11β-HSD1
Yeast-based assays for screening 11β-HSD1 inhibitors
... (200 μg/ml). In the RVY102 assay strain, the N-degron fluorescent reporter protein construct (Evolva SA), con- trolled by GAL1 promoter was integrated as a single copy into the genome at the KIN1 locus of chromosome IV. ...
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11β HSD1 plays a critical role in trabecular bone loss associated with systemic glucocorticoid therapy
... Subcommittee). 11β-HSD1 KO mice were gener- ated as previously described through crossing HSD11B1 floxed mice with the ZP3-Cre expressing strain to achieve germline deletion of 11β-HSD1 ...or ...
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TNFα-mediated Hsd11b1 binding of NF-κB p65 is associated with suppression of 11β-HSD1 in muscle
... with all three depicted in Fig. 5B. ChIP analysis of samples amplified with primers for the putative p65-binding regions following p65 pull down indicated no enrichment of p65 binding in putative regions 1 and 3 in ...
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Biomarkers of hypothalamic-pituitary-adrenal axis activity in mice lacking 11β-HSD1 and H6PDH
... 11b-HSD1 and H6PDH KO mice have also been valuable in understanding the role of these enzymes in integrating GC metabolism and HPA activity. 11b-HSD1 KO mice have elevated plasma corticosterone and ACTH ...
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11β-HSD1 Modulates the Set Point of Brown Adipose Tissue Response to Glucocorticoids in Male Mice
... Glucocorticoids (GCs) are potent regulators of energy metabolism. Chronic GC exposure suppresses brown adipose tissue (BAT) thermogenic capacity in mice, with evidence for a similar effect in humans. Intracellular GC ...
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Differential glucocorticoid metabolism in patients with persistent versus resolving inflammatory arthritis
... here, it was impossible to determine the tissue that con- tributed most to the global measures of 11β-HSD1 activity used in this study. At a tissue level the amount of GC ex- posure will depend on both ...
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Differential expression, function and response to inflammatory stimuli of 11β hydroxysteroid dehydrogenase type 1 in human fibroblasts: a mechanism for tissue specific regulation of inflammation
... increased 11β-HSD1 activity was able to mediate autocrine regulation of the cytokine IL-6 in each of the different fibroblast types (Figure ...the 11β-HSD inhibitor glycyrrhetinic acid, sug- gesting ...
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11β Hydroxysteroid dehydrogenase – 1 activity in type 2 diabetes mellitus: a comparative study
... β HSD1 activity was significantly increased in those diabetes subjects, who exercise as compared to healthy subjects with same range of physical ...β HSD1 activity on > 180 min/week of ...induced ...
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11β-Hydroxysteroid dehydrogenase type 1 within muscle protects against the adverse effects of local inflammation
... the 11β-HSD1 gene (C) and the rate of generation of cortisol from cortisone (D) in differentiated human myotubes over a period of 16 h following 24 h of pretreatment with TNF-α (10 ng/ml), determined by ...
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Differential expression, function and response to inflammatory stimuli of 11β-hydroxysteroid dehydrogenase type 1 in human fibroblasts: a mechanism for tissue-specific regulation of inflammation
... enzyme 11β-hydroxyster- oid dehydrogenase type 1 (11β-HSD1), which is located on the luminal surface of the endoplasmic reticulum ...of 11β-HSD1 means that it has capacity for both ...
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The role of glucocorticoid action in the pathophysiology of the Metabolic Syndrome
... Both 11β-HSD1 and 11β-HSD2 are located at the endo- plasmic reticulum (ER) but with distinct ...topologies. 11β- HSD1 has one short N-terminal transmembrane region with the catalytic ...
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Hypertension in mice lacking 11β hydroxysteroid dehydrogenase type 2
... novel 11β-HSD isoform, this seems more likely merely to reflect 11β-HSD1, which may continue moderate activity without added NADP, probably due to use of endogenous cosubstrate NADP, itself increased ...
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11β Hydroxysteroid dehydrogenase blockade prevents age induced skin structure and function defects
... 11β-HSD1 protein detection in frozen human skin sec- tions (fixed in 3:1 acetone/ethanol) was analyzed by immunohistochemistry using a primary mAb (Abcam) and an alkaline phosphatase–conjugated goat ...
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Regulation of 11β Hydroxysteroid Dehydrogenase Type 1 and 2 in Rheumatoid Arthritis
... Over the 24 weeks period disease activity of RA de- creased significantly (median PV week 0 = 1.85 mPa (IQR 1.76 - 1.90), week 12 = 1.77 (IQR 1.71 - 1.89), week 24 = 1.77 (1.66 - 1.84), p < 0.01; median AI week 0 = 24 ...
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Increased Expression of 11β Hydroxysteroid Dehydrogenase Type 1 in Experimental Periodontitis Induced by Lipopolysaccharide from Porphyromonas gingivalis
... increased levels of intracellular active glucocorticoids. Although glucocorticoids usually exert anti-inflammatory effects [1], it has been reported that glucocorti- coids may have pro-inflammatory effects under chronic ...
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Luteinizing hormone induces expression of 11beta-hydroxysteroid dehydrogenase type 2 in rat Leydig cells
... of 11β-HSD1 in cultured Leydig cells, the reducase activity of 11β-HSD1 increased slightly and the oxidase activity declined ...of 11β-HSD1 ...of 11β-HSD1 activity ...
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Effect of Sugars on mRNA Expression of 11β-HSD1in the Hypothalamus of Rats after 24 hour Exposure
... However, how sugars affect the expression of hypothalamic 11β-HSD1 is not known yet. Different hypothalamic regions have differing effects on feeding behaviors(Schwartz, Woods, Porte, Seeley, & Baskin, ...
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The expression of 11β-hydroxysteroid dehydrogenase type 1 is increased in experimental periodontitis in rats
... of 11β-HSD1 in other chronic inflamma- tory diseases has been ...of 11β-HSD1 was demonstrated in inflammatory bowel diseases and rheumatoid arthritis [27–30], suggesting that the increased ...
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Idiopathic intracranial hypertension, hormones, and 11ß-hydroxysteroid dehydrogenases
... During a low calorie diet in IIH, while systemic cortisol levels remained within normal levels, urinary cortisol metabolites decreased (P = 0.001) with substantial weight loss (15 ⋅ 7 kg [standard deviation {SD} 8.0], ...
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Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects
... inhibiting 11β-hydroxylase at daily doses above 3 mg led to further development of LCI699 as a drug candidate for indications in which metyrapone is currently used, both for diagnosis and ...
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