title: Direct spectroscopic evidence for binding of anastrozole to the iron heme of human aromatase. Peering into the mechanism of aromatase inhibition.
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.
authors.affiliation: Dipartimento di Chimica IFM, Università di Torino and NIS, Nanostructured Interfaces and Surfaces Centre of Excellence, Via P. Giuria 7, I-10125 Torino, Italy.
authors.forename: Sara
authors.initials: S
authors.lastname: Maurelli
authors.forename: Mario
authors.initials: M
authors.lastname: Chiesa
authors.forename: Elio
authors.initials: E
authors.lastname: Giamello
authors.forename: Giovanna
authors.initials: G
authors.lastname: Di Nardo
authors.forename: Valentina E V
authors.initials: VE
authors.lastname: Ferrero
authors.forename: Gianfranco
authors.initials: G
authors.lastname: Gilardi
authors.forename: Sabine
authors.initials: S
authors.lastname: Van Doorslaer
mesh_terms: D000077384:Anastrozole; D001141:Aromatase / Q000737:chemistry / Q000378:metabolism*; D047072:Aromatase Inhibitors / Q000737:chemistry*; D001665:Binding Sites; D003198:Computer Simulation; D004578:Electron Spin Resonance Spectroscopy; D006418:Heme / Q000737:chemistry*; D006801:Humans; D007501:Iron / Q000737:chemistry; D009570:Nitriles / Q000737:chemistry* / Q000378:metabolism; D011789:Quantum Theory; D014230:Triazoles / Q000737:chemistry* / Q000378:metabolism
chemical_list: D047072:Aromatase Inhibitors; D009570:Nitriles; D014230:Triazoles; D000077384:Anastrozole; D006418:Heme; D007501:Iron; D001141:Aromatase