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

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

doi:10.1039/c1cc13872c

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

Chem Commun (Camb). 2011 Oct 14;47(38):10737-9. doi: 10.1039/c1cc13872c. Epub 2011 Aug 22.

Authors

Sara Maurelli¹, Mario Chiesa, Elio Giamello, Giovanna Di Nardo, Valentina E V Ferrero, Gianfranco Gilardi, Sabine Van Doorslaer

Affiliation

¹ Dipartimento di Chimica IFM, Università di Torino and NIS, Nanostructured Interfaces and Surfaces Centre of Excellence, Via P. Giuria 7, I-10125 Torino, Italy.

PMID: 21858332
DOI: 10.1039/c1cc13872c

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.

MeSH terms

Anastrozole
Aromatase / chemistry
Aromatase / metabolism*
Aromatase Inhibitors / chemistry*
Binding Sites
Computer Simulation
Electron Spin Resonance Spectroscopy
Heme / chemistry*
Humans
Iron / chemistry
Nitriles / chemistry*
Nitriles / metabolism
Quantum Theory
Triazoles / chemistry*
Triazoles / metabolism

Substances

Aromatase Inhibitors
Nitriles
Triazoles
Anastrozole
Heme
Iron
Aromatase