Chemical Communications · 2013 · 72 citations · 14 references
Bufalin 5β-HydroxylationMolecular BiologyKinetic CharacterizationChemical BiologyEnzymatic ModificationMolecular PharmacologySelective ProbeBioanalysisAnalytical ChemistryIsoform SelectivityBiochemistryBiocatalysisProbe ReactionCytochrome P450 3A4Natural SciencesEnzyme CatalysisChemical ProbeMedicineDrug DiscoveryHigh-throughput ScreeningDrug Analysis
Bufalin 5β-hydroxylation was found to be an isoform-specific biotransformation probe substrate for cytochrome P450 3A4 (CYP3A4). The probe reaction was well-characterized and it can be used for measuring the real catalytic activities of CYP3A4 from different enzyme sources.
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