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17β-Hydroxysteroid dehydrogenase (17β-HSD) type 1 converts estrone to estradiol, a potent ligand for estrogen receptors. It represents an important target for the development of drugs for treatment of estrogen-dependent diseases. In the present study, we have examined the inhibitory activities of some flavonoids, their biosynthetic precursors (cinnamic acids and coumaric acid), and their derivatives...
Different phytoestrogens were tested as inhibitors of 17β-hydroxysteroid dehydrogenase from the fungus Cochliobolus lunatus (17β-HSDcl), a member of the short-chain dehydrogenase/reductase superfamily. Phytoestrogens inhibited the oxidation of 100μM 17β-hydroxyestra-4-en-3-one and the reduction of 100μM estra-4-en-3,17-dione, the best substrate pair known. The best inhibitors of oxidation, with IC...
Different phytoestrogens were tested as inhibitors of 17β-hydroxysteroid dehydrogenase from the fungus Cochliobolus lunatus (17β-HSDcl), a member of the short-chain dehydrogenase/reductase superfamily. Phytoestrogens inhibited the oxidation of 100μM 17β-hydroxyestra-4-en-3-one and the reduction of 100μM estra-4-en-3,17-dione, the best substrate pair known. The best inhibitors of oxidation, with IC...
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