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

Cytochrome P450 Family 1 Inhibitors and Structure-Activity Relationships

Department of Chemistry, Xavier University of Louisiana, New Orleans, LA 70125, USA
Author to whom correspondence should be addressed.
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)
View Full-Text   |   Download PDF [983 KB, uploaded 18 June 2014]   |  


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. View Full-Text
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

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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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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