Direct spectroscopic evidence for binding of anastrozole to the iron heme of human aromatase. Peering into the mechanism of aromatase inhibition
Direct spectroscopic evidence for binding of anastrozole to the iron heme of human aromatase. Peering into the mechanism of aromatase inhibition
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DOI：
10.1039/c1cc13872c
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发表时间：
2011-01-01
影响因子：
4.9
通讯作者：
Van Doorslaer, Sabine
中科院分区：
文献类型：
--
作者：
Maurelli, Sara;Chiesa, Mario;Van Doorslaer, Sabine
芳香化酶（CYP19A1）是微粒体细胞色素P450，催化雄激素向雌激素的转化。非甾体抑制剂，如阿那曲唑，是乳腺癌治疗中的重要药物。利用超精细亚水平相关（HYSCORE）光谱，我们首次提供了阿那曲唑与人芳香酶铁血红素结合的实验证据。
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.