Department of Chemistry, Xavier University of Louisiana, New Orleans, LA 70125, USA.
Molecules. 2013 Nov 25;18(12):14470-95. doi: 10.3390/molecules181214470.
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.
自 20 世纪 90 年代以来，O-烷氧基resorufin 脱烷基化测定法得到广泛应用，数千种细胞色素 P450 家族 1 酶（P450s 1A1、1A2 和 1B1）的抑制剂已被鉴定和研究。通常，平面多环分子，如多环芳烃、芪类和类黄酮，被认为是这些酶的潜在有效抑制剂，然而，这些抑制剂的结构-活性关系和选择性的详细信息仍然不清楚。在这篇综述中，我们通过荟萃分析彻底讨论了过去 20 年报道的许多代表性 P450 家族 1 抑制剂的选择性。
