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 preliminary results of the synthesis and biochemical evaluation of a number of 4-hydroxyphenyl ketones as inhibitors of the isozyme of the enzyme 17beta-hydroxysteroid dehydrogenase (17beta-HSD) responsible for the conversion of androstenedione to testosterone (T), more specifically type 3 are reported.
14 citations
TL;DR: The present study suggests that HSDs may catalyze the C-3 epimerization of vitamin D compounds and modulate their concentrations and biological activities in animals and humans.
14 citations
TL;DR: An X-ray crystallographic study has been undertaken and the optimal conditions for crystallization of 17beta-HSDcl (apo form) were established, resulting in well shaped crystals that diffracted to 1.7 A resolution.
Abstract: 17β-Hydroxysteroid dehydrogenase from the filamentous fungus Cochliobolus lunatus (17β-HSDcl) is an NADP(H)-dependent enzyme that preferentially catalyses the oxidoreduction of oestrogens and androgens. The enzyme belongs to the short-chain dehydrogenase/reductase superfamily and is the only fungal hydroxysteroid dehydrogenase known to date. 17β-HSDcl has recently been characterized and cloned and has been the subject of several functional studies. Although several hypotheses on the physiological role of 17β-HSDcl in fungal metabolism have been formulated, its function is still unclear. An X-ray crystallographic study has been undertaken and the optimal conditions for crystallization of 17β-HSDcl (apo form) were established, resulting in well shaped crystals that diffracted to 1.7 A resolution. The space group was identified as I4122, with unit-cell parameters a = b = 67.14, c = 266.77 A. Phasing was successfully performed by Patterson search techniques. A catalytic inactive mutant Tyr167Phe was also engineered, expressed, purified and crystallized for functional and structural studies.
14 citations
TL;DR: In vitro biological evaluation of these steroid derivatives revealed that a spacer of 13 methylenes, between the 16β-position of E2 and the adenosine mimic bearing a carboxylic acid group, gave the best inhibition of 17β-HSD1.
Abstract: A series of estradiol (E2) derivatives were designed to interact with both the substrate- and the cofactor-binding sites of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1). These analogues of po...
14 citations
TL;DR: Results indicate that the pelvic nerves participate in the orchestration of endocrine and uterine events in the pre-parturient and parturient periods in the rat.
Abstract: Summary Several workers have reported that section of the pelvic parasympathetic nerves [pelvic neurectomy (PN)] in pregnant rats is compatible with pregnancy, but parturition is blocked. The cause of this blocked parturition remains unexplained. To determine if PN had a possible action on progesterone and prostaglandin, two endocrine mediators of labor, we neurectomized (PN) or sham-operated (S) rats on days 8-10 of pregnancy. Then on days 20, 21, 22, 23 and 24 (PN only) rats were lightly etherized and utero-ovarian vein (UOV) blood was collected, centrifuged and plasma frozen and stored at −60° until radioimmunoassay for progesterone, 20α-dihydroprogesterone (20α-ol), prostaglandin F2α (PGF), and prostaglandin E2 (PGE). One ovary from each rat was immersed in a BEEM capsule containing OCT compound, frozen and stored at −20° for 20α-hydroxysteroid dehydrogenase (20α-HSD) histochemistry. Analysis of variance indicated a significant (P < 0.01) decline in plasma progesterone in the S animals on the days studied but the PN animals remained unchanged through day 22. Student's Newman-Keuls (SNK) analysis for multiple critical values indicated that plasma progesterone on days 20 and 21 was not different in the S animals but declined (P < 0.01) on day 22. Progesterone also declined on days 23 and 24 in PN animals. There was a significant increase (P < 0.05) between day 20, 21 and 22 plasma PGF in the S but no change in the plasma PGF in the PN animals on any of these days or on days 23 and 24. SNK analysis showed increased PGF (P < 0.05) on day 22 in the S animals. But UOV PGE did not change in the PN or S groups. The density and intensity of ovarian 20α-HSD reaction product was low in both S and PN rats on days 20 and 21. Increased density and intensity of ovarian 20α-HSD reaction product was characteristic of five animals on day 22 and PN rats on days 22, 23 and 24. Collectively, these results indicate that the pelvic nerves participate in the orchestration of endocrine and uterine events in the pre-parturient and parturient periods in the rat.
14 citations