Enzymes of the oxidoreductase class that catalyze the dehydrogenation of hydroxysteroids. (From Enzyme Nomenclature, 1992) EC 1.1.-.
A low-affinity 11 beta-hydroxysteroid dehydrogenase found in a variety of tissues, most notably in LIVER; LUNG; ADIPOSE TISSUE; vascular tissue; OVARY; and the CENTRAL NERVOUS SYSTEM. The enzyme acts reversibly and can use either NAD or NADP as cofactors.
An high-affinity, NAD-dependent 11-beta-hydroxysteroid dehydrogenase that acts unidirectionally to catalyze the dehydrogenation of CORTISOL to CORTISONE. It is found predominantly in mineralocorticoid target tissues such as the KIDNEY; COLON; SWEAT GLANDS; and the PLACENTA. Absence of the enzyme leads to a fatal form of childhood hypertension termed, APPARENT MINERALOCORTICOID EXCESS SYNDROME.
A class of enzymes that catalyzes the oxidation of 17-hydroxysteroids to 17-ketosteroids. EC 1.1.-.
Catalyze the oxidation of 3-hydroxysteroids to 3-ketosteroids.
Hydroxysteroid dehydrogenases that catalyzes the reversible conversion of CORTISOL to the inactive metabolite CORTISONE. Enzymes in this class can utilize either NAD or NADP as cofactors.
A group of enzymes that catalyze the reversible reduction-oxidation reaction of 20-hydroxysteroids, such as from a 20-ketosteroid to a 20-alpha-hydroxysteroid (EC 1.1.1.149) or to a 20-beta-hydroxysteroid (EC 1.1.1.53).
A microsomal cytochrome P450 enzyme that catalyzes the 17-alpha-hydroxylation of progesterone or pregnenolone and subsequent cleavage of the residual two carbons at C17 in the presence of molecular oxygen and NADPH-FERRIHEMOPROTEIN REDUCTASE. This enzyme, encoded by CYP17 gene, generates precursors for glucocorticoid, androgen, and estrogen synthesis. Defects in CYP17 gene cause congenital adrenal hyperplasia (ADRENAL HYPERPLASIA, CONGENITAL) and abnormal sexual differentiation.
A 3-hydroxysteroid dehydrogenase which catalyzes the reversible reduction of the active androgen, DIHYDROTESTOSTERONE to 5 ALPHA-ANDROSTANE-3 ALPHA,17 BETA-DIOL. It also has activity towards other 3-alpha-hydroxysteroids and on 9-, 11- and 15- hydroxyprostaglandins. The enzyme is B-specific in reference to the orientation of reduced NAD or NADPH.
The main glucocorticoid secreted by the ADRENAL CORTEX. Its synthetic counterpart is used, either as an injection or topically, in the treatment of inflammation, allergy, collagen diseases, asthma, adrenocortical deficiency, shock, and some neoplastic conditions.
Enzymes that catalyze the oxidation of estradiol at the 17-hydroxyl group in the presence of NAD+ or NADP+ to yield estrone and NADH or NADPH. The 17-hydroxyl group can be in the alpha- or beta-configuration. EC 1.1.1.62
A naturally occurring glucocorticoid. It has been used in replacement therapy for adrenal insufficiency and as an anti-inflammatory agent. Cortisone itself is inactive. It is converted in the liver to the active metabolite HYDROCORTISONE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p726)
Enzymes which transfer sulfate groups to various acceptor molecules. They are involved in posttranslational sulfation of proteins and sulfate conjugation of exogenous chemicals and bile acids. EC 2.8.2.
A subclass of enzymes which includes all dehydrogenases acting on primary and secondary alcohols as well as hemiacetals. They are further classified according to the acceptor which can be NAD+ or NADP+ (subclass 1.1.1), cytochrome (1.1.2), oxygen (1.1.3), quinone (1.1.5), or another acceptor (1.1.99).
A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)
A coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage. It is found widely in nature and is involved in numerous enzymatic reactions in which it serves as an electron carrier by being alternately oxidized (NAD+) and reduced (NADH). (Dorland, 27th ed)
Reversibly catalyze the oxidation of a hydroxyl group of carbohydrates to form a keto sugar, aldehyde or lactone. Any acceptor except molecular oxygen is permitted. Includes EC 1.1.1.; EC 1.1.2.; and 1.1.99.
The rate dynamics in chemical or physical systems.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.
A tetrameric enzyme that, along with the coenzyme NAD+, catalyzes the interconversion of LACTATE and PYRUVATE. In vertebrates, genes for three different subunits (LDH-A, LDH-B and LDH-C) exist.
A metabolite of TESTOSTERONE or ANDROSTENEDIONE with a 3-alpha-hydroxyl group and without the double bond. The 3-beta hydroxyl isomer is epiandrosterone.
A zinc-containing enzyme which oxidizes primary and secondary alcohols or hemiacetals in the presence of NAD. In alcoholic fermentation, it catalyzes the final step of reducing an aldehyde to an alcohol in the presence of NADH and hydrogen.
An enzyme that oxidizes an aldehyde in the presence of NAD+ and water to an acid and NADH. This enzyme was formerly classified as EC 1.1.1.70.
Enzymes that catalyze the dehydrogenation of GLYCERALDEHYDE 3-PHOSPHATE. Several types of glyceraldehyde-3-phosphate-dehydrogenase exist including phosphorylating and non-phosphorylating varieties and ones that transfer hydrogen to NADP and ones that transfer hydrogen to NAD.
An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.
Cytoplasmic proteins that specifically bind MINERALOCORTICOIDS and mediate their cellular effects. The receptor with its bound ligand acts in the nucleus to induce transcription of specific segments of DNA.
An enzymes that catalyzes the reversible reduction-oxidation reaction of 20-alpha-hydroxysteroids, such as from PROGESTERONE to 20-ALPHA-DIHYDROPROGESTERONE.
An enzyme that catalyzes the dehydrogenation of inosine 5'-phosphate to xanthosine 5'-phosphate in the presence of NAD. EC 1.1.1.205.

High dietary potassium chloride intake augments rat renal mineralocorticoid receptor selectivity via 11beta-hydroxysteroid dehydrogenase. (1/271)

Glucocorticoid access to renal corticosteroid receptors is regulated by 11beta-hydroxysteroid dehydrogenases (11beta-HSDs), converting 11beta-hydroxyglucocorticoids into inactive 11-ketones. This mechanism plays a key role in maintaining normal salt-water homeostasis and blood pressure. To study whether renal cortical proximal and distal tubular 11beta-HSDs are modulated, upon shifting the electrolyte status (and may thereby contribute to adjusting the salt-water homeostasis), rats were treated for 14 days with diets with low (0.058 w/w%), normal (0.58%, which is the KCl content of standard European laboratory rat food) or high (5.8%) potassium chloride content. In proximal tubules, dietary KCl had no effect regarding corticosterone 11beta-oxidation in intact cells as well as 11beta-HSD1 and 11beta-HSD2 protein (Western blotting) and mRNA levels (semi-quantitative RT-PCR). In distal tubules, the low KCl diet also had no effect. However, distal tubules of rats fed the high KCl diet showed increased corticosterone 11beta-oxidation rates (1.6-fold, P<0.01) and 11beta-HSD2 protein (4-fold, P<0.01), whereas 11beta-HSD1 protein was decreased (no longer detected, P<0.05). Distal tubular 11beta-HSD mRNA levels were not changed upon dietary treatment. Our results suggest that upon dietary KCl loading distal tubular mineralocorticoid receptor selectivity for aldosterone is increased because of enhanced corticosterone 11beta-oxidation. This may contribute to the fine-tuning of salt-water homeostasis by the kidney.  (+info)

Full induction of rat myometrial 11beta-hydroxysteroid dehydrogenase type 1 in late pregnancy is dependent on intrauterine occupancy. (2/271)

The 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1) enzyme catalyses the conversion of the biologically inert glucocorticoid 11-dehydrocorticosterone to active corticosterone (11-oxoreductase activity) in vivo, and it is dramatically up-regulated in uterine myometrium in the days leading up to parturition. 11beta-HSD-1 is likely to enhance local concentrations of glucocorticoid within the myometrium and thus facilitate uterine contractility, but the stimulus for the increase in myometrial 11beta-HSD-1 is unknown. The objective of the present study was to test whether the induction of myometrial 11beta-HSD-1 is dependent on uterine occupancy or systemic hormonal signals of late pregnancy. This involved use of a unilateral pregnancy (ULP) model in which the gravid and nongravid uterine horns are both exposed to the normal systemic hormonal milieu of pregnancy. Western blot analysis showed that the 11beta-HSD-1 signal was only partially induced in the nongravid horn of ULP rats on Day 22 of pregnancy (term: Day 23). Moreover, artificial distension of this nongravid horn had no effect on myometrial 11beta-HSD-1 immunoreactivity or bioactivity at either Day 16 or Day 22 of pregnancy. Removal of fetuses and placentas on Day 18 reduced myometrial 11beta-HSD-1 bioactivity 4 days later, and this effect was not overcome by artificial maintenance of uterine distension. In contrast, after fetectomy at Day 18 (i.e., removal of the fetus but not placenta), myometrial 11beta-HSD-1 bioactivity was largely maintained on Day 22, indicative of placental support for myometrial 11beta-HSD-1 over this period. In conclusion, our data show that full induction of myometrial 11beta-HSD-1 expression and associated 11-oxoreductase bioactivity late in rat pregnancy is dependent upon intrauterine occupancy. Although the hormonal milieu of late pregnancy appears to stimulate myometrial 11beta-HSD-1 marginally, full induction clearly requires an additional stimulus. Manipulations involving fetectomy and artificial uterine distension indicate that the placenta provides at least part of this stimulus, but uterine stretch does not appear to play a role.  (+info)

Role of 11beta-hydroxysteroid dehydrogenase in nongenomic aldosterone effects in human arteries. (3/271)

The aim of the present study was to demonstrate rapid effects of aldosterone on the Na(+)-H(+) exchanger in strips of human vascular vessels and to determine whether 11beta-hydroxysteroid dehydrogenase enzyme (11beta-HSD) could play a protective role in this response, such as that described for the classic type I mineralocorticoid receptor (MR). The activity of 11beta-HSD isoforms 1 and 2 were measured in fetal and adult arteries. Both isoforms are present in adult and fetal vessels. However, a significant difference in the proportion of each isoform was found. Isoform 1 activity (in pmol x min(-1) x 100 mg(-1) protein) was 42+/-5 in fetal vessels and 29+/-2 in adult arteries, and isoform 2 activity was 78+/-7 in fetal and 12+/-2 in adult tissue. The nongenomic effect of aldosterone on Na(+)-H(+) exchanger activity was measured in strips of chorionic and radial uterine arteries loaded with the pH-sensitive dye 2',7'-bis(2-carboxyethyl)-5,6-carboxyfluorescein. Recordings of intracellular pH (pH(i)) were made by videofluorescence microscopy. Aldosterone (0.5 nmol/L) rapidly increased pH(i), with a half-maximal effect between 2 and 3 nmol/L in both fetal and adult vessels. Ethylisopropylamiloride, a specific inhibitor of the Na(+)-H(+) exchanger, inhibited this effect. The hormone-mediated increase in pH(i) was unaffected by spironolactone, a classic antagonist of MR, but was completely blocked by RU28318. Cortisol (up to 1 micromol/L) had no effect on pH(i), but when applied in the presence of carbenoxolone, a dramatic increase in Na(+)-H(+) exchanger activity was evident. The increments on pH(i) for each cortisol concentration were similar to those observed for aldosterone. These findings suggest that vascular 11beta-HSD plays an active role in maintaining the specificity of the rapid effects of aldosterone.  (+info)

Novel nuclear corticosteroid binding in rat small intestinal epithelia. (4/271)

When small intestinal epithelial cells are incubated with [(3)H]corticosterone, nuclear binding is displaced neither by aldosterone nor RU-28362, suggesting that [(3)H]corticosterone is binding to a site distinct from mineralocorticoid receptor and glucocorticoid receptor. Saturation and Scatchard analysis of nuclear [(3)H]corticosterone binding demonstrate a single saturable binding site with a relatively low affinity (49 nM) and high capacity (5 fmol/microg DNA). Competitive binding assays indicate that this site has a unique steroid binding specificity, which distinguishes it from other steroid receptors. Steroid specificity of nuclear binding mirrors inhibition of the low 11beta-dehydrogenase activity, suggesting that binding may be to an 11beta-hydroxysteroid dehydrogenase (11betaHSD) isoform, although 11betaHSD1 is not present in small intestinal epithelia and 11betaHSD2 does not colocalize intracellularly with the binding site. In summary, a nuclear [(3)H]corticosterone binding site is present in small intestinal epithelia that is distinct from other steroid receptors and shares steroid specificity characteristics with 11betaHSD2 but is distinguishable from the latter by its distinct intracellular localization.  (+info)

Peroxisome proliferator-activated receptor-gamma ligands inhibit adipocyte 11beta -hydroxysteroid dehydrogenase type 1 expression and activity. (5/271)

Peroxisome proliferator-activated receptor-gamma (PPARgamma) has been shown to play an important role in the regulation of expression of a subclass of adipocyte genes and to serve as the molecular target of the thiazolidinedione (TZD) and certain non-TZD antidiabetic agents. Hypercorticosteroidism leads to insulin resistance, a variety of metabolic dysfunctions typically seen in diabetes, and hypertrophy of visceral adipose tissue. In adipocytes, the enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1) converts inactive cortisone into the active glucocorticoid cortisol and thereby plays an important role in regulating the actions of corticosteroids in adipose tissue. Here, we show that both TZD and non-TZD PPARgamma agonists markedly reduced 11beta-HSD-1 gene expression in 3T3-L1 adipocytes. This diminution correlated with a significant decrease in the ability of the adipocytes to convert cortisone to cortisol. The half-maximal inhibition of 11beta-HSD-1 mRNA expression by the TZD, rosiglitazone, occurred at a concentration that was similar to its K(d) for binding PPARgamma and EC(50) for inducing adipocyte differentiation thereby indicating that this action was PPARgamma-dependent. The time required for the inhibitory action of the TZD was markedly greater for 11beta-HSD-1 gene expression than for leptin, suggesting that these genes may be down-regulated by different molecular mechanisms. Furthermore, whereas regulation of PPARgamma-inducible genes such as phosphoenolpyruvate carboxykinase was maintained when cellular protein synthesis was abrogated, PPARgamma agonist inhibition of 11beta-HSD-1 and leptin gene expression was ablated, thereby supporting the conclusion that PPARgamma affects the down-regulation of 11beta-HSD-1 indirectly. Finally, treatment of diabetic db/db mice with rosiglitazone inhibited expression of 11beta-HSD-1 in adipose tissue. This decrease in enzyme expression correlated with a significant decline in plasma corticosterone levels. In sum, these data indicate that some of the beneficial effects of PPARgamma antidiabetic agents may result, at least in part, from the down-regulation of 11beta-HSD-1 expression in adipose tissue.  (+info)

Functional expression, characterization, and purification of the catalytic domain of human 11-beta -hydroxysteroid dehydrogenase type 1. (6/271)

11-beta-hydroxysteroid dehydrogenase type 1 catalyzes the conversion of cortisone to hormonally active cortisol and has been implicated in the pathogenesis of a number of disorders including insulin resistance and obesity. The enzyme is a glycosylated membrane-bound protein that has proved difficult to purify in an active state. Extracted enzyme typically loses the reductase properties seen in intact cells and shows principally dehydrogenase activity. The C-terminal catalytic domain is known to contain a disulfide bond and is located within the lumen of the endoplasmic reticulum, anchored to the membrane by a single N-terminal transmembrane domain. We report here the functional expression of the catalytic domain of the human enzyme, without the transmembrane domain and the extreme N terminus, in Escherichia coli. Moderate levels of soluble active protein were obtained using an N-terminal fusion with thioredoxin and a 6xHis tag. In contrast, the inclusion of a 6xHis tag at the C terminus adversely affected protein solubility and activity. However, the highest levels of active protein were obtained using a construct expressing the untagged catalytic domain. Nonreducing electrophoresis revealed the presence of both monomeric and dimeric disulfide bonded forms; however, mutation of a nonconserved cysteine residue resulted in a recombinant protein with no intermolecular disulfide bonds but full enzymatic activity. Using the optimal combination of plasmid construct and E. coli host strain, the recombinant protein was purified to apparent homogeneity by single step affinity chromatography. The purified protein possessed both dehydrogenase and reductase activities with a K(m) of 1.4 micrometer for cortisol and 9.5 micrometer for cortisone. This study indicates that glycosylation, the N-terminal region including the transmembrane helix, and intermolecular disulfide bonds are not essential for enzyme activity and that expression in bacteria can provide active recombinant protein for future structural and functional studies.  (+info)

A transgenic model of visceral obesity and the metabolic syndrome. (7/271)

The adverse metabolic consequences of obesity are best predicted by the quantity of visceral fat. Excess glucocorticoids produce visceral obesity and diabetes, but circulating glucocorticoid levels are normal in typical obesity. Glucocorticoids can be produced locally from inactive 11-keto forms through the enzyme 11beta hydroxysteroid dehydrogenase type 1 (11beta HSD-1). We created transgenic mice overexpressing 11beta HSD-1 selectively in adipose tissue to an extent similar to that found in adipose tissue from obese humans. These mice had increased adipose levels of corticosterone and developed visceral obesity that was exaggerated by a high-fat diet. The mice also exhibited pronounced insulin-resistant diabetes, hyperlipidemia, and, surprisingly, hyperphagia despite hyperleptinemia. Increased adipocyte 11beta HSD-1 activity may be a common molecular etiology for visceral obesity and the metabolic syndrome.  (+info)

Correlation between decrease of 11beta-hydroxysteroid dehydrogenase activity and hypokalemia induced by furosemide in rats. (8/271)

AIM: To investigate the correlation between decrease of 11beta-hydroxysteroid dehydrogenase (11beta-HSD) activity and hypokalemia induced by furosemide (Fur) in rats. METHODS: SD rats were given single dose or successive doses of Fur by gavage. The activity of 11beta-HSD was evaluated by measuring the ratio of 11-dehydrocorticosterone (A) and corticosterone (B) in urine and conversion rate of B to A in renal cortex microsome preparation was determined with HPLC. RESULTS: After giving single dose of Fur (40, 100, and 250 mg/kg) or multiple doses of Fur (10, 20, and 100 mg/kg, bid x 20 d), the ratio of A/B was reduced by 29.0 %, 58.6 %, and 60.9 % at 0 - 2 h; 14.4 %, 36.0 %, and 44.9 %, respectively; the conversion rate of B to A was decreased by 29 %, 33 %, and 37 %; 6 %, 17 %, and 23 %, respectively. The serum potassium was significantly reduced by multiple doses of Fur (20 and 100 mg/kg, bid x 20 d) (P < 0.01). The reduction in serum potassium was positively correlated with the lowering of A/B ratio and the conversion of B to A (P < 0.01). CONCLUSION: The inhibition of renal 11beta-HSD activity may be another new biochemical mechanism for hypokalemia induced by Fur.  (+info)

TY - JOUR. T1 - 11 beta-hydroxysteroid dehydrogenase type 2 in mouse aorta - Localization and influence on response to glucocorticoids. AU - Christy, C AU - Hadoke, P W F AU - Paterson, J M AU - Mullins, J J AU - Seckl, J R AU - Walker, B R PY - 2003/10. Y1 - 2003/10. N2 - Both isozymes of 11 beta-hydroxysteroid dehydrogenase, which interconvert active and inactive glucocorticoids, are expressed in the mouse aortic wall. Mice deficient in 11HSD type 2 ( which converts active corticosterone into inert 11-dehydrocorticosterone) have hypertension and impaired endothelial nitric oxide activity. It has been suggested that 11HSD2 influences vascular function directly by limiting glucocorticoid-mediated inhibition of endothelium-derived nitric oxide. This study sought to determine (1) the cellular distribution of the 11HSD isozymes within the mouse aortic wall and (2) the influence of 11HSD2 on direct glucocorticoid-mediated changes in aortic function. Mouse aortas were separated into their component ...
The global epidemic of obesity has heightened the need to understand the mechanisms that underpin its pathogenesis. Clinical observations in patients with Cushings syndrome have highlighted the link between cortisol and central obesity. However, although circulating cortisol levels are normal or reduced in obesity, local regeneration of cortisol, from inactive cortisone, by 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) has been postulated as a pathogenic mechanism. Although levels of expression of 11betaHSD1 in adipose tissue in human obesity are debated in the literature, global inhibition of 11betaHSD1 improves insulin sensitivity. We have determined the effects of significant weight loss on cortisol metabolism and adipose tissue 11betaHSD1 expression after 10-wk ingestion of a very low calorie diet in 12 obese patients (six men and six women; body mass index, 35.9 +/- 0.9 kg/m2; mean +/- SE). All patients achieved significant weight loss (14.1 +/- 1.3% of initial body weight). Total fat
KEE316Hu, HSD11b1L; SCDR10; HSD3; SDR26C2; 11-Beta Hydroxysteroid Dehydrogenase Type 1 Like Protein; Short chain dehydrogenase/reductase family 26C member 2 | Products for research use only!
4FAL: Crystal structure of human 17beta-hydroxysteroid dehydrogenase type 5 in complex with 3-((3,4-dihydroisoquinolin-2(1H)-yl)sulfonyl)-N-methylbenzamide (80)
Glucocorticoids are important regulators of glucose, lipid and protein metabolism, acting mainly in the liver, adipose tissue and muscle. Chronic glucocorticoid excess is associated with clinical features, such as insulin resistance, visceral obesity, hypertension, and dyslipidemia, which also represent the classical hallmarks of the metabolic syndrome. Elevenbeta-hydroxysteroid dehydrogenase type 1 (11beta-HSD-1), a key intracellular enzyme which catalyses the conversion of inactive cortisone to active cortisol, has been implicated in the development of the metabolic syndrome. The shift of this reaction towards cortisol generation may lead to tissutal overexposure to glucocorticoids even with normal circulating cortisol levels. The most robust evidence in support of a pathogenetic role of this enzyme in the development of the metabolic syndrome has been reported in experimental animals, whereas results of human studies are less convincing with several case control and cross-sectional studies ...
Local brain amplification of glucocorticoids (GCs) by 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) plays a pivotal role in age-related memory deficits. 11β-HSD1 deficient mice are protected from...
The enzyme 11 beta-hydroxysteroid dehydrogenase (11 beta HSD) is thought to protect the non-selective mineralocorticoid receptor from occupation by glucocorticoids, and to modulate access of glucocorticoids to glucocorticoid receptors resulting in protection of the fetus and gonads. A ubiquitous low …
|i|Background|/i|. Glucocorticoid excess has been linked to clinical observations associated with the pathophysiology of metabolic syndrome. The intracellular glucocorticoid levels are primarily modulated by 11|i|β|/i|-hydroxysteroid dehydrogenase type 1 (11|i|β|/i|-HSD1) enzyme that is highly expressed in key metabolic tissues including fat, liver, and the central nervous system.|i| Methods|/i|. In this study we synthesized a set of novel tetrahydrothiazolopyridine derivatives, TR-01–4, that specifically target 11|i|β|/i|-HSD1 and studied their ability to interfere with the glucocorticoid and lipid metabolism in the 3T3-L1 adipocytes.|i| Results|/i|. Based on the docking model and structure-activity relationships, tetrahydrothiazolopyridine derivatives TR-02 and TR-04 showed the highest potency against 11|i|β|/i|-HSD1 by dose-dependently inhibiting conversion of cortisone to cortisol (IC|sub|50|/sub| values of 1.8 |i|μ|/i|M and 0.095 |i|μ|/i|M,
Q9EQC1: 3 beta-hydroxysteroid dehydrogenase type 7; 3 beta-hydroxysteroid dehydrogenase type VII; 3-beta-HSD VII; 3-beta-hydroxy-Delta(5)-C27 steroid oxidoreductase; C(27) 3-beta-HSD; 1.1.1.-; Cholest-5-ene-3-beta,7-alpha-diol 3-beta-dehydrogenase; 1.1. ...
Human 17beta-hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a steroid-converting enzyme that has long been known to play critical roles in estradiol synthesis and more recently in dihydrotestosterone (DHT) inactivation, showing a dual function that promotes breast cancer cell proliferation. Previously, we reported the first observation of the influence of the enzyme on endogenous estrogen-responsive gene expression. Here, we demonstrate the impact of 17β-HSD1 expression on the breast cancer cell proteome and investigate its role in cell migration. 17β-HSD1 was stably transfected in MCF7 cells and the proteome of the generated cells overexpressing 17β-HSD1 (MCF7-17βHSD1 cells) was compared to that of the wild type MCF7 cells. Proteomics study was performed using two-dimensional gel electrophoresis followed by mass spectrometry analysis of differentially expressed protein spots. Reverse transcription quantitative real-time PCR (RT-qPCR) was used to investigate the transcription of individual gene.
4FAL: 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic acids; a New Class of Highly Potent and Selective Inhibitors of the Type 5 17-beta-hydroxysteroid Dehydrogenase AKR1C3
17beta-hydroxysteroid dehydrogenase type12 (HSD17B12) has been demonstrated to be involved in regulation of in situ biosynthesis of estradiol (E2). HSD17B12 expression was reported in breast carcinomas but its functions have remained unknown. Therefore, we examined the correlation between mRNA expression profiles determined by microarray analysis and tissue E2 concentrations obtained from 16 postmenopausal breast carcinoma cases in order to analyze an association of the enzyme expression with intratumoral E2 production. No significant correlations were detected between intratumoral HSD17B12expression and E2 concentration.These findings suggest that the presence of HSD17B12 in carcinoma cells contributes to a development of human breast carcinoma via a pathway other than in situ E2 biosynthesis.
Expression in E. coli and tissue distribution of the human homologue of the mouse Ke 6 gene, 17beta-hydroxysteroid dehydrogenase type 8 ...
The relationship between stress, cortisol and an increase in body fat has been well established. However, new research has identified a little known enzyme deep within fat cells called 11 beta-hydroxysteroid dehydrogenase-1 or HSD. The HSD enzyme converts the inactive form of cortisol (called cortisone) into the active, fat storing form called cortisol.. Researchers in Germany noted that the rate of activity of the HSD enzyme determines the rate of fat storage in the individual. When individuals were experiencing high levels of HSD activity, no amount of exercise, diet or stress management are able to prevent fat gain.. The activity of the HSD enzyme increases with age. Women and men in their thirties and forties can experience as much a 300% increase in HSD activity compared to an individual in their twenties. This may account to for steady increase in stubborn body fat observed in individuals as they age.. ...
Journal Article: On-column ligand exchange for structure-based drug design: a case study with human 11[beta]-hydroxysteroid dehydrogenase type 1 ...
The enzyme 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2) is selectively expressed in aldosterone target tissues, conferring aldosterone selectivity for the mineralocorticoid receptor. A diminished activity causes salt-sensitive hypertension. The mechanism of the variable and distinct 11β-hydroxysteroid dehydrogenase type 2 gene (HSD11B2) expression in the cortical collecting duct is poorly understood. Here, we analyzed for the first time whether the 11β-HSD2 expression is modulated by microRNAs (miRNAs). In silico analysis revealed 53 and 27 miRNAs with potential binding sites on human or rat HSD11B2 3′-untranslated region. A reporter assay demonstrated 3′-untranslated region-dependent regulation of human and rodent HSD11B2. miRNAs were profiled from cortical collecting ducts and proximal convoluted tubules. Bioinformatic analyses showed a distinct clustering for cortical collecting ducts and proximal convoluted tubules with 53 of 375 miRNAs, where 13 were predicted to bind to the ...
11 beta-hydroxysteroid dehydrogenase (11 beta HSD) has both dehydrogenase (11 beta DH) and reductase (11 beta R) activities, which catalyse the interconversion of cortisol and cortisone, and prednisolone and prednisone. This enzyme confers specificity
11ß-hydroxysteroid dehydrogenase type1 (11β-HSD1) converts inactive glucocorticoids to active glucocorticoids which, in excess, leads to development of the various risk factors of the metabolic syndrome. Recent studies clearly suggest that both increased expression and activity of 11β-HSD1 in metabolically active tissues such as liver, muscle and adipose are implicated in tissue specific dysregulation which collectively contribute to the whole body pathology seen in metabolic syndrome. In the present study we have evaluated CNX-010-49, a highly potent, selective and pan tissue acting 11β-HSD1 inhibitor, for its potential to modulate multiple risk factors of the metabolic syndrome. Male C57B6/J mice on high fat diet (DIO mice) were orally dosed with CNX-010-49 (30 mg/kg twice daily; n = 8) or vehicle for 10 weeks. Fasting glucose, triglycerides, glycerol, free fatty acids, body weight and feed intake were measured at selected time points. At the end of the treatment an OGTT and subsequently organ
Similar phenotypes in 46,XY DSD have different etiopathogenesis. Androgen (A) synthesis are rare respect to A action/metabolism defects. The most frequent cause in the former group is a mutation of HSD17B3, gene encoding for an enzyme (17BHSD3) converting delta4-androstenedione (D4) into testosterone (T). Homozygotes/compound heterozygotes have testes, male wolffian structures, completely female (F) or mildly virilized external genitalia (EG). Pts with not palpable testes may appear as F, but they virilize at puberty for the increase in serum T. Our patient (12-yrs-old. 46,XY) for FEG at birth was raised as girl until puberty, when clitoris enlargement (, 4 cm) and male pattern of body hair and timbre of voice appeared. The EG corresponded to Prader stage III. Pelvic echography: two hypoechogenic ovoid masses in inguinal regions, compatible with testes, no Müllerian structures, echogenic structure (20x5mm) like hypoplastic uterus, posteriorly to the bladder. T synthesis: reduced before (3.3 ...
Bile acids (BAs) are important modulators of metabolic functions such as lipid, triglyceride and glucose homeostasis. Intrahepatic accumulation of BAs is known to cause liver injury in cholestatic conditions, where normal trans-hepatic BA flow is impaired due to pathological conditions or induced by toxic drugs. Therefore, it is important to understand the mechanisms of BA homeostasis regulation and to identify novel players and characterize their functions. The main goal of the present work was to investigate the impact of altered hepatic glucocorticoid activation by the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) on BA homeostasis and to unravel the mechanisms of adaptations in a scenario of impaired 11β-HSD1 function. In order to achieve this goal, we developed and validated an ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for the quantification of a total of 24 BAs, including 11 unconjugated, 6 glycine-conjugated and 7 ...
Status of 17β-hydroxysteroid dehydrogenase type 2 (17βHSD2) immunoreactivity was significantly higher in invasive lobular carcinoma (ILC) than in invasive duc
TY - JOUR. T1 - The NGFI-B family of transcription factors regulates expression of 3β-hydroxysteroid dehydrogenase type 2 in the human ovary. AU - Havelock, Jon C.. AU - Smith, Allison L.. AU - Seely, Jeremiah B.. AU - Dooley, Christina A.. AU - Rodgers, Raymond J.. AU - Rainey, William E.. AU - Carr, Bruce R.. N1 - Funding Information: The authors would like to thank Bobbie Mayhew for her technical support. This work was supported by National Institutes of Health grant T32-HD007190 (BRC).. PY - 2005/2. Y1 - 2005/2. N2 - The nerve growth factor-induced clone B (NGFI-B) family of transcription factors are orphan members of the steroid hormone receptor superfamily. The NGFI-B expression was recently shown in the rat ovarian tissue and appears to be regulated by gonadotrophins. The purpose of our study was to investigate the role of the three members of this family [NGFI-B, Nur-related factor 1 (NURR1) and neuron derived orphan receptor 1 (NOR-1)] in the transcription of genes that encode key ...
The biological activity of steroid hormones is regulated at the pre-receptor level by several enzymes including 17 beta-hydroxysteroid dehydrogenases (17 beta -HSD). The latter are present in many microorganisms, invertebrates and vertebrates. Dysfunctions in human 17 beta-hydroxysteroid dehydrogenases result in disorders of biology of reproduction and neuronal diseases, the enzymes are also involved in the pathogenesis of various cancers. 17 beta-hydroxysteroid dehydrogenases reveal a remarkable multifunctionality being able to modulate concentrations not only of steroids but as well of fatty and bile acids. Current knowledge on genetics, biochemistry and medical implications is presented in this review.
17 beta-hydroxysteroid dehydrogenases catalyze the oxidoreduction of hydroxy/oxo groups at position C17 of steroid hormones, thereby constituting a prereceptor control mechanism of hormone action. At present, 11 different mammalian 17 beta-hydroxysteroid dehydrogenases have been identified, catalyzing the cell- and steroid-specific activation and inactivation of estrogens and androgens. The human type 10 17 beta-hydroxysteroid dehydrogenase (17 beta-HSD-10) is a multifunctional mitochondrial enzyme that efficiently catalyzes the oxidative inactivation at C17 of androgens and estrogens. However, it also mediates oxidation of 3 alpha-hydroxy groups of androgens, thereby reactivating androgen metabolites. Finally, it is involved in beta-oxidation of fatty acids by catalyzing the L-hydroxyacyl CoA dehydrogenase reaction of the beta-oxidation cycle. These features and expression profiles suggest a critical role of 17 beta-HSD-10 in neurodegenerative and steroid-dependent cancer forms. Since no three
TY - JOUR. T1 - Increased in vivo regeneration of cortisol in adipose tissue in human obesity and effects of the 11beta-hydroxysteroid dehydrogenase type 1 inhibitor carbenoxolone. AU - Sandeep, Thekkepat C. AU - Andrew, Ruth. AU - Homer, Natalie Z M. AU - Andrews, Robert C. AU - Smith, Ken. AU - Walker, Brian R. PY - 2005. Y1 - 2005. N2 - 11beta-Hydroxysteroid dehydrogenase type 1 (11HSD1) regenerates cortisol from cortisone within adipose tissue and liver. 11HSD1 inhibitors may enhance insulin sensitivity in type 2 diabetes and be most efficacious in obesity when 11HSD1 is increased in subcutaneous adipose biopsies. We examined the regeneration of cortisol in vivo in obesity, and the effects of the 11HSD1 inhibitor carbenoxolone. We compared six lean and six obese men and performed a randomized, placebo-controlled crossover study of carbenoxolone in obese men. The obese men had no difference in their whole-body rate of regenerating cortisol (measured with 9,11,12,12-[(2)H(4)]cortisol tracer), ...
Clinical observations have highlighted the link between glucocorticoids and obesity. While exogenous glucocorticoids in excess predispose to the development of central obesity, we have focused on cortisol metabolism within human adipose tissue. 11beta-hydroxysteroid dehydrogenase (11beta-HSD) inter-converts the active glucocorticoid, cortisol, and inactive cortisone. 11beta-HSD1, the only isoform expressed in adipose tissue, acts predominantly as an oxoreductase to generate cortisol. Expression is higher in omental compared to subcutaneous preadipocytes and activity and expression are potently regulated by growth factors and cytokines. Mice over-expressing 11beta-HSD1 specifically within adipocytes develop central obesity. However, the situation is less clear in humans. Globally, there appears to be inhibition of the enzyme, but expression in human obesity is still not fully characterized; its functional role in adipocyte biology remains to be elucidated. In vitro, 11beta-HSD1 appears to function in
Clinical observations have highlighted the link between glucocorticoids and obesity. While exogenous glucocorticoids in excess predispose to the development of central obesity, we have focused on cortisol metabolism within human adipose tissue. 11beta-hydroxysteroid dehydrogenase (11beta-HSD) inter-converts the active glucocorticoid, cortisol, and inactive cortisone. 11beta-HSD1, the only isoform expressed in adipose tissue, acts predominantly as an oxoreductase to generate cortisol. Expression is higher in omental compared to subcutaneous preadipocytes and activity and expression are potently regulated by growth factors and cytokines. Mice over-expressing 11beta-HSD1 specifically within adipocytes develop central obesity. However, the situation is less clear in humans. Globally, there appears to be inhibition of the enzyme, but expression in human obesity is still not fully characterized; its functional role in adipocyte biology remains to be elucidated. In vitro, 11beta-HSD1 appears to function in
There are increasing data on the central role of miRNAs in the development of various diseases, including some kidney and cardiovascular entities.27,32,33 Whether miRNAs and the 3′-UTR of specific players in the field of renal or blood pressure physiology are relevant is yet to be addressed specifically. The 11β-HSD2 is an essential enzyme for blood pressure control.3 Therefore, the mechanisms accounting for its regulation are a prerequisite for understanding blood pressure in health and disease states. Here, we present evidence that HSD11B2 mRNA fulfills the prerequisites to be modulated by miRNAs. Because a multitude of miRNAs directly or indirectly affect the expression of a protein, special emphasis was given to the miRNA expression profile in the CCD, the main site of 11β-HSD2 action.. To the best of our knowledge, the relationship between miRNA and 11β-HSD2 was reported previously only once.34 Shang et al34 starved a human placental cell line (BeWo) from amino acids and observed a ...
11 beta-Hydroxysteroid dehydrogenase (11 beta HSD) catalyzes the conversion of corticosterone to inert 11-dehydrocorticosterone, thus regulating glucocorticoid access to intracellular receptors. This type 1 isoform (11 beta HSD-1) is a bidirectional NADPH(H)-dependent enzyme in vitro and is highly e …
17Beta-hydroxysteroid dehydrogenases (17beta-HSDs) catalyze the NAD(P)(H) dependent oxidoreduction at C17 oxo/beta-hydroxyl groups of androgen and estrogen hormones. This reversible reaction constitutes an important pre-receptor control mechanism for nuclear receptor ligands, since the conversion switches between the 17beta-OH receptor ligands and their inactive 17-oxo metabolites. At present, 14 mammalian 17beta-HSDs are described, of which at least 11 exist within the human genome, encoded by different genes. The enzymes differ in their expression pattern, nucleotide cofactor preference, steroid substrate specificity and subcellular localization, and thus constitute a complex system ensuring cell-specific adaptation and regulation of sex steroid hormone levels. Broad and overlapping substrate specificities with enzymes involved in lipid metabolism suggest interactions of several 17beta-HSDs with other metabolic pathways. Several 17beta-HSDs enzymes constitute promising drug targets, of particular
17Beta-hydroxysteroid dehydrogenases (17beta-HSDs) catalyze the NAD(P)(H) dependent oxidoreduction at C17 oxo/beta-hydroxyl groups of androgen and estrogen hormones. This reversible reaction constitutes an important pre-receptor control mechanism for nuclear receptor ligands, since the conversion switches between the 17beta-OH receptor ligands and their inactive 17-oxo metabolites. At present, 14 mammalian 17beta-HSDs are described, of which at least 11 exist within the human genome, encoded by different genes. The enzymes differ in their expression pattern, nucleotide cofactor preference, steroid substrate specificity and subcellular localization, and thus constitute a complex system ensuring cell-specific adaptation and regulation of sex steroid hormone levels. Broad and overlapping substrate specificities with enzymes involved in lipid metabolism suggest interactions of several 17beta-HSDs with other metabolic pathways. Several 17beta-HSDs enzymes constitute promising drug targets, of particular
STUDY QUESTION: What are the in vivo and in vitro actions of kisspeptin-54 on the expression of genes involved in ovarian reproductive function, steroidogenesis and ovarian hyperstimulation syndrome (OHSS) in granulosa lutein (GL) cells when compared with traditional triggers of oocyte maturation? SUMMARY ANSWER: The use of kisspeptin-54 as an oocyte maturation trigger augmented expression of genes involved in ovarian steroidogenesis in human GL cells including, FSH receptor (FSHR), LH/hCG receptor (LHCGR), steroid acute regulatory protein (STAR), aromatase, estrogen receptors alpha and beta (ESR1, ESR2), 3-beta-hydroxysteroid dehydrogenase type 2 (3BHSD2) and inhibin A (INHBA), when compared to traditional maturation triggers, but did not alter markers of OHSS ...
An exciting era is upon us in terms of new therapies for patients with diabetes, obesity, and metabolic syndrome. One such advance is the ability to selectively manipulate tissue levels of glucocorticoids through targeted inhibition of cortisol metabolic pathways. Perhaps the best paradigm for metabolic syndrome comes from patients with Cushings syndrome, with their characteristic central obesity, glucose intolerance, hypertension, and premature cardiovascular mortality. Although circulating cortisol concentrations are invariably normal in patients with obesity and metabolic syndrome (1), in vitro, in vivo, and clinical studies over the last decade have collectively shown the importance of local generation of cortisol, via 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) in liver and fat, in mediating many facets of the metabolic syndrome (2). Major pharmaceutical companies are now engaged; over 50 patents have been issued detailing compounds and strategies for selective 11β-HSD1 ...
Rationale Rescuing adverse myocardial redesigning can be an unmet clinical goal and, correspondingly, pharmacological opportinity for its meant reversal are urgently required. cardiac redesigning without influencing the vasculature. Increasing the arsenal of remodeling-reversing medicines to pathways apart from RAAS, a particular inhibitor of 11-hydroxy-steroid dehydrogenase type 1 (11 HSD1), an integral enzyme necessary for producing active glucocorticoids, completely rescued myocardial hypertrophy. This is connected with mitigating the hypertrophy-associated gene personal, including reversing the myosin weighty chain isoform change however in a design distinguishable from that connected with neovascularization-induced reversal. Conclusions Something was developed ideal for determining novel remodeling-reversing medicines operating in various pathways as well as for getting insights to their systems of actions, exemplified right here by uncoupling their vascular impacts. Introduction Cardiac ...
[Inhibitory effect on pig testicular 20 beta-hydroxysteroid dehydrogenase by various inhibitors of steroid metabolizing enzymes].:
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Mutations in HSD3B2, the gene for 3beta-hydroxysteroid dehydrogenase type II (3beta-HSD II) have been detected and activities analysed through the in vitro expression of mutant cDNAs. Two full sibs with male pseudohermaphroditism were found to be double heterozygotes: N100S/266DeltaA. This genotype leads to the most profound loss of 3beta-HSD II enzyme activity (1.3% of normal) described to date in cases without severe salt-loss. One sib (N100S/266DeltaA) is the first reported male case of type II deficiency affected with premature adrenarche. Three apparently independent kindreds had propositi affected with the HSD3B2 mutation A82T/A82T, which is associated with a non salt-losing phenotype with variable expressivity in females. These three families had the same extended HSD3B haplotype and are likely to have inherited the same ancestral mutation. The significance of this finding is discussed in the light of the presence of A82T mutation at a homologous position in pseudogene varphi5 that is ...
Oestrogens play key roles in the development of the majority of breast tumours, a fact that has been exploited successfully in treating breast cancer with tamoxifen, which is a selective oestrogen receptor modulator. In post-menopausal women, oestrogens are synthesised in peripheral hormone-target tissues from adrenally derived precursors. Important in the peripheral fine-tuning of sex hormone levels are the 17β hydroxysteroid dehydrogenases (17βHSDs). These enzymes catalyse the oxidation/reduction of carbon 17β of androgens and oestrogens. Upon receptor binding, the 17β-hydroxy conformation of androgens and oestrogens (testosterone and oestradiol) triggers a greater biological response than the corresponding keto-conformation of the steroids (androstenedione and oestrone), and the 17βHSD enzymes are therefore important mediators in pre-receptor regulation of sex hormone action.. Breast tumours differ substantially with regards to molecular and/or biochemical signatures and thus clinical ...
Carbonyl reduction is a significant step in the biotransformation leading to the elimination, of endogenous and exogenous aldehydes, ketones and quinones. This reaction is mediated by members of the aldo-keto reductase and short-chain dehydrogenase/reductase (SDR) superfamilies. The essential role of these enzymes in protecting organisms from damage by the accumulation of toxic carbonyl compounds is generally accepted, although their physiological roles are not always clear. Recently, the SDR enzyme 11beta-hydroxysteroid dehydrogenase-1 has been identified to perform an important role in the detoxification of non-steroidal carbonyl compounds, in addition to metabolising its physiological glucocorticoid substrates. This review summarises the current knowledge of type-1 11beta-hydroxysteroid dehydrogenase and discusses possible substrate/inhibitor interactions. They might impair either the physiological function of glucocorticoids or the detoxification of non-steroid carbonyl compounds.
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Alterations in glucocorticoid (GC) biosynthesis and metabolism are associated with a variety of pathophysiological disorders including cholestasis, diabetes and other metabolic disorders. Bile acids (BA) are also important modulators of metabolic functions and regulate cholesterol, triglyceride and glucose homeostasis as well as being critical for dietary fat digestion, enterohepatic function, and postprandial thermogenesis. In intact cells and in vivo, the 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme converts inactive GC precursors (cortisone in humans, and 11-dehydrocorticosterone in mice and rats) into their active forms (cortisol and corticosterone, respectively) thereby amplifying local intracellular GC levels. Interconversion by 11β-HSD1 of other sterols has also been described. These include conversions of 7keto-cholesterol to 7β-hydroxycholesterol, 7-oxodehydroepiandrosterone (7-oxo-DHEA) to 7α-hydroxy- and 7β-hydroxy DHEA, 7- oxo-lithocholic acid (LCA, a bile acid; ...
Mutagenetic replacements of conserved residues within the active site of the short-chain dehydrogenase/reductase (SDR) superfamily were studied using prokaryotic 3 beta/17 beta-hydroxysteroid dehydrogenase (3 beta/17 beta-HSD) from Comamonas testosteroni as a model system. The results provide novel data to establish Ser 138 as a member of a catalytically important triad of residues also involving Tyr151 and Lys155. A Ser--|Ala exchange at position 138 results in an almost complete (| 99.9%) loss of enzymatic activity, which is not observed with a Ser--|Thr replacement. This indicates that an essential factor for catalysis is the ability of side chain 138 to form hydrogen bond interactions. Mutations in the NAD(H) binding region, in strands beta A, beta D, and adjacent turns, reveal two additional residues, Thr12 and Asn87, which are important for correct binding of the coenzyme and with a differential effect on the reactions catalyzed. Thus, mutation of Thr12 to Ala results in a complete loss of the 3
Glucocorticoid (GC) excess adversely affects skin integrity, inducing thinning and impaired wound healing. Aged skin, particularly that which has been photo-exposed, shares a similar phenotype. Previously, we demonstrated age-induced expression of the GC-activating enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) in cultured human dermal fibroblasts (HDFs). Here, we determined 11β-HSD1 levels in human skin biopsies from young and older volunteers and examined the aged 11β-HSD1 KO mouse skin phenotype. 11β-HSD1 activity was elevated in aged human and mouse skin and in PE compared with donor-matched photo-protected human biopsies. Age-induced dermal atrophy with deranged collagen structural organization was prevented in 11β-HSD1 KO mice, which also exhibited increased collagen density. We found that treatment of HDFs with physiological concentrations of cortisol inhibited rate-limiting steps in collagen biosynthesis and processing. Furthermore, topical 11β-HSD1 inhibitor treatment ...
Glucocorticoid (GC) excess adversely affects skin integrity, inducing thinning and impaired wound healing. Aged skin, particularly that which has been photo-exposed, shares a similar phenotype. Previously, we demonstrated age-induced expression of the GC-activating enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) in cultured human dermal fibroblasts (HDFs). Here, we determined 11β-HSD1 levels in human skin biopsies from young and older volunteers and examined the aged 11β-HSD1 KO mouse skin phenotype. 11β-HSD1 activity was elevated in aged human and mouse skin and in PE compared with donor-matched photo-protected human biopsies. Age-induced dermal atrophy with deranged collagen structural organization was prevented in 11β-HSD1 KO mice, which also exhibited increased collagen density. We found that treatment of HDFs with physiological concentrations of cortisol inhibited rate-limiting steps in collagen biosynthesis and processing. Furthermore, topical 11β-HSD1 inhibitor treatment ...
BARNARD L. The Biosynthesis of Adrenal C11-Oxy C21 Steroids, Implicated in 21-Hydroxylase Deficiency - Desoxycortisol and Desoxycortisone and Their Downstream Metabolism. MSc, 2017. 105 pp. Studieleier: SWART AC.. BARNARD M. The characterization of 17β-hydroxysteroid dehydrogenase type 2 (17βHSD2) activity towards novel C19 substrates. MSc, 2017. 104 pp. Studieleier: STORBECK K.. BARRY CJ. Modelling the glucocorticoid receptor dimerisation cycle. MSc, 2017. 123 pp. Studieleier: ROHWER JM. Medestudieleier: LOUW A.. BURGER R. Flux balance analysis of Plasmodium falciparum growth and energy metabolism. MSc, 2017. 100 pp. Studieleier: SNOEP JL. Medestudieleier: EICHER JJ.. JOHNSTONE E. Comparative secretome analysis of normal prostate and prostate cancer cell models. MSc, 2017. 134 pp. Studieleier: STORBECK K. Medestudieleier: VLOK NM.. JONKER HI. Evaluation of DNA vaccines against Mycoplasma nasistruthionis sp. nov. str. Ms03 infections in ostriches and the production of IgA heavy chain proteins. ...
Cortisol opposes the activity of anabolic hormones, including testosterone, growth hormone, insulinlike growth factor 1 - a.k.a. IGF-1 - and insulin, although, conversely, the same hormones oppose cortisols catabolic activity. One measure of overtraining is the ratio of testosterone to cortisol - if it tips in favour of cortisol, youve slipped into overtraining. Interestingly, however, one study found that cortisol actually encourages greater activity of free - that is, active - testosterone following exercise by stimulating its release from its protein binder in the blood.1 Another recent study showed that intense training increases cortisol by stimulating the enzyme that converts inactive cortisone into active cortisol.2 Yet another found that, contrary to popular belief, low-intensity exercise not only doesnt increase cortisol but actually lowers it.3 ...
Differentiated OADs for geriatric and post-menopausal population with impact on sarcopenia, visceral adiposity and other metabolic outcomes.. 11HSDβ1 is a member of the short-chain dehydrogenase-reductase family and a key intracellular enzyme which catalyses the conversion of inactive cortisone to active cortisol. Tissue level 11HSDβ1 expression and activity is reported to be high in obese individuals with T2D. Reducing cortisol levels by inhibiting 11HSDβ1 activity in multiple metabolic tissues can provide an important therapeutic handle in these patient populations.. CNX-010-49 is the most advanced candidate from this program fulfilling the TPP of a next generation anti-diabetic, demonstrating significant impact on multiple metabolic parameters without causing HPA activation:. ...
This highly specific HSD17B4 / 17-beta-Hydroxysteroid dehydrogenase 4 antibody is suitable for use in WB, IHC-P and is guaranteed to work as stated on the product data sheet. | R30817
Stort Valley Healthcare, the federation for Stort Valley and Villages practices, continues to thrive in spite of practice pressures. Practices worked together to provide additional appointments for patients in the locality throughout the winter months to help manage the increased demand during this busy period. A new website has been developed which now allows for all the practices and practitioners to have their say and influence decision making at the locality board. An innovative pilot project is taking place to offer testing in practices to see if patients require antibiotics for respiratory tract infections. The federation has also helped develop links with external providers to bring about an improvement in the provision of sexual health services at Herts and Essex Hospital.. ...
"Hexose-6-phosphate dehydrogenase determines the reaction direction of 11beta-hydroxysteroid dehydrogenase type 1 as an ... and 5-beta tetrahydrocortisol (5-beta THF), reactions for which 5-alpha reductase and 5-beta-reductase are the rate-limiting ... The cells do not lose all their fight-or-flight override because of interleukin-1's synergism with CRH. Cortisol even has a ... "11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response". Endocrine Reviews. 25 (5 ...
... beta}-hydroxysteroid dehydrogenase type 1 activity". Endocrinology. 146 (6): 2539-43. doi:10.1210/en.2005-0117. PMID 15774558. ... "Mutations in the genes encoding 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase interact to ... "Mutations in the genes encoding 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase interact to ... "Cortisone-reductase deficiency associated with heterozygous mutations in 11beta-hydroxysteroid dehydrogenase type 1". ...
... possible interference with type 1 11beta-hydroxysteroid dehydrogenase-mediated processes". J. Steroid Biochem. Mol. Biol. 104 ( ... "CYP7B generates a selective estrogen receptor beta agonist in human prostate". J. Clin. Endocrinol. Metab. 89 (6): 2928-35. doi ... 316 (1): 158-64. doi:10.1016/j.bbrc.2004.02.029. PMID 15003524. Yau JL, Rasmuson S, Andrew R, Graham M, Noble J, Olsson T, ... "Entrez Gene: CYP7B1 cytochrome P450, family 7, subfamily B, polypeptide 1". Stapleton G, Steel M, Richardson M, Mason JO, Rose ...
Cooper MS, Stewart PM (2009). "11Beta-hydroxysteroid dehydrogenase type 1 and its role in the hypothalamus-pituitary-adrenal ... p. 1. Quirke, Viviane (2005). "Making British Cortisone: Glaxo and the development of Corticosteroids in Britain in the 1950s- ... 2010-11-16. Retrieved July 31, 2013. "Prednisone and other corticosteroids: Balance the risks and benefits". MayoClinic.com. ... It must be converted to cortisol by the action of 11β-Hydroxysteroid dehydrogenase type 1. This primarily happens in the liver ...
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11beta-hydroxysteroid dehydrogenase type 1- a tissue-specific amplifier of glucocorticoid action". Endocrinology. 142 (4): 1371 ... Seckl JR (January 1997). "11beta-Hydroxysteroid dehydrogenase in the brain: a novel regulator of glucocorticoid action?". Front ... There are two types of 11β-Hydroxysteroid dehydrogenases that control cortisol concentration: HSD-11β Type 1 and HSD-11β Type 2 ... The dehydrogenase activity of a HSD-11β converts a 11beta-hydroxysteroid to the corresponding 11-oxosteroid by reducing NADP+ ...
... beta-hydroxysteroid dehydrogenase isoforms using reverse-transcriptase-polymerase chain reaction and localization of the type 2 ... Wake DJ, Walker BR (February 2006). "Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 in obesity". Endocrine. 29 (1): ... Agarwal AK (November 2003). "Cortisol metabolism and visceral obesity: role of 11beta-hydroxysteroid dehydrogenase type I ... "11beta-Hydroxysteroid dehydrogenase types 1 and 2 are up- and downregulated in cortisol-secreting adrenal adenomas". Journal of ...
3-hydroxysteroid dehydrogenases MeSH D08.811.682.047.436.350.100 - 3alpha-hydroxysteroid dehydrogenase (B-specific) MeSH ... myosin type iii MeSH D08.811.277.040.025.525.843 - myosin type iv MeSH D08.811.277.040.025.525.875 - myosin type v MeSH D08.811 ... dopamine beta-hydroxylase MeSH D08.811.682.690.708.392 - fatty acid desaturases MeSH D08.811.682.690.708.392.312 - beta- ... 20-hydroxysteroid dehydrogenases MeSH D08.811.682.047.436.400.074 - 20alpha-hydroxysteroid dehydrogenase MeSH D08.811.682.047. ...
2003). "Mutations in the genes encoding 11beta-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase ... Ikegwuonu FI, Jefcoate CR (1999). "Evidence for the involvement of the fatty acid and peroxisomal beta-oxidation pathways in ... Beutler E, Morrison M (1968). "Localization and characteristics of hexose 6-phosphate dehydrogenase (glucose dehydrogenase)". J ... "An autosomal glucose-6-phosphate dehydrogenase (hexose-6-phosphate dehydrogenase) polymorphism in human saliva". Hum. Hered. 26 ...
"17 beta-hydroxysteroid dehydrogenase type XI localizes to human steroidogenic cells". Endocrinology. 144 (5): 2084-91. doi: ... "Entrez Gene: HSD17B11 hydroxysteroid (17-beta) dehydrogenase 11". Li KX, Smith RE, Krozowski ZS (1999). "Cloning and expression ... Estradiol 17-beta-dehydrogenase 11 is an enzyme that in humans is encoded by the HSD17B11 gene. GRCh38: Ensembl release 89: ... Haeseleer F, Palczewski K (2000). "Short-chain dehydrogenases/reductases in retina". Methods in Enzymology. 316: 372-83. doi: ...
... the type II 3 beta-hydroxysteroid dehydrogenase gene in a patient with classic salt-wasting 3 beta-hydroxysteroid dehydrogenase ... of type II 3 beta-hydroxysteroid dehydrogenase gene in Japanese patients with classical 3 beta-hydroxysteroid dehydrogenase ... 1992). "Structure of the human type II 3 beta-hydroxysteroid dehydrogenase/delta 5-delta 4 isomerase (3 beta-HSD) gene: adrenal ... 1995). "A novel missense mutation in the type II 3 beta-hydroxysteroid dehydrogenase gene in a family with classical salt- ...
Moghrabi N, Head JR, Andersson S (Nov 1997). "Cell type-specific expression of 17 beta-hydroxysteroid dehydrogenase type 2 in ... Oliveira IO, Lhullier C, Brum IS, Spritzer PM (Sep 2003). "Gene expression of type 2 17 beta hydroxysteroid dehydrogenase in ... 17β-Hydroxysteroid dehydrogenase 2 (17β-HSD2) is an enzyme of the 17β-hydroxysteroid dehydrogenase (17β-HSD) family that in ... "The human type II 17 beta-hydroxysteroid dehydrogenase gene encodes two alternatively spliced mRNA species". DNA and Cell ...
42 (1): 1-23. doi:10.1016/j.jchemneu.2011.05.003. PMC 3148274. PMID 21605659. Dong, HW; Petrovich, GD; Watts, AG; Swanson, LW ( ... 1115 (1): 54-64. doi:10.1016/j.brainres.2006.07.091. PMID 16935272. Geerling, JC; Kawata, M; Loewy, AD (Jan 20, 2006). " ... Geerling, JC; Engeland, WC; Kawata, M; Loewy, AD (Jan 11, 2006). "Aldosterone target neurons in the nucleus tractus solitarius ... Geerling, JC; Loewy, AD (Aug 1, 2006). "Aldosterone-sensitive neurons in the nucleus of the solitary tract: bidirectional ...
... type 2 deficiency 17 alpha hydroxylase deficiency 17 beta hydroxysteroide dehydrogenase deficiency 17-beta-hydroxysteroid ... type 3, rare (NIH) 3 beta hydroxysteroid dehydrogenase deficiency 3 hydroxyisobutyric aciduria 3 hydroxyisobutyric aciduria, ... dehydrogenase deficiency, rare (NIH) 17q21.31 microdeletion syndrome 18-Hydroxylase deficiency, rare (NIH) 18p deletion ... 3 methylglutaconyl coa hydratase deficiency 3-hydroxy 3-methyl glutaryl-coa lyase deficiency 3-hydroxyacyl-coa dehydrogenase ...
3(or+17)beta-hydroxysteroid+dehydrogenase at the US National Library of Medicine Medical Subject Headings (MeSH) Portal: ... Soubhye J, Alard IC, van Antwerpen P, Dufrasne F (2015). "Type 2 17-β hydroxysteroid dehydrogenase as a novel target for the ... Yang SY, He XY, Isaacs C, Dobkin C, Miller D, Philipp M (2014). "Roles of 17β-hydroxysteroid dehydrogenase type 10 in ... Aka JA, Mazumdar M, Chen CQ, Poirier D, Lin SX (April 2010). "17beta-hydroxysteroid dehydrogenase type 1 stimulates breast ...
Rheault P, Dufort I, Soucy P, Luu-The V (1999). "Assignment of HSD17B5 encoding type 5 17 beta-hydroxysteroid dehydrogenase to ... 3-alpha hydroxysteroid dehydrogenase, type II)". Theisen, J. Graham; Sundaram, Viji; Filchak, Mary S.; Chorich, Lynn P.; ... also known as 17β-hydroxysteroid dehydrogenase type 5 (17β-HSD5, HSD17B5) is a key steroidogenic enzyme that in humans is ... "Structural basis of the multispecificity demonstrated by 17beta-hydroxysteroid dehydrogenase types 1 and 5". Molecular and ...
... estradiols having inhibitory effect on human placental estradiol 17 beta-hydroxysteroid dehydrogenase (17 beta-HSD type 1)". ... "Entrez Gene: HSD17B1 Hydroxysteroid (17-beta) dehydrogenase 1". Saloniemi T, Jokela H, Strauss L, Pakarinen P, Poutanen M (2012 ... Aka JA, Mazumdar M, Chen CQ, Poirier D, Lin SX (Apr 2010). "17beta-hydroxysteroid dehydrogenase type 1 stimulates breast cancer ... Sawetawan C, Milewich L, Word RA, Carr BR, Rainey WE (Mar 1994). "Compartmentalization of type I 17 beta-hydroxysteroid ...
This type of receptor becomes activated upon ligand binding. After a hormone binds to the corresponding receptor, the newly ... 1 (1). doi:10.15347/wjm/2014.005. ISSN 2002-4436. Omar, HR; Komarova, I; El-Ghonemi, M; Fathy, A; Rashad, R; Abdelmalak, HD; ... This enzyme, 11-beta hydroxysteroid dehydrogenase type II (Protein:HSD11B2), catalyzes the deactivation of glucocorticoids to ... 11 ed)., Saunders Elsevier, Philadelphia, pp. 445-504. Bennett PN and Brown MJ (2008) "Adrenal corticosteroids, antagonists, ...
Studies on the stably transfected isoforms and localization of the type 2 isozyme within renal tissue". Steroids. 62 (1): 77-82 ... 11α-OHP is a more potent inhibitor of 11β-HSD than enoxolone (glycyrrhetinic acid) or carbenoxolone in vitro (IC50 = 0.9 nM; ... 11 alpha-Hydroxyprogesterone (11 alpha OH-P) was an order of magnitude more potent a competitive inhibitor of the 11 beta HSD-2 ... 11α-OHP was investigated as a topical antiandrogen for the treatment of androgen-dependent skin conditions in the early 1950s, ...
... metabolism Disorders of sexual development Intersex 17β-Hydroxysteroid dehydrogenase 17β-Hydroxysteroid dehydrogenase Type III ... "HSD17B3 hydroxysteroid 17-beta dehydrogenase 3 [Homo sapiens (human)] - Gene - NCBI". www.ncbi.nlm.nih.gov. Retrieved 2017-03- ... "17-beta hydroxysteroid dehydrogenase 3 deficiency , Genetic and Rare Diseases Information Center (GARD) - an NCATS Program". ... "17-beta hydroxysteroid dehydrogenase 3 deficiency". Genetics Home Reference. Retrieved 2017-03-11. "OMIM Entry - # 264300 - 17- ...
"Polymorphism in exon 4 of the human 3 beta-hydroxysteroid dehydrogenase type I gene (HSD3B1) and blood pressure". Biochemical ... "Localization of type 5 17beta-hydroxysteroid dehydrogenase, 3beta-hydroxysteroid dehydrogenase, and androgen receptor in the ... "Immunoelectron microscopic localization of 3beta-hydroxysteroid dehydrogenase and type 5 17beta-hydroxysteroid dehydrogenase in ... HSD3B1 is a human gene that encodes for a 3beta-hydroxysteroid dehydrogenase/delta(5)-delta(4)isomerase type I or hydroxy-delta ...
Soubhye J, Alard IC, van Antwerpen P, Dufrasne F (2015). "Type 2 17-β hydroxysteroid dehydrogenase as a novel target for the ... Sam KM, Auger S, Luu-The V, Poirier D (1995). "Steroidal spiro-gamma-lactones that inhibit 17 beta-hydroxysteroid dehydrogenase ... Poirier D (2003). "Inhibitors of 17 beta-hydroxysteroid dehydrogenases". Curr. Med. Chem. 10 (6): 453-77. doi:10.2174/ ... "Spironolactone-related inhibitors of type II 17beta-hydroxysteroid dehydrogenase: chemical synthesis, receptor binding ...
"Abundant type 10 17 beta-hydroxysteroid dehydrogenase in the hippocampus of mouse Alzheimer's disease model". Brain Research. ... 17-β-Hydroxysteroid dehydrogenase X (HSD10) also known as 3-hydroxyacyl-CoA dehydrogenase type-2 is a mitochondrial enzyme that ... 17-beta) dehydrogenase 10". He XY, Yang YZ, Schulz H, Yang SY (Jan 2000). "Intrinsic alcohol dehydrogenase and hydroxysteroid ... Yang SY, He XY, Isaacs C, Dobkin C, Miller D, Philipp M (Sep 2014). "Roles of 17β-hydroxysteroid dehydrogenase type 10 in ...
... type I (dexamethasone suppressible), and type II, which has been linked to the 7p22 gene. Features Hypertension Hypokalemia (e. ... November 2000). "A novel genetic locus for low renin hypertension: familial hyperaldosteronism type II maps to chromosome 7 ( ... 37 (11): 831-5. doi:10.1136/jmg.37.11.831. PMC 1734468. PMID 11073536. Dominguez A, Muppidi V, Gupta S. "Hyperaldosteronism". ... Through inhibition of 11-beta-hydroxysteroid dehydrogenase type 2 (11-beta-HSD2), glycyrrhizin allows cortisol to activate ...
Dehydrogenase/reductase (SDR family) member 7B is an enzyme encoded by the DHRS7B gene in humans, found on chromosome 17p11.2. ... CD44 is an antigen found on the surface of most cell types and functions as a receptor that binds tissue macromolecules. ... "Entrez Gene: Dehydrogenase/reductase (SDR family) member 7B". "Genecards: DHRS7B Gene protein-coding GIFtS 47". Tannin GM, ... DHRS7B is a member of the short chain dehydrogenase/reductase (SDR) superfamily and possesses characteristic features of an SDR ...
testicular: enzymatic (5-alpha-reductase deficiency, 17-beta-hydroxysteroid dehydrogenase deficiency) · Androgen receptor ( ... types: (type 1, type 2, MODY 1 2 3 4 5 6) · complications (coma, angiopathy, ketoacidosis, nephropathy, neuropathy, retinopathy ... 11] Epidemiolojia[hariri , hariri chanzo]. Ugonjwa wa Cushing wa iatrojeniki (unaosababishwa na matibabu kwa kutumia steroidi ... Autoimmune polyendocrine syndrome (APS1, APS2) · Carcinoid syndrome · Multiple endocrine neoplasia (1, 2A, 2B) · Progeria ( ...
... adrenal hyperplasia due to 21-hydroxylase deficiency Congenital adrenal hyperplasia due to 3 beta-hydroxysteroid dehydrogenase ... CDG syndrome type 1A CDG syndrome type 1B CDG syndrome type 1C CDG syndrome type 2 CDG syndrome type 3 CDG syndrome type 4 CDK4 ... Tooth disease type 1C Charcot-Marie-Tooth disease type 2A Charcot-Marie-Tooth disease type 2B1 Charcot-Marie-Tooth disease type ... disease type 2C Charcot-Marie-Tooth disease type 2D Charcot-Marie-Tooth disease type 4A Charcot-Marie-Tooth disease type 4B ...
... in vitro induction of 20 alpha-hydroxysteroid dehydrogenase in splenic lymphocytes from athymic mice by a unique lymphokine". J ... It is thought that this genetic change is the key in development of this leukemia type. Human IL-3 was first cloned in 1986 and ... Kitamura T, Sato N, Arai K, Miyajima A (1991). "Expression cloning of the human IL-3 receptor cDNA reveals a shared beta ... IL-3 is mainly produced by activated T cells with the goal of initiating proliferation of various other immune cell types. ...
CYP17A1 17-beta-hydroxysteroid dehydrogenase X deficiency; 300438; HSD17B10 2-methylbutyrylglycinuria; 610006; ACADSB 3- ... type 1B; 276900; MYO7A Usher syndrome, type 1C; 276904; USH1C Usher syndrome, type 1D; 601067; CDH23 Usher syndrome, type 1D/F ... F5 Factor XI deficiency, autosomal dominant; 612416; F11 Factor XI deficiency, autosomal recessive; 612416; F11 Factor XII ... type I; 125850; HNF4A MODY, type II; 125851; GCK MODY, type III; 600496; HNF1A MODY, type IV; 606392; IPF1 Mohr-Tranebjærg ...
Osteoporosis is a type of bone disease characterized by a loss of bone density, mass and architecture that leaves a patient ... beta]-hydroxy-20[alpha]-hydroxymethylprednisolone. As stated previously, the primary use of methylprednisolone is to suppress ... The prevalence of mGRs ranges per cell type, with the highest concentration in B lymphocytes at up to 12.3%, up to 9.2% in ... The type and severity of neuropsychiatric symptoms also varies significantly between patients, with 33% of patients reporting ...
Rosler A (August 2006). "17 beta-hydroxysteroid dehydrogenase 3 deficiency in the Mediterranean population". Pediatric ... Bare lymphocyte syndrome high in western Arabic block Morocco, type II limb-girdle muscular dystrophy, type 2C in Libya, ... Jerash type of the distal hereditary motor neuropathy (2000) •• Karak syndrome (2003) •• Omani type of spondyloepiphy Below is ... Lebanese type of mannose 6--phosphate receptor recognition defect (1984) •• Algerian type of spondylometaphyseal dysplasia ( ...
Type A (express A antigens), Type B (express B antigens), Type AB (express both A and B antigens) and Type O (express neither A ... Herbst EA, MacPherson RE, LeBlanc PJ, Roy BD, Jeoung NH, Harris RA, Peters SJ (Jan 2014). "Pyruvate dehydrogenase kinase-4 ... Due to this, alcohol sulfotransferase is also known by several other names including "hydroxysteroid sulfotransferase," " ... Earliest discoveries of transferase activity occurred in other classifications of enzymes, including beta-galactosidase, ...
"Entrez Gene: HSD17B8 hydroxysteroid (17-beta) dehydrogenase 8". Kikuti YY, Tamiya G, Ando A, et al. (1997). "Physical mapping ... 2007). "Transcriptional regulation of the human type 8 17beta-hydroxysteroid dehydrogenase gene by C/EBPbeta". J. Steroid ... In mice, the Ke6 protein is a 17-beta-hydroxysteroid dehydrogenase that can regulate the concentration of biologically active ... 2006). "Expression of aromatase and 17beta-hydroxysteroid dehydrogenase types 1, 7 and 12 in breast cancer. An ...
... in the regulation of human corpus luteum 3beta-hydroxysteroid dehydrogenase type II". The Journal of Clinical Endocrinology and ... LRH-1 is a member of the nuclear receptor family of intracellular transcription factors. LRH-1 plays a critical role in the ... 5 (1): 1-2. doi:10.1016/S1534-5807(03)00196-5. PMID 12852843. Fayard E, Schoonjans K, Annicotte JS, Auwerx J (Sep 2003). "Liver ... Cai YN, Zhou Q, Kong YY, Li M, Viollet B, Xie YH, Wang Y (Dec 2003). "LRH-1/hB1F and HNF1 synergistically up-regulate hepatitis ...
Then, 16α-OH-DHEA is converted by 3β-hydroxysteroid dehydrogenase type I (3β-HSD1) into 16α-hydroxyandrostenedione (16α-OH-A4) ... "Evaluation of ligand selectivity using reporter cell lines stably expressing estrogen receptor alpha or beta". Biochemical ... DHEA is converted by 3β-hydroxysteroid dehydrogenase type I into androstenedione, and androstenedione is aromatized into ... Then, placental 17β-hydroxysteroid dehydrogenase interconverts estrone and estradiol and the two hormones are secreted into the ...
This is due to its inability to be inactivated by uterine 17β-hydroxysteroid dehydrogenase (17β-HSD). Because of its ... Type of aqueous (solution or suspension) was not specified. Testosterone levels in relation to estradiol levels (and ... Lobo RA, Cassidenti DL (January 1992). "Pharmacokinetics of oral 17 beta-estradiol". J Reprod Med. 37 (1): 77-84. PMID 1548642 ... As a result of the alkylation in 17-C position it is not a substrate for 17β dehydrogenase, an enzyme which transforms natural ...
3β-Hydroxysteroid dehydrogenase (3β-HSD) inhibitors such as amphenone B, azastene, cyanoketone, epostane, mitotane, and ... Schroepfer GJ, Parish EJ, Kisic A, Jackson EM, Farley CM, Mott GE (1982). "5 alpha-Cholest-8(14)-en-3 beta-ol-15-one, a potent ... A steroidogenesis inhibitor, also known as a steroid biosynthesis inhibitor, is a type of drug which inhibits one or more of ... 17β-Hydroxysteroid dehydrogenase (17β-HSD) inhibitors prevent the reversible conversion of the weak androgens ...
In the final and rate limiting step, the C17 keto group androstenedione is reduced by 17β-hydroxysteroid dehydrogenase to yield ... These include adult-type body odor, increased oiliness of skin and hair, acne, pubarche (appearance of pubic hair), axillary ... In addition, the 3β-hydroxyl group is oxidized by 3β-hydroxysteroid dehydrogenase to produce androstenedione. ... 3α-hydroxysteroid dehydrogenase, and 17β-HSD, in that order. Androsterone and etiocholanolone are then glucuronidated and to a ...
... allowing it to inhibit the activity of aromatase and 3α-hydroxysteroid dehydrogenase. These enzymes are involved in the ... The highest concentrations of coumestrol are found in clover, Kala Chana (a type of chick pea), and Alfalfa sprouts. Coumestrol ... "Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta". ... 3α-Hydroxysteroid dehydrogenase inhibitors, Aromatase inhibitors, Coumestans, Phytoestrogens, Selective ERβ agonists, Phenols) ...
3β-Hydroxysteroid dehydrogenase inhibitors, CYP17A1 inhibitors, Hepatotoxins, Thiazolidinediones, Aminopyridines, Phenol ethers ... It doubled the risk of fractures among women with type 2 diabetes, without a significant increase in risk of fractures among ... It is also found in pancreatic beta cells, vascular endothelium, and macrophages Rosiglitazone is a selective ligand of PPARγ ... Investigators from the Cochrane Collaboration published a meta-analysis of their own on the use of rosiglitazone in Type II ...
Enzymes involved in this process include both mitochondrial and microsomal P450s and hydroxysteroid dehydrogenases. Usually a ... This type of adrenal insufficiency usually does not affect the production of mineralocorticoids, which are under regulation of ... The central adrenomedullary vein, in the adrenal medulla, is an unusual type of blood vessel. Its structure is different from ... The adrenal glands are composed of two heterogenous types of tissue. In the center is the adrenal medulla, which produces ...
Zennaro MC, Farman N, Bonvalet JP, Lombès M (May 1997). "Tissue-specific expression of alpha and beta messenger ribonucleic ... "Mutations in the mineralocorticoid receptor gene cause autosomal dominant pseudohypoaldosteronism type I". Nature Genetics. 19 ... 52 (1-2): 83-4. doi:10.1159/000132846. PMID 2558856. Edwards CR, Stewart PM, Burt D, Brett L, McIntyre MA, Sutanto WS, et al. ( ... 85 (1): 130-2. doi:10.1007/BF00276340. PMID 2162806. S2CID 9264993. Fan YS, Eddy RL, Byers MG, Haley LL, Henry WM, Nowak NJ, ...
17 beta-dihydroxy-17-methyl-1, 4-androstadien-3-one and related compounds". Steroids. 43 (3): 271-82. doi:10.1016/0039-128x(84) ... beta)-diol-3-one) in humans". J. Int. Med. Res. 4 (2): 96-105. doi:10.1177/030006057600400203. PMID 799985. S2CID 86157607. ... 27 (3 Pt 1): 421-5. doi:10.1161/01.hyp.27.3.421. PMID 8698448. Fürstenberger C, Vuorinen A, Da Cunha T, Kratschmar DV, Saugy M ... 577-. ISBN 978-1-4757-2085-3. I.K. Morton; Judith M. Hall (31 October 1999). Concise Dictionary of Pharmacological Agents: ...
17 beta-dihydroxy-17-methyl-1, 4-androstadien-3-one and related compounds". Steroids. 43 (3): 271-82. doi:10.1016/0039-128x(84) ... 27 (3 Pt 1): 421-5. doi:10.1161/01.hyp.27.3.421. PMID 8698448. Fürstenberger C, Vuorinen A, Da Cunha T, Kratschmar DV, Saugy M ... In accordance, 11α- and 11β-hydroxyprogesterone are known to be potent inhibitors of 11β-hydroxysteroid dehydrogenase (11β-HSD ... ISBN 978-1-4757-2085-3. Felippone F, Resnati G, Scolastico C, Tronconi G (1984). "Synthesis of 2-carboxy-11 beta, ...
Subsequently, 20α-hydroxysteroid dehydrogenase and 20β-hydroxysteroid dehydrogenase reduce these metabolites to form the ... Collaborative Group on Hormonal Factors in Breast Cancer (September 2019). "Type and timing of menopausal hormone therapy and ... "Progesterone receptor knockout mice have an improved glucose homeostasis secondary to beta -cell proliferation". Proceedings of ... This is followed by the further reduction of these metabolites via 3α-hydroxysteroid dehydrogenase and 3β-hydroxysteroid ...
11beta-HSD) catalyzes the reversible oxidoreduction of 11beta-OH/11-oxo groups of glucocorticoid hormones. Besides this ... Purified recombinant 11beta-HSD1 mediated oxidative reactions, however, the labile reductive activity component could not be ... In conclusion, evidence is provided that human 11beta-HSD1 in vitro is involved in phase I reactions of anti-inflammatory non- ... The aim of this study was to explore novel substrate specificities of human 11beta-HSD1, using heterologously expressed protein ...
Human ALDH1A2(Aldehyde Dehydrogenase 1 Family, Member A2) ELISA Kit. *Human ALDOC(Aldolase C, Fructose Bisphosphate) ELISA Kit ... Human PCSK5(Proprotein Convertase Subtilisin/Kexin Type 5) ELISA Kit. *Human PDCD1LG1(Programmed Cell Death Protein 1 Ligand 1 ... Human ALDH1A1(Aldehyde Dehydrogenase 1 Family, Member A1) ELISA Kit. * ... Human CELSR2(Cadherin EGF LAG Seven Pass G-Type Receptor 2) ELISA Kit ...
11 beta-hydroxysteroid dehydrogenase type 1 in obese children Wiegand S., Richardt A., Remer T., Wudy SA., Tomlinson JW., ...
... beta-hydroxysteroid dehydrogenase isoforms using reverse-transcriptase-polymerase chain reaction and localization of the type 2 ... Wake DJ, Walker BR (February 2006). "Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 in obesity". Endocrine. 29 (1): ... Agarwal AK (November 2003). "Cortisol metabolism and visceral obesity: role of 11beta-hydroxysteroid dehydrogenase type I ... "11beta-Hydroxysteroid dehydrogenase types 1 and 2 are up- and downregulated in cortisol-secreting adrenal adenomas". Journal of ...
The impact of endogenous cortisone on bone and fat: demonstration of in vivo 11beta-hydroxysteroid dehydrogenase type 1 ... Analysis of hCG beta core fragment glycosylation in normal and aberrant pregnancy by matrix-assisted laser desorption/ ... A novel non-steroidal inhibitor of 11beta-hydroxysteroid dehydrogenase type 1 improves features of metabolic syndrome in murine ... A model for evaluating 11beta-hydroxysteroid dehydrogenase type 1 activity in ocular and orbital tissues ...
11beta-hydroxysteroid dehydrogenase type 1 activity in lean and obese males with type 2 diabetes mellitus. ... Product OverviewBeta ProgramS2AG APISemantic Reader. Research. PublicationsTeamResearch CareersResources ... Apparent mineralocorticoid excess: Type I and type II. *F. Mantero, M. Palermo, M. Petrelli, R. Tedde, P. Stewart, C. ... hydroxysteroid dehydrogenase (11β‐HSD) catalyse the interconversion of cortisol to hormonally… Expand. ...
The 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor is an enzyme that converts the inert hormone cortisone ... 44 Using a model involving GPR119 beta-cell-expressing mice with type 2 diabetes, the investigators demonstrated a significant ... Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Drug Disc Today. 2007;12:504-520. ... Effects of the 11beta-hydroxysteroid dehydrogenase inhibitor carbenoxolone in insulin sensitivity in men with type 2 diabetes. ...
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Rapid hepatic metabolism of 7-ketocholesterol by 11beta-hydroxysteroid dehydrogenase type 1: species-specific differences ... In our simulation, E169, R188, H220, T223 and S244 located on the beta sheets of the cholesterol binding cavity next to helix 3 ... However, only ∼25% of such patients were found to be the carriers of MC2R mutations and have been classified as type 1 FGD [7] ... Vectors expressing cDNAs of wild-type (wt) StAR and the fusion protein P450 side-chain cleavage/adrenodoxin/adrenodoxin ...
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To test this hypothesis, Flier and his colleagues studied the enzyme 11beta hydroxysteroid dehydrogenase type 1 (11 beta HSD-1 ... US Obesity-Related Costs (Annual) Obesity Related Disease Costs Overwhelm HealthCare System Type II Diabetes ($63.14… Read More ... The researchers created a group of transgenic (Tg) mice that overproduce 11 beta HSD-1 in roughly the same quantities ... the findings strongly suggest that the 11 beta HSD-1 enzyme is an exciting pharmaceutical target for the treatment of visceral ...
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11beta-hydroxysteroid dehydrogenase types 1 and 2: an important pharmacokinetic determinant for the activity of synthetic ... Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the rea.... Gene Name. ... 11beta-hydroxysteroid dehydrogenase types 1 and 2: an important pharmacokinetic determinant for the activity of synthetic ... SummaryBrand NamesNameAccession NumberBackgroundTypeGroupsStructureWeightChemical FormulaSynonyms ...
... and water reabsorption is mediated by 11beta-hydroxysteroid dehydrogenase type 2 that protects the mineralocorticoid receptor ... 11beta-HSD type 1 (11beta-HSD1), that generates intraocular cortisol. In a mechanism analogous to that of the embryologically ... an 11beta-HSD inhibitor). Using the real time-polymerase chain reaction, rabbit CP tissue was found to express levels of 11beta ... Expression of 11beta-HSD1 may be fundamental in the regulation of CSF secretion and the local generation of cortisol may ...
2 - Via inhibition of 11beta-hydroxysteroid dehydrogenase type 1.. 3 - All measurements were taken at least three times and ... You want a the highest concentration of beta waves in that part of the brain. In clients with low F3/C3 beta activity, I see a ... Im typing into my Evernote (Slow carb "rules," Occams routine, various instructional bits from the book that I might want to ... I agree with Katie regarding the type of diet you should follow. As someone who has trained a lot, at one point I had a bodyfat ...
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2002) 11beta-hydroxysteroid dehydrogenase types 1 and 2: An important pharmacokinetic determinant for the activity of synthetic ... 2009) Latent TGF-beta-binding protein 4 modifies muscular dystrophy in mice. J Clin Invest 119: 3703-3712. doi:10.1172/jci39845 ... In wild-type mice, the only effect observed for aldosterone was a smaller increase in LV mass (P , 0.05), which was similar to ... Wild-type (strain 000476; C57BL/10ScSnJ) and mdx (strain 001801; C57BL/10ScSn-Dmdmdx/J) mice were obtained from The Jackson ...
The expression of the IUGR marker genes leptin and 11beta-hydroxysteroid dehydrogenase 2 (11beta-HSD2) was measured ... CRH did not influence the differentiation of isolated trophoblasts into functional syncytium as determined by beta-hCG ... The induction of leptin and 11beta-HSD2 in the syncytiotrophoblast by CRH might promote fetal nutrient supply and placental ... Following syncytialisation, CRH treatment significantly increased leptin and 11beta-HSD2 expression, as well as leptin ...
Mouse Monoclonal Estrogen Receptor beta antibody [14C8]. Validated in WB, ICC/IF, IHC-P, IHC-Fr, FACS, Dot, ChIP assay, IHC, ... 167 Intratumoral localization and activity of 17β-hydroxysteroid dehydrogenase type 1 in non-small cell lung cancer: a potent ... PLoS One 2009; 4 (7):e6271 Drug and cell type-specific regulation of genes with different classes of estrogen receptor beta- ... Estrogen Receptor beta stained by Estrogen Receptor beta antibody [14C8] (GTX70174) diluted at 1:200.. Antigen Retrieval: ...
34, 1, p. 1-16 . IF = 2.643 [ASEP] [ doi ] Ergang, Peter - Vodička, Martin - Vagnerová, Karla - Moravec, Martin - Kvapilová, ... 2020; 10(1)); 8529 . IF = 4.379 [ASEP] [ doi ] Vodička; Martin - Vavřínová; Anna - Mikulecká; Anna - Zicha; Josef - Behuliak; ... Regulation of 11 beta-Hydroxysteroid Dehydrogenase Type 1 and 7 alpha-Hydroxylase CYP7B1 during Social Stress . PLoS ONE 2014, ... Expression of 11 beta-hydroxysteroid dehydrogenase type 2 is deregulated in colon carcinoma . Histology and Histopathology 2014 ...
Association between 11beta-hydroxysteroid dehydrogenase type 1 gene polymorphisms and metabolic syndrome in Bosnian population. ... beta}-HSD1 activity and metabolic syndrome in women with and without polycystic ovary syndrome. European journal of ... Genetic variation in 11beta-hydroxysteroid dehydrogenase type 1 predicts adrenal hyperandrogenism among lean women with ... Relationship of 11ß-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase gene polymorphisms with metabolic ...
11beta-hydroxysteroid dehydrogenase type 1 mRNA is increased in both visceral and subcutaneous adipose tissue of obese patients ... pseudo-Cushings syndrome is associated with increased regeneration of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 ... A particular type of hypercortisolism presenting during the above conditions, named functional hypercortisolism, is caused by ... 15] In a study of 190 patients with type 2 diabetes, 63 subjects (33%) had high cortisol concentrations. [16] ...
Reconstitute second 1-mg vial. *Reconstitute the second 1-mg vial with the entire solution from the first reconstituted vial ... Serious - Use Alternative (1)tesamorelin will decrease the level or effect of cortisone by altering metabolism. Avoid or Use ... Serious - Use Alternative (1)tesamorelin will decrease the level or effect of prednisone by altering metabolism. Avoid or Use ... Serious - Use Alternative (1)tesamorelin will decrease the level or effect of ulipristal by altering metabolism. Avoid or Use ...
However, D7 cortisol enrichment was detectable in abdominal sc fat of overweight/obese participants with type 2 diabetes ... However, D7 cortisol enrichment was detectable in abdominal sc fat of overweight/obese participants with type 2 diabetes ... However, D7 cortisol enrichment was detectable in abdominal sc fat of overweight/obese participants with type 2 diabetes ... However, D7 cortisol enrichment was detectable in abdominal sc fat of overweight/obese participants with type 2 diabetes ...
Do Legal Steroids not show similar fiber type and improved energy. Doctor and pharmacist of all users with the Revised Male ... Week 1-12: Test Cypionate association of endogenous testosterone know as much as possible because steroids do have all kinds of ... 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD-1) required for many physical and discover everything you need to know ...
3-beta hydroxysteroid dehydrogenase deficiency, and 17 alpha-hydroxylase/17,20-lyase deficiency are generally not characterized ... Type 1 GFND maps to chromosome 1q32, but the gene is unknown at this time. Type 2 GFND is caused by mutations in the FN1 gene ... Beta-adrenergic agonists enhance potassium entry into cells, whereas beta-blockers and alpha-adrenergic agonists inhibit it. ... Type I pseudohypoaldosteronism (PHAI) can be caused by an inactivating mutation of 1 of 3 encoding subunits of the epithelial ...
3-beta hydroxysteroid dehydrogenase deficiency, and 17 alpha-hydroxylase/17,20-lyase deficiency are generally not characterized ... Type 1 GFND maps to chromosome 1q32, but the gene is unknown at this time. Type 2 GFND is caused by mutations in the FN1 gene ... Beta-adrenergic agonists enhance potassium entry into cells, whereas beta-blockers and alpha-adrenergic agonists inhibit it. ... Type I pseudohypoaldosteronism (PHAI) can be caused by an inactivating mutation of 1 of 3 encoding subunits of the epithelial ...
... identifying the liver as a major site of extra-adrenal cortisol production via intrahepatic 11beta-hydroxysteroid dehydrogenase ... His research focuses on the molecular mechanisms regulating insulitis and beta cell apoptosis in type 1 diabetes and on the ... Recorded Presentation Title: Therapy of Type 1 Diabetes: The DCCT-EDIC Trials. Live Discussion: April 16, 1030-1110 [EDT]. Dr. ... Recorded Presentation Title: A Primary Role for Insulin Therapy in Type 2 Diabetes. Live Discussion: April 15, 0940-1020. Dr. ...
  • The human enzyme 11beta-hydroxysteroid dehydrogenase (11beta-HSD) catalyzes the reversible oxidoreduction of 11beta-OH/11-oxo groups of glucocorticoid hormones. (ox.ac.uk)
  • To test this hypothesis, Flier and his colleagues studied the enzyme 11beta hydroxysteroid dehydrogenase type 1 (11 beta HSD-1), which has the unique ability to produce cortisol in cells that are not normally associated with cortisol production. (annecollins.com)
  • The enzyme 11beta-hydroxysteroid dehydrogenase (11B-HSD) reversibly converts biologically active cortisol to inactive cortisone, and when present in placentae may act to protect fetuses from high concentrations of maternal glucocorticoids. (usda.gov)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human 11-Beta-Hydroxysteroid Dehydrogenase Type 1 (HSD11b1) in tissue homogenates, cell lysates and other biological fluids. (lipidx.org)
  • Variants in HSD11B1 gene modulate susceptibility to diabetes kidney disease and to insulin resistance in type 1 diabetes. (cdc.gov)
  • Interaction of HSD11B1 and H6PD polymorphisms in subjects with type 2 diabetes are protective factors against obesity: a cross-sectional study. (cdc.gov)
  • Association of HSD11B1 gene polymorphisms with type 2 diabetes and metabolic syndrome in South Indian population. (cdc.gov)
  • Association of HSD11B1 polymorphic variants and adipose tissue gene expression with metabolic syndrome, obesity and type 2 diabetes mellitus: a systematic review. (cdc.gov)
  • A combination of polymorphisms in HSD11B1 associates with in vivo 11{beta}-HSD1 activity and metabolic syndrome in women with and without polycystic ovary syndrome. (cdc.gov)
  • 11β-Hydroxysteroid dehydrogenase type 1, also known as cortisone reductase, is an NADPH-dependent enzyme highly expressed in key metabolic tissues including liver, adipose tissue, and the central nervous system. (wikipedia.org)
  • This is opposite to classical Na(+) transporting tissues, such as the kidney, where Na(+) and water reabsorption is mediated by 11beta-hydroxysteroid dehydrogenase type 2 that protects the mineralocorticoid receptor by abrogating active cortisol to inactive cortisone. (ox.ac.uk)
  • [ 22 , 23 ] In obesity, postulated mechanisms of hyperactivation of HPA axis include hyper-responsiveness to different neuropeptides, stress events, dietary factors, as well as a stimulation caused by augmented peripheral metabolism and clearance of cortisol by reduced conversion of cortisone to cortisol by 11β-HSD1 and increased conversion of cortisol to 5α-reduced derivatives. (medscape.com)
  • Design: 11β-HSD-1 and -2 enzyme activities in abdominal and leg sc adipose tissue were measured by infusing [2,2,4,6,6,12,12-2H7] cortisone (D7 cortisone) and [9,12,12-2H3] cortisol (D3 cortisol) via microdialysis catheters placed in sc fat depots. (elsevier.com)
  • Main Outcome Measures: The conversion of infused D7 cortisone to D7 cortisol (via 11β-HSD reductase activity) and D3 cortisol to D3 cortisone (via 11β-HSD dehydrogenase activity) in sc adipose tissue. (elsevier.com)
  • D3 cortisone enrichment did not differ in the three cohorts, indicating that 11β-HSD-2 enzyme activity (conversion of cortisol to cortisone) occurs equally in all groups. (elsevier.com)
  • However, D7 cortisol enrichment was detectable in abdominal sc fat of overweight/obese participants with type 2 diabetes mellitus only, implying 11β-HSD-1 reductase activity (conversion of cortisone to cortisol) occurs in obese subjects with type 2 diabetes. (elsevier.com)
  • Conclusions: There is conversion of cortisone to cortisol via the 11β-HSD-1 enzyme pathway in abdominal sc fat depots in overweight/obese participants with type 2 diabetes mellitus. (elsevier.com)
  • It has been suggested for humans and rodents that the placental enzyme, a biological catalyst, 11beta-hydroxysteroid dehydrogenase (11B-HSD) converts biologically active cortisol to an inactive steroid, cortisone. (usda.gov)
  • Reduced nicotinamide adenine dinucleotide phosphate is a necessary cofactor for the reductase activity of 11β-hydroxysteroid dehydrogenase type 1 (EC 1.1.1.146), which converts hormonally inactive cortisone to active cortisol (in rodents, 11-dehydrocorticosterone to corticosterone). (elsevier.com)
  • 3 (1) : vdab099 Histone deacetylase inhibitors enhance estrogen receptor beta expression and augment agonist-mediated tumor suppression in glioblastoma. (genetex.com)
  • This observation has significant implications for developing tissue-specific 11β-HSD-1 inhibitors in type 2 diabetes mellitus. (elsevier.com)
  • Relationship of 11ß-hydroxysteroid dehydrogenase type 1 and hexose-6-phosphate dehydrogenase gene polymorphisms with metabolic syndrome and type 2 diabetes. (cdc.gov)
  • Hexose-6-phosphate dehydrogenase (EC 1.1.1.47) catalyzes the conversion of glucose 6-phosphate to 6-phosphogluconolactone within the lumen of the endoplasmic reticulum, thereby generating reduced nicotinamide adenine dinucleotide phosphate. (elsevier.com)
  • Mice with targeted inactivation of hexose-6-phosphate dehydrogenase lack 11β-hydroxysteroid dehydrogenase type 1 reductase activity, whereas dehydrogenase activity (corticosterone to 11- dehydrocorticosterone) is increased. (elsevier.com)
  • Description: A sandwich ELISA kit for detection of Free Fatty Acid Receptor 1 from Rat in samples from blood, serum, plasma, cell culture fluid and other biological fluids. (hiv-pharmacogenomics.org)
  • The induction of leptin and 11beta-HSD2 in the syncytiotrophoblast by CRH might promote fetal nutrient supply and placental corticosteroid metabolism in the phase before labour induction. (biomedcentral.com)
  • Journal of Clinical Endocrinology and Metabolism , 100 (1), E70-E76. (elsevier.com)
  • In terms of tissue-specific cortisol metabolism, it is said that the enzyme 11 beta - hydroxysteroid dehydrogenase type 1 (11B-HSD1) is relevant in HPA axis activity, regenerating active cortisol from its inactive forms intracellularly. (mindbodyfunctionalmedicine.com)
  • She then undertook her research fellowship with Profs Robert Sherwin and Bill Tamborlane, learning techniques for investigating human metabolism, studying changes in insulin sensitivity in childhood and adolescence and starting her life-long interest in the issues of hypoglycaemia in type 1 diabetes treatments. (insulin100.com)
  • In the tetrapods the two CRs have diverged in function, with MR playing a principal role in the control of mineral balance and GR being predominantly involved in glucose metabolism and immune function [ 10 , 11 ]. (biomedcentral.com)
  • 41 Research have demonstrated that some mycotoxins intrude with the performance of the 17-beta-hydroxysteroid dehydrogenase class of enzymes, 11 that are required for correct androgenic metabolism, together with testosterone manufacturing. (feelhealthyagain.net)
  • It belongs to the family of short-chain dehydrogenases. (wikipedia.org)
  • DHEA-S is a C-19 (19 carbon atoms) steroid hormones and 1 of 3 androgens (DHEA, DHEAS, androstenedione) secreted by the adrenal gland. (medscape.com)
  • a protein superfamily that includes receptors for estrogens (ER), progestins (PR), and androgens (AR), as well as the corticosteroid receptors (CRs), which in turn comprise the glucocorticoid (GR) and mineralocorticoid receptors (MR). The ancestral steroid receptor is believed to have resembled an ER [ 1 ]. (biomedcentral.com)
  • It seemed that one answer would be a topical lotion that inhibits the A-2 receptor or blocks phosphodiesterase (1). (tim.blog)
  • 29 (1) : 3 Estradiol-mediated inhibition of Sp1 decreases miR-3194-5p expression to enhance CD44 expression during lung cancer progression. (genetex.com)
  • Table1)1) is involved in proliferation inhibition of acute myeloid leukemia mediated by Maesopsin 4-O-beta-D-glucoside a natural compound isolated from the leaves of Artocarpus tonkinensis) [21]. (biotech2012.org)
  • The aim of this study was to explore novel substrate specificities of human 11beta-HSD1, using heterologously expressed protein in the yeast system Pichia pastoris. (ox.ac.uk)
  • A second genetic cause of FGD was identified in 15-20% of patients resulting from defects in the MC2R receptor accessory protein ( MRAP ) (FGD type 2) [7] , [8] . (plos.org)
  • Estrogen Receptor beta antibody [14C8] detects Estrogen Receptor beta protein at nucleus by immunohistochemical analysis. (genetex.com)
  • Description: A sandwich quantitative ELISA assay kit for detection of Human Elongation Of Very Long Chain Fatty Acids Like Protein 1 (ELOVL1) in samples from tissue homogenates, cell lysates or other biological fluids. (operatiebrp.nl)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Rat Elongation Of Very Long Chain Fatty Acids Like Protein 1 (ELOVL1) in tissue homogenates, cell lysates and other biological fluids. (operatiebrp.nl)
  • Description: Enzyme-linked immunosorbent assay based on the Double-antibody Sandwich method for detection of Rat Elongation Of Very Long Chain Fatty Acids Like Protein 1 (ELOVL1) in samples from tissue homogenates, cell lysates and other biological fluids with no significant corss-reactivity with analogues from other species. (operatiebrp.nl)
  • WW domain binding protein 1 like [Sour. (gsea-msigdb.org)
  • Intrathecal application route has not yet been investigated for TRIAM in autoimmune diseases of the peripheral nervous system (PNS) although the first sites of inflammation and increase of blood-nerve barrier permeability are the proximal nerve roots, as indicated by the early intrathecal protein increase found in these patients [ 11 , 12 ]. (biomedcentral.com)
  • They found elevations in the testosterone and DHT concentrations in the muscle and a particularly significant increase in the levels of 5α-reductase type 1 protein, a protein required to convert testosterone to DHT. (e-pan.org)
  • Both endogenous GH and its active protein, Insulin like growth factor-1 (IGF-1) have been found to be at high levels in diabetes, especially in patients. (endocrine-abstracts.org)
  • The p53 protein is an important tumor suppressor protein and is mutated in about 50 % of human cancers [ 1 ]. (biomedcentral.com)
  • We further validate 2 downstream candidates (oxidative stress-induced growth inhibitor 1) and (X-ray repair cross-complementing protein 5) and evaluate their functional relationship with PEL cell survival/proliferation and chemoresistance respectively. (biotech2012.org)
  • Using the real time-polymerase chain reaction, rabbit CP tissue was found to express levels of 11beta-HSD1, glucocorticoid receptor alpha and serum and glucocorticoid-regulated kinase 1 mRNA comparable to that expressed in rabbit ocular ciliary body, thereby highlighting the similarity between these two tissues. (ox.ac.uk)
  • with PbGR2b and PbGR1, the glucocorticoid 11-deoxycortisol was a more potent agonist than cortisol. (biomedcentral.com)
  • Salicylate downregulates 11β-HSD1 expression in adipose tissue in obese mice and hence may explain why aspirin improves glycemic control in type 2 diabetes. (wikipedia.org)
  • The researchers created a group of transgenic (Tg) mice that overproduce 11 beta HSD-1 in roughly the same quantities previously found in the fatty tissue of obese humans. (annecollins.com)
  • Participants: Lean nondiabetic (n = 13), overweight/obese nondiabetic (n = 15), and overweight/ obese participants with type 2 diabetes mellitus (n = 15) participated in the study. (elsevier.com)
  • Week 1-12: Test Cypionate association of endogenous testosterone know as much as possible because steroids do have all kinds of impact on the body. (enids.net)
  • Dehydroepiandrosterone (DHEA), a well-known precursor of sex hormones, is metabolized to testosterone through the activity of 17β-hydroxysteroid dehydrogenase, a sex-hormone-synthesizing hormone. (e-pan.org)
  • Testosterone is converted to dihydrotestosterone (DHT) as a result of elevated 5α-reductase expression (typically SRD5A1 and SRD5A2) 1 , 2 . (e-pan.org)
  • DNA information is delivered to the nucleus as testosterone and DHT binds to androgen receptors, based on which essential proteins are produced 1 , 2 . (e-pan.org)
  • Corticosteroids, 11beta-hydroxysteroid dehydrogenase isozymes and the rabbit choroid plexus. (ox.ac.uk)
  • Besides this important endocrinological property, the type 1 isozyme (11beta-HSD1) mediates reductive phase I reactions of several carbonyl group bearing xenobiotics, including drugs, insecticides and carcinogens. (ox.ac.uk)
  • Human hypertension caused by mutations in the kidney isozyme of 11 beta-hydroxysteroid dehydrogenase, Mune T. Rogerson FM. (childrens.com)
  • Context: The role of 11β-hydroxysteroid dehydrogenase types 1 (11β-HSD-1) and 2 (11β-HSD-2) enzymes in sc adipose tissue is controversial. (elsevier.com)
  • Objective: The objective of the study was to determine the activity of 11β-HSD-1 and -2 enzymes in the abdominal and leg sc adipose tissue in obesity and diabetes. (elsevier.com)
  • Sebocytes contain androgen-metabolizing enzymes, including 5-alpha-reductase type I, 3-beta-hydroxysteroid dehydrogenase, and 17-beta-hydroxysteroid dehydrogenase type II. (medscape.com)
  • Among these promising pharmacotherapies are agents that target the kidney, liver, and pancreas as a significant focus of treatment in type 2 diabetes. (ahdbonline.com)
  • [ 1 ] Chronic kidney disease alone generally will not cause hyperkalemia until the eGFR is less than 20-25 mL/min. (medscape.com)
  • The expression of the IUGR marker genes leptin and 11beta-hydroxysteroid dehydrogenase 2 (11beta-HSD2) was measured continuously over a period of 72 h. (biomedcentral.com)
  • The most important genes controlling the initial phase of gonadal development, identical in females and males, are Wilms' tumor suppressor 1 ( WT1 ) and steroidogenic factor 1 ( SF1 ). (hormones.gr)
  • Precise diagnosis of C. innocuum is necessary because of its unique intrinsic resistance to vancomycin, presumably caused by the presence of 2 chromosomal genes that enable the synthesis of a peptidoglycan precursor terminating in serine with low vancomycin affinity ( 9 , 11 ). (cdc.gov)
  • Notably BC-1 cells which are also EBV+ had a much higher number of uniquely altered genes than BCBL-1 and Edivoxetine HCl BCP-1. (biotech2012.org)
  • Within the common gene set the top 20 upregulated or downregulated candidate genes in SASP-treated BCP-1 BC-1 and BCBL-1 cell-lines are listed in Table ?Table11 and Table ?Table2 2 respectively including gene description and the altered level of transcription in these cell-lines. (biotech2012.org)
  • Interestingly we found that the functional role of most genes in PEL pathogenesis have never been reported although some of them have been implicated in other types of malignancies. (biotech2012.org)
  • Our results indicated that all the 5 genes (and (Oxidative stress-induced growth inhibitor 1) one of the highly upregulated genes in SASP-treated KSHV+ PEL cells from microarray data to determine its role in SASP-induced cell apoptosis. (biotech2012.org)
  • Mutations in the StAR gene were first described in patients with classic congenital lipoid adrenal hyperplasia (CLAH) in which both the adrenals and the gonads seemed to completely lack steroidogenesis [1] . (plos.org)
  • Patients with simple virilizing congenital adrenal hyperplasia (CAH), as well as those with CAH and severe virilization, are less likely to have psychosexual disorders than patients with other types of DSD. (nature.com)
  • Pathogenesis includes many genetic pathways , most prominent being Wnt-Beta catenin pathway and also association with other diseases such as multiple endocrine neoplasia ( MEN1 and MEN2 ), familial adenomatous polyposis , Beckwith-Wiedemann syndrome , Li-Fraumeni syndrome , Lynch syndrome , von Hippel-Lindau disease , carney Complex / Syndrome , neurofibromatosis type 1 and congenital adrenal hyperplasia . (wikidoc.org)
  • The IMPC applies a panel of phenotyping screens to characterise single-gene knockout mice by comparison to wild types. (mousephenotype.org)
  • Enzyme assays performed on intact rabbit CP whole tissue explants confirmed predominant 11beta-HSD1 activity, generating cortisol that was inhibited by glycyrrhetinic acid (an 11beta-HSD inhibitor). (ox.ac.uk)
  • Purified recombinant 11beta-HSD1 mediated oxidative reactions, however, the labile reductive activity component could not be maintained. (ox.ac.uk)
  • Coupled with findings from the University of Edinburgh showing a correlation between increased enzyme activity in fat tissue and obesity in human subjects, the findings strongly suggest that the 11 beta HSD-1 enzyme is an exciting pharmaceutical target for the treatment of visceral obesity. (annecollins.com)
  • Studies were conducted to determine 1) if 11B-HSD was present in pig placentae, 2) if its activity changed during gestation, and 3) if its activity was related (correlated) to fetal development. (usda.gov)
  • Since p53 induces cell death after its activation, significant research efforts are focused on harnessing this activity for tumor therapy, at least for those tumors with wild type p53. (biomedcentral.com)
  • Acute administration of corticosterone (the endogenous Type I and Type II receptor agonist), or RU28362 (a specific Type II receptor agonist), to adrenalectomized animals induced changes in leukocyte distribution. (newworldencyclopedia.org)
  • FGD has been described as a syndrome secondary to ACTH resistance, and inactivating mutations in the gene encoding melanocortin type 2 receptor ( MC2R ) were the first to be associated with FGD [6] . (plos.org)
  • Association between a 11ß-hydroxysteroid dehydrogenase type 1 gene polymorphism and metabolic syndrome in a South Indian population. (cdc.gov)
  • Metabolic syndrome and related disorders 2013 Dec 11 (6): 397-402. (cdc.gov)
  • Association between 11beta-hydroxysteroid dehydrogenase type 1 gene polymorphisms and metabolic syndrome in Bosnian population. (cdc.gov)
  • Genetic variation in 11beta-hydroxysteroid dehydrogenase type 1 predicts adrenal hyperandrogenism among lean women with polycystic ovary syndrome. (cdc.gov)
  • [ 1 , 2 ] is a group of conditions associated with clinical and biochemical features of Cushing syndrome, but the hypercortisolemia is usually secondary to other factors. (medscape.com)
  • reported a NAFLD liver fat score system (NAFLD LFS) which could predict the fat score in liver according to the metabolic syndrome (MS), type 2 diabetes (T2D), fasting insulin, AST and ALT. (researchsquare.com)
  • Animal research have demonstrated that mycotoxins are able to altering elements of each Section 1, 12-14 and Section 2 detox pathways. (feelhealthyagain.net)
  • Comparisons of their ligand structures indicate that the Δ9,11 modification of the first-in-class drug vamorolone enables it to avoid interaction with a conserved receptor residue (N770/N564), which would otherwise activate transcription factor properties of both receptors. (life-science-alliance.org)
  • Non-transfected (-) and transfected (+) 293T whole cell extracts (30 μg) were separated by 7.5% SDS-PAGE, and the membrane was blotted with Estrogen Receptor beta antibody [14C8] (GTX70174) diluted at 1:5000. (genetex.com)
  • Various tissue extracts (20 μg) were separated by 7.5% SDS-PAGE, and the membrane was blotted with Estrogen Receptor beta antibody [14C8] (GTX70174) diluted at 1:500. (genetex.com)
  • Estrogen Receptor beta stained by Estrogen Receptor beta antibody [14C8] (GTX70174) diluted at 1:200. (genetex.com)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Rat Free Fatty Acid Receptor 1 (FFAR1) in Tissue homogenates, cell lysates and other biological fluids. (hiv-pharmacogenomics.org)
  • CD4-CD8- (double negative, DN) cells become CD4+CD8+ (double positive, DP) cells following productive T cell receptor (TCR) beta chain rearrangement. (gsea-msigdb.org)
  • In vitro studies in Schwann cell cultures showed an increased expression of IL-1 receptor antagonist and reduced expression of Toll-like receptor 4 after incubation with TRIAM as well as a protective effect of TRIAM against oxidative stress after H 2 O 2 exposure. (biomedcentral.com)
  • Genetic testing and molecular biomarkers 0 15 (1-2): 43-9. (cdc.gov)
  • 1 The differentiation of the bipotent gonad to an ovary or testis follows and is also under genetic control. (hormones.gr)
  • Hence, genetic differences may also be responsible for differentiating the brain into male and female types. (biomedcentral.com)
  • While 10% of patients carry single gene mutations that cause PD (monogenic PD), over 90% of patients have no known family history or known genetic cause of their disease (sporadic PD, or sPD) [ 1 ]. (biomedcentral.com)
  • Since biology operates under the rule that anything that can go wrong will go wrong, patients have been described with a genetic defect in 11-beta-hydroxysteroid dehydrogenase. (medicine-opera.com)
  • After CRH stimulation the trophoblast syncytialisation rate was monitored via syncytin-1 gene expression and beta-hCG (beta-human chorionic gonadotropine) ELISA in culture supernatant. (biomedcentral.com)
  • Studies have established that inflammation and excess insulin are the leading cause of type 2 diabetes and the increasing weight issues in global populations. (mindbodyfunctionalmedicine.com)
  • Low insulin sensitivity signifies hyperinsulinemia, which is a precursor to type 2 diabetes. (mindbodyfunctionalmedicine.com)
  • She worked with Prof Khalida Ismail to work on aspects of mental health in both type 1 and type 2 diabetes and she developed the UK's DAFNE programme, a structured education programme for flexible insulin self-management for adults with type 1 diabetes, which reduced severe hypoglycemia, with colleagues in Sheffield, North Tyneside and Germany. (insulin100.com)
  • Whither the Future of Insulin Management in Type 2 Diabetes? (insulin100.com)
  • However, only ∼25% of such patients were found to be the carriers of MC2R mutations and have been classified as type 1 FGD [7] . (plos.org)
  • Histamine (from mast cells), serotonin (from platelets), bradykinin (from the plasma), and platelet-activating factor (from many types of cells) stimulate the endothelium to produce NO causing vasodilation. (oncohemakey.com)
  • In the human ocular ciliary epithelium, Na(+) and water secretion is dependent on a novel mediator of ciliary epithelial Na(+) transport, 11beta-HSD type 1 (11beta-HSD1), that generates intraocular cortisol. (ox.ac.uk)
  • Expression of 11beta-HSD1 may be fundamental in the regulation of CSF secretion and the local generation of cortisol may represent a pathophysiological mechanism underlying cortisol-dependent neuroendocrine diseases. (ox.ac.uk)
  • CRH did not influence the differentiation of isolated trophoblasts into functional syncytium as determined by beta-hCG secretion, albeit inducing syncytin-1 expression. (biomedcentral.com)
  • Following syncytialisation, CRH treatment significantly increased leptin and 11beta-HSD2 expression, as well as leptin secretion into culture supernatant after 48 h. (biomedcentral.com)
  • While somatotroph activation and glucagon secretion occur in a deferred manner 1, 4 . (medicinabuenosaires.com)
  • 8 reported that prolonged moderate-intensity running leads to elevations in sex hormone synthesis in the skeletal muscles, particularly 5α-reductase type 1 expression and DHT concentration. (e-pan.org)
  • Endocrine journal 2011 58 (11): 949-59. (cdc.gov)
  • Novel enzymological profiles of human 11beta-hydroxysteroid dehydrogenase type 1. (ox.ac.uk)
  • In conclusion, evidence is provided that human 11beta-HSD1 in vitro is involved in phase I reactions of anti-inflammatory non-steroidal drugs like ketoprofen and DFU-lactol. (ox.ac.uk)
  • The human gene for 11 beta-hydroxysteroid dehydrogenase. (wikipedia.org)
  • Amino acids 1-153 of human ER-beta expressed in E. coli. (genetex.com)
  • PDB-4fam: Crystal structure of human 17beta-hydroxysteroid dehydrogenase ty. (pdbj.org)
  • KD topics (10 sub-acute topics: 5 men, 5 females aged 2.0C15.5 years at time of study) and 6 convalescent subjects: 5 males, 1 female, aged 2.4C15.7 years at time of study) were evaluated by echocardiography through the severe admission with 2 and 6 weeks and 12 months following diagnosis. (forgetmenotinitiative.org)