Discovery of cytochrome p450 1B1 inhibitors as new promising anti-cancer agents

Human cytochrome P450 (CYP)1B1 is a major enzyme for carcinogenic estrogen metabolism and involved in the metabolic activation of procarcinogens of the polycyclic aromatic hydrocarbons (PAHs). CYP1B1 is known to be expressed at a high frequency in various human cancers, but not in normal tissues. It also plays an important role in the metabolism of various anticancer drugs. These findings suggest inhibition of CYP1B1 as a new oncological therapeutic strategy. Several natural and synthetic compounds have been studied in an effort to find the isoform-specific inhibitors of the CYP1 subfamily. A survey of the inhibitors of CYP1B1 and other related inhibitors of the CYP1 subfamily is provided in this review. (C) 2003 Wiley Periodicals, Inc.