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: A library of fused (di)cycloalkeno thieno[2,3-d]pyrimidin-4(3H)-one based compounds was synthesized and the majority of these compounds exhibited excellent selectivity over the oxidative isoform 17beta-HSD2 and lacked estrogenic effects in an estrogen receptor (ER) binding assay.
Abstract: Many breast tumors are hormone-dependent, and estrogens, especially estradiol (E2), have a pivotal role in their growth and development. 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of female sex steroids, catalyzing the NADPH-dependent reduction of estrone into biologically active estradiol. In this study, a library of fused (di)cycloalkeno thieno[2,3-d]pyrimidin-4(3H)-one based compounds was synthesized, and the biological activities against 17β-HSD1 in a cell-free and in a cell-based assay were evaluated. Several thieno[2,3-d]pyrimidin-4(3H)-one based compounds, at 0.1 and 1 μM test concentrations, were found to be potent 17β-HSD1 inhibitors. For example, 4-(3-hydroxyphenylthio)-1,2,7,8,9,10,11,13-octahydro-13-oxo-[1]benzothieno[2′,3′:4,5]-pyrimido[1,2-a]azepine-3-carboxaldehyde (7f) is one of the most potent nonsteroidal 17β-HSD1 inhibitors reported to date with 94% inhibition of the recombinant enzyme at 0.1 μM test concentration. Importantly, the majority of...
39 citations
TL;DR: The present study investigates the expression patterns of 17β-hydroxysteroid dehydrogenase (17βHSD) isozymes in human fetal tissues to understand how estrogenic activity is regulated in the human fetus.
Abstract: The present study investigates the expression patterns of 17β-hydroxysteroid dehydrogenase (17βHSD) isozymes in human fetal tissues to understand how estrogenic activity is regulated in the human fetus. Using enzyme assay, high 17βHSD activity was detected in the placenta and liver, and low levels of 17βHSD activity were also present in the gastrointestinal tract and kidney. After Northern blot analysis, we detected the messenger ribonucleic acid for 17βHSD type 1 (17βHSD1) only in the placenta, whereas that for 17βHSD type 2 (17βHSD2) was detected in the placenta, liver, gastrointestinal tract, and urinary tract at 20 gestational weeks. In RT-PCR analysis of the messenger ribonucleic acid transcripts, 17βHSD1 was predominantly expressed in the placenta, brain, heart, lung, and adrenal, whereas 17βHSD2 expression was predominantly detected in the liver, gastrointestinal tract, and kidney. In addition, we detected 17βHSD2 immunoreactive protein in surface epithelial cells of the stomach, absorptive epithel...
39 citations
TL;DR: Cell-specific expression of 17HSD/KSR7 in the ovaries, uteri, and placentas of pregnant and nonpregnant mice using in situ hybridization is demonstrated and messenger RNA is distinctly and exclusively expressed in a proportion of corpora lutea (CLs).
Abstract: Rodent 17β-hydroxysteroid dehydrogenase/17-ketosteroid reductase type 7 (17HSD/KSR7) catalyzes the conversion of estrone (E1) to estradiol (E2) and is abundantly expressed in the ovaries of pregnant animals in particular. In the present work we demonstrate cell-specific expression of 17HSD/KSR7 in the ovaries, uteri, and placentas of pregnant and nonpregnant mice using in situ hybridization. The results show that mouse 17HSD/KSR7 (m17HSD/KSR7) messenger RNA is distinctly and exclusively expressed in a proportion of corpora lutea (CLs). During pregnancy, expression of m17HSD/KSR7 is most abundant around embryonic day 14.5 (E14.5), when the ovaries are filled with CLs expressing 17HSD/KSR7. In the uterus, m17HSD/KSR7 is first detected on E5.5, when expression surrounds the implantation site on the antimesometrial side. As gestation progresses, m17HSD/KSR7 is expressed in the decidua capsularis on E8 and E9.5, disappearing thereafter from the antimesometrial decidua. On E9 onward, m17HSD/KSR7 messenger RNA e...
39 citations
TL;DR: The virtual absence of 5α-reductase in mouse kidney is consistent with the thesis that testosterone rather than dihydrotestosterone may be the intracellular androgen in this organ.
39 citations
TL;DR: The HSD activity was significantly lost after incubation with these enzymes, especially with phospholipase A2, and detergents, indicating that HSD is tightly associated with the particulate components and the activity is stabilized by binding to the membrane.
39 citations