Luminescence-based methods and probes for measuring cytochrome P450 activity
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United States of America
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Sep 10, 2019
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Jul 6, 2017
app pub date -
Jan 18, 2017
filing date -
Jan 18, 2017
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Abstract
The invention provides compounds, compositions, methods, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferins or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. The present method further provides a method for stabilizing and prolonging the luminescent signal in a luciferase-based assay using luciferase stabilizing agents such as reversible lucifetrase inhibitors.
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