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Molecules 2013, 18(12), 14470-14495; doi:10.3390/molecules181214470
Review

Cytochrome P450 Family 1 Inhibitors and Structure-Activity Relationships

,  and *
Received: 22 September 2013 / Revised: 15 November 2013 / Accepted: 19 November 2013 / Published: 25 November 2013
(This article belongs to the Special Issue Enzyme Chemistry)
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Abstract

With the widespread use of O-alkoxyresorufin dealkylation assays since the 1990s, thousands of inhibitors of cytochrome P450 family 1 enzymes (P450s 1A1, 1A2, and 1B1) have been identified and studied. Generally, planar polycyclic molecules such as polycyclic aromatic hydrocarbons, stilbenoids, and flavonoids are considered to potentially be effective inhibitors of these enzymes, however, the details of the structure-activity relationships and selectivity of these inhibitors are still ambiguous. In this review, we thoroughly discuss the selectivity of many representative P450 family 1 inhibitors reported in the past 20 years through a meta-analysis.
Keywords: cytochrome P450; enzyme inhibitor; stilbenoids; flavonoids; structure activity relationships; mechanism-based inhibitor cytochrome P450; enzyme inhibitor; stilbenoids; flavonoids; structure activity relationships; mechanism-based inhibitor
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Liu, J.; Sridhar, J.; Foroozesh, M. Cytochrome P450 Family 1 Inhibitors and Structure-Activity Relationships. Molecules 2013, 18, 14470-14495.

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