse and longitudinal relaxation times (T1ρ and T1 ) have been widely exploited in NMR to probe the binding of ligands and putative drugs to target proteins. We have shown recently that long-lived states (LLS) can be more sensitive to ligand binding. LLS can be excited if the ligand comprises at least two coupled spins. Herein we broaden the scope of ligand screening by LLS to arbitrary ligands by covalent attachment of a functional group, which comprises a pair of coupled protons that are isolated from neighboring magnetic nuclei. The resulting functionalized ligands have longitudinal relaxation times T1 ((1) H) that are sufficiently long to allow the powerf…

BromidesMagnetic Resonance SpectroscopyStereochemistryDrug Evaluation PreclinicalThiophenesLigands010402 general chemistry01 natural sciencesBiochemistrydynamic nuclear polarizationchemistry.chemical_compoundNMR spectroscopyCatalytic DomainDrug DiscoveryGeneral Pharmacology Toxicology and PharmaceuticsPharmacologySpins[CHIM.ORGA]Chemical Sciences/Organic chemistry010405 organic chemistryDrug discoveryOrganic ChemistryRelaxation (NMR)ProteinsNuclear magnetic resonance spectroscopyFull PapersLigand (biochemistry)0104 chemical sciencesCrystallographychemistryCovalent bondlong-lived statesExcited stateFunctional groupMolecular MedicineChemMedChem
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