| Autor: |
Woo, L. W. L., Sutcliffe, O. B., Bubert, C., Grasso, A., Chander, S. K., Purohit, A., Reed, M. J., Potter, B. V. L. |
| Zdroj: |
Journal of Medicinal Chemistry; July 2003, Vol. 46 Issue: 15 p3193-3196, 4p |
| Abstrakt: |
Aromatase inhibitors in clinical use block the biosynthesis of estrogens. Hydrolysis of estrone 3-sulfate by steroid sulfatase is an important additional source of tumor estrogen, and blockade of both enzymes should provide a more effective endocrine therapy. Sulfamoylated derivatives of the aromatase inhibitor YM511 inhibited sulfatase and aromatase in JEG-3 cells with respective IC50 values of 20−227 and 0.82−100 nM (cf. letrozole, 0.89 nM). One dual inhibitor was potent against both enzymes in vivo, validating the concept. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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