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Literature DB >> 21858332

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

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

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. This journal is © The Royal Society of Chemistry 2011

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Year: 2011 PMID： 21858332 DOI： 10.1039/c1cc13872c

Source DB: PubMed Journal: Chem Commun (Camb) ISSN： 1359-7345 Impact factor: 6.222

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Cited

7 in total

1. Organoruthenium(II) Complexes Bearing an Aromatase Inhibitor: Synthesis, Characterization, in Vitro Biological Activity and in Vivo Toxicity in Zebrafish Embryos.

Authors: Golara Golbaghi; Mohammad Mehdi Haghdoost; Debbie Yancu; Yossef López de Los Santos; Nicolas Doucet; Shunmoogum A Patten; J Thomas Sanderson; Annie Castonguay
Journal: Organometallics Date: 2019-01-31 Impact factor: 3.876

2. Synthesis and biological assessment of a ruthenium(II) cyclopentadienyl complex in breast cancer cells and on the development of zebrafish embryos.

Authors: Golara Golbaghi; Irène Pitard; Matthieu Lucas; Mohammad Mehdi Haghdoost; Yossef López de Los Santos; Nicolas Doucet; Shunmoogum A Patten; J Thomas Sanderson; Annie Castonguay
Journal: Eur J Med Chem Date: 2020-01-03 Impact factor: 6.514

3. Evidence for an elevated aspartate pK(a) in the active site of human aromatase.

Authors: Giovanna Di Nardo; Maximilian Breitner; Andrea Bandino; Debashis Ghosh; Gareth K Jennings; John C Hackett; Gianfranco Gilardi
Journal: J Biol Chem Date: 2014-11-25 Impact factor: 5.157

Review 4. Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021.

Authors: Qing Wu; Wei Qian; Xiaoli Sun; Shaojie Jiang
Journal: J Hematol Oncol Date: 2022-10-08 Impact factor: 23.168

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

1. Organoruthenium(II) Complexes Bearing an Aromatase Inhibitor: Synthesis, Characterization, in Vitro Biological Activity and in Vivo Toxicity in Zebrafish Embryos.

2. Synthesis and biological assessment of a ruthenium(II) cyclopentadienyl complex in breast cancer cells and on the development of zebrafish embryos.

3. Evidence for an elevated aspartate pK(a) in the active site of human aromatase.

Review 4. Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021.

5. Probing the origins of aromatase inhibitory activity of disubstituted coumarins via QSAR and molecular docking.

6. Strength of axial water ligation in substrate-free cytochrome P450s is isoform dependent.

7. Dynamics and flexibility of human aromatase probed by FTIR and time resolved fluorescence spectroscopy.