Department of Defense (DOD), National Institutes of Health (NIH)
DoD (award # W81XWH-11-1-0105) and NIH-MBRS SCORE (award # S06 GM 08008) NIH RCMI (award number 8G12MD007595-04)
Department of Chemistry
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.
Molecules 2013, 18, 14470-14495; doi:10.3390/molecules181214470