Journal
MOLECULES
Volume 18, Issue 12, Pages 14470-14495Publisher
MDPI
DOI: 10.3390/molecules181214470
Keywords
cytochrome P450; enzyme inhibitor; stilbenoids; flavonoids; structure activity relationships; mechanism-based inhibitor
Funding
- DoD [W81XWH-11-1-0105]
- NIH-MBRS SCORE [S06 GM 08008]
- NIH RCMI [8G12MD007595]
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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.
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