Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR

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Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR

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Title: Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR
Author: Buratto, Roberto; Bornet, Aurélien; Milani, Jonas; Mammoli, Daniele; Vuichoud, Basile; Salvi, Nicola; Singh, Maninder; Laguerre, Aurélien; Passemard, Solène; Gerber-Lemaire, Sandrine; Jannin, Sami; Bodenhausen, Geoffrey

Note: Order does not necessarily reflect citation order of authors.

Citation: Buratto, R., A. Bornet, J. Milani, D. Mammoli, B. Vuichoud, N. Salvi, M. Singh, et al. 2014. “Drug Screening Boosted by Hyperpolarized Long-Lived States in NMR.” Chemmedchem 9 (11): 2509-2515. doi:10.1002/cmdc.201402214. http://dx.doi.org/10.1002/cmdc.201402214.
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Abstract: 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(1H) that are sufficiently long to allow the powerful combination of LLS with dissolution dynamic nuclear polarization (D-DNP). Hyperpolarized weak “spy ligands” can be displaced by high-affinity competitors. Hyperpolarized LLS allow one to decrease both protein and ligand concentrations to micromolar levels and to significantly increase sample throughput.
Published Version: doi:10.1002/cmdc.201402214
Other Sources: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4506523/pdf/
Terms of Use: This article is made available under the terms and conditions applicable to Other Posted Material, as set forth at http://nrs.harvard.edu/urn-3:HUL.InstRepos:dash.current.terms-of-use#LAA
Citable link to this page: http://nrs.harvard.edu/urn-3:HUL.InstRepos:17820887
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