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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 IC(50) 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.

Original publication

DOI

10.1021/jm034033b

Type

Journal article

Journal

J Med Chem

Publication Date

17/07/2003

Volume

46

Pages

3193 - 3196

Keywords

Animals, Anti-Inflammatory Agents, Non-Steroidal, Antineoplastic Agents, Aromatase Inhibitors, Arylsulfatases, Cell Line, Enzyme Inhibitors, Estradiol, Estrogen Antagonists, Female, Humans, Liver, Rats, Rats, Wistar, Steryl-Sulfatase