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 anti-cancer 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.
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