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: The most active compounds in this series represent promising starting points for further structural modifications in the search for more potent inhibitors of AKR1C3.
43 citations
TL;DR: Compound 19 turned out to be the most potent and selective inhibitor of 17 β-HSD2 in cell-free assays and had a very good cellular activity in MDA-MB-231 cells, expressing naturally 17β- HSD2.
Abstract: Estrogen deficiency in postmenopausal women or elderly men is often associated with the skeletal disease osteoporosis. The supplementation of estradiol (E2) in osteoporotic patients is known to prevent bone fracture but cannot be administered because of adverse effect. As 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) oxidizes E2 to its inactive form estrone (E1) and has been found in osteoblastic cells, it is an attractive target for the treatment of osteoporosis. Twenty-one novel, naphthalene-derived compounds have been synthesized and evaluated for their 17β-HSD2 inhibition and their selectivity toward 17β-HSD1 and the estrogen receptors (ERs) α and β. Compound 19 turned out to be the most potent and selective inhibitor of 17β-HSD2 in cell-free assays and had a very good cellular activity in MDA-MB-231 cells, expressing naturally 17β-HSD2. It also showed marked inhibition of the E1-formation by the rat and mouse orthologous enzymes and strong inhibition of monkey 17β-HSD2. It is thus an appropriate...
43 citations
TL;DR: Syntheses and biological evaluation of novel non-steroidal inhibitors designed to mimic the E1 template are reported using information from potent steroidal inhibitors.
43 citations
TL;DR: Property and kinetics of 3β- Hydroxysteroid dehydrogenase and Δ 5 -3- ketosteroid isomerase from the bovine ovary have been examined and non-identity of the sites effecting dehydrogenation and isomerization is indicated by variation of activity ratios during purification, different inactivation rates and different pH curves.
43 citations
TL;DR: The cloned 17βHSD expressed in mammalian cell lines specifically catalyzed the reductive reaction in androgen formation with androstenedione as the preferred substrate, and this reaction was significantly reduced in the absence of glucose.
Abstract: 17β-Hydroxysteroid dehydrogenase (17βHSD), the enzyme that catalyzes the final step of testosterone biosynthesis in the testis, was cloned from a rat Leydig cell complementary DNA library to gain insights into the functional requirements, activation mechanisms, and molecular regulation The 17βHSD complementary DNA encoded 306 amino acids (molecular mass of 337 kDa) and displayed 75% and 85% amino acid sequence homology to the human and mouse 17βHSD type III enzymes, respectively Northern analysis revealed a single 14-kb messenger RNA (mRNA) species in rat Leydig cells, whereas ovarian mRNA was detected only by RT-PCR amplification The cloned 17βHSD expressed in mammalian cell lines specifically catalyzed the reductive reaction in androgen formation with androstenedione as the preferred substrate This reaction was significantly reduced in the absence of glucose Expression of the endogenous 17βHSD gene in rat Leydig cells was inhibited by a single dose of hCG in vivo, with maximum reduction of steady
43 citations