A direct time-based ITC approach for substrate turnover measurements demonstrated on human FMO3

Transient binding events are a challenging issue in enzymology. Here we demostrate a time-based ITC approach to human flavin-containing monooxygenase 3, an important drug metabolising enzyme. We measure kinetic constants and we demonstrate how this approach can be exploited for measuring the inhibit...

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Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2019-05, Vol.55 (44), p.6217-622
Main Authors: Catucci, Gianluca, Sadeghi, Sheila J, Gilardi, Gianfranco
Format: Article
Language:English
Subjects:
Calorimetry - methods
Enzymology
Humans
Kinetics
Methylamines - metabolism
Oxygenases - metabolism
Substrate Specificity
Substrates
Trimethylamine
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Summary:Transient binding events are a challenging issue in enzymology. Here we demostrate a time-based ITC approach to human flavin-containing monooxygenase 3, an important drug metabolising enzyme. We measure kinetic constants and we demonstrate how this approach can be exploited for measuring the inhibiton of the conversion of the key substrate trimethylamine into trimethylamine N -oxide. Using human FMO3 we demonstrate how time-based ITC can be exploited for measuring kinetic constants and the inhibiton of the conversion of the key substrate trimethylamine into trimethylamine N -oxide.
ISSN:1359-7345
1364-548X
DOI:10.1039/c9cc01356c