Topic
Hydroxysteroid dehydrogenase
About: Hydroxysteroid dehydrogenase is a research topic. Over the lifetime, 1087 publications have been published within this topic receiving 28468 citations. The topic is also known as: hydroxysteroid dehydrogenase.
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TL;DR: It is demonstrated that 11 beta-HSD activity attributed to the chorion is due to decidual contamination and oxidative activity was higher than reductive activity.
15 citations
TL;DR: Inhibition of 20 alpha-HSD activity by steroids was demonstrable at pH 8.8, and Androstenedione was by far the most potent inhibitor, followed by progesterone and 17 alpha-hydroxyprogesterone, Compound S and 20 beta-OH-P.
15 citations
15 citations
TL;DR: New 17β-HSD2 inhibitors from nature are described and insights into the binding pocket of 17 β- HSD2 are provided, offering a promising starting point for further research in this area.
Abstract: 17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) converts the active steroid hormones estradiol, testosterone, and 5α-dihydrotestosterone into their weakly active forms estrone, Δ4-androstene-3,17-dione, and 5α-androstane-3,17-dione, respectively, thereby regulating cell- and tissue-specific steroid action. As reduced levels of active steroids are associated with compromised bone health and onset of osteoporosis, 17β-HSD2 is considered a target for antiosteoporotic treatment. In this study, a pharmacophore model based on 17β-HSD2 inhibitors was applied to a virtual screening of various databases containing natural products in order to discover new lead structures from nature. In total, 36 hit molecules were selected for biological evaluation. Of these compounds, 12 inhibited 17β-HSD2 with nanomolar to low micromolar IC50 values. The most potent compounds, nordihydroguaiaretic acid (1), IC50 0.38 ± 0.04 μM, (−)-dihydroguaiaretic acid (4), IC50 0.94 ± 0.02 μM, isoliquiritigenin (6), IC50 0.36 ± 0.08 μM, a...
15 citations