Cookies on this website

We use cookies to ensure that we give you the best experience on our website. If you click 'Accept all cookies' we'll assume that you are happy to receive all cookies and you won't see this message again. If you click 'Reject all non-essential cookies' only necessary cookies providing core functionality such as security, network management, and accessibility will be enabled. Click 'Find out more' for information on how to change your cookie settings.

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