Direct spectroscopic evidence for binding of anastrozole to the iron heme of human aromatase. Peering into the mechanism of aromatase inhibition

Literature Information

Publication Date 2011-08-22
DOI 10.1039/C1CC13872C
Impact Factor 6.222
Authors

Sara Maurelli, Mario Chiesa, Elio Giamello, Giovanna Di Nardo, Valentina E. V. Ferrero, Gianfranco Gilardi, Sabine Van Doorslaer


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Abstract

Aromatase (CYP19A1), is a microsomal cytochrome P450 catalysing the conversion of androgens to estrogens. Non-steroidal inhibitors, such as anastrozole, are important drugs in breast cancer therapy. Using hyperfine sublevel correlation (HYSCORE) spectroscopy we provide the first experimental evidence of the binding of anastrozole to the iron heme of human aromatase.

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