Vorozole has been reported to be a potent, long acting and selective non-steroidal aromatase inhibitor.  It has the potential to treat estrogen dependent diseases and its carbon-11-analog is currently being tested as a radiotracer for brain aromatase (CYP19).  It was found that the carbon-11-vorozole binds tightly to an unknown protein in the liver that is not CYP19.  While vorozole is considered selective, this selectivity has only been shown when compared to enzymes involved in steroidogenesis.  Since CYP19 is in a superfamily of enzymes called cytochrome P450s (CYPs) and there are many other enzymes in this class that are in high concentration in the liver, it is highly likely that vorozole is binding to a CYP. Screening of vorozole on these CYPs may lead to the identification of this unknown liver enzyme that vorozole is binding to.  Our lab uses fluorometric high-throughput screening assays to screen vorozole on these CYPs.

Screening vorozole on a series of human liver cytochrome P450s

243rd National Meeting (2012)

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