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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; in revised form: 15 November 2013 / Accepted: 19 November 2013 / Published: 25 November 2013
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
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Cite This Article
MDPI and ACS Style
Liu, J.; Sridhar, J.; Foroozesh, M. Cytochrome P450 Family 1 Inhibitors and Structure-Activity Relationships. Molecules 2013, 18, 14470-14495.
Liu J, Sridhar J, Foroozesh M. Cytochrome P450 Family 1 Inhibitors and Structure-Activity Relationships. Molecules. 2013; 18(12):14470-14495.
Liu, Jiawang; Sridhar, Jayalakshmi; Foroozesh, Maryam. 2013. "Cytochrome P450 Family 1 Inhibitors and Structure-Activity Relationships." Molecules 18, no. 12: 14470-14495.