Abstract
The cytochrome P450 (CYP) family contains 57 enzymes in humans. The activity of CYPs against xenobiotics is a primary consideration in drug optimization efforts. Here we describe a series of bioluminescent assays that enable the rapid profiling of CYP activity against compound collections. The assays employ a coupled-enzyme format where firefly luciferase is used to measure CYP enzyme activity through metabolism of pro-luciferase substrates.
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Acknowledgements
This research was supported by the Molecular Libraries Initiative of the NIH Roadmap for Medical Research and the Intramural Research Program of the National Institutes of Health.
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Auld, D.S., Veith, H., Cali, J.J. (2013). Bioluminescent Assays for Cytochrome P450 Enzymes. In: Phillips, I., Shephard, E., Ortiz de Montellano, P. (eds) Cytochrome P450 Protocols. Methods in Molecular Biology, vol 987. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-321-3_1
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DOI: https://doi.org/10.1007/978-1-62703-321-3_1
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Publisher Name: Humana Press, Totowa, NJ
Print ISBN: 978-1-62703-320-6
Online ISBN: 978-1-62703-321-3
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