Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 43, Issue 11, Pages 2298-2306Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.01.044
Keywords
Inhibitor; Enzyme; Hydroxysteroid dehydrogenase; Steroid; Cancer; Estradiol
Categories
Funding
- Canadian Institutes of Health Research (CIHR
- National Science and Engineering Research Council (NSERC) [EM-1745]
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Type 1 17 beta-hydroxysteroid dehydrogenase (17 beta-HSD1) is a key steroidogenic enzyme that catalyses the reduction of steroid estrone into the most potent endogerrous estrogen estradiol using the cofactor NAD(P)H. Bisubstrate inhibition is a good way to enhance the potency of inhibitors of cofactor-assisted enzymes. The design of a bisubstrate inhibitor of 17 beta-HSD1, the estradiol/adenosine hybrid EM-1745, is reviewed and strategies for future designs of inhibitors are proposed. (C) 2008 Elsevier Masson SAS. All rights reserved.
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