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CYP3As catalyze nifedipine oxidation in pig liver microsomes: Enzyme kinetics, inhibition and functional expression

Paper ID Volume ID Publish Year Pages File Format Full-Text
50878 46820 2011 4 PDF Available
Title
CYP3As catalyze nifedipine oxidation in pig liver microsomes: Enzyme kinetics, inhibition and functional expression
Abstract

Cytochrome P450 (CYP) 3As have received much attention because of their importance in drug metabolism. However, information on CYP3As in pigs is still largely incomplete. Herein, we focused on the involvement of CYP3As in nifedipine oxidation in pig liver microsomes. Enzyme kinetics, inhibition and immunochemical studies indicated that CYP3As might catalyze nifedipine oxidation and that ketoconazole could strongly inhibit this reaction in a noncompetitive and time-dependent manner. Furthermore, pig CYP3A46, showing the highest amino acid sequence identity to human CYP3A4, exhibited nifedipine oxidation activity. Collectively, these results provide strong evidence that CYP3As catalyze nifedipine oxidation in pig liver microsomes.

Graphical AbstractFigure optionsDownload full-size imageDownload as PowerPoint slideResearch Highlights►Ketoconazole noncompetitively and time-dependently inhibited nifedipine oxidation in pig liver microsomes. ►Recombinant CYP3A46 exhibited nifedipine oxidation activity. ►CYP3As catalyze nifedipine oxidation in pig liver microsomes.

Keywords
Pig liver microsomes; CYP3A; Nifedipine oxidation; Ketoconazole; CYP3A46
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CYP3As catalyze nifedipine oxidation in pig liver microsomes: Enzyme kinetics, inhibition and functional expression
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Publisher
Database: Elsevier - ScienceDirect
Journal: Catalysis Communications - Volume 12, Issue 8, 31 March 2011, Pages 694–697
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Catalysis
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us