Affinity screening using competitive binding with fluorine-19 hyperpolarized ligands.
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ABSTRACT:
SUBMITTER: Kim Y
PROVIDER: S-EPMC4472436 | biostudies-literature | 2015 Apr
REPOSITORIES: biostudies-literature
Publications
Affinity screening using competitive binding with fluorine-19 hyperpolarized ligands.
Kim Yaewon Y Hilty Christian C
Angewandte Chemie (International ed. in English) 20150220 16
Fluorine-19 NMR and hyperpolarization form a powerful combination for drug screening. Under a competitive equilibrium with a selected fluorinated reporter ligand, the dissociation constant (K(D)) of other ligands of interest is measurable using a single-scan Carr-Purcell-Meiboom-Gill (CPMG) experiment, without the need for a titration. This method is demonstrated by characterizing the binding of three ligands with different affinities for the serine protease trypsin. Monte Carlo simulations show ...[more]
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