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Journal articles on the topic '11Β-Hsd1 Inhibitors'

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Published: 2 June 2025

Last updated: 31 July 2025

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1

Zhao, Leping, Yong Pan, Kesong Peng та ін. "Inhibition of 11β-HSD1 by LG13 improves glucose metabolism in type 2 diabetic mice". Journal of Molecular Endocrinology 55, № 2 (2015): 119–31. http://dx.doi.org/10.1530/jme-14-0268.

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11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) controls the production of active glucocorticoid (GC) and has been proposed as a new target for the treatment of type 2 diabetes. We have previously reported that a natural product, curcumin, exhibited moderate inhibition and selectivity on 11β-HSD1. By analyzing the models of protein, microsome, cells and GCs-induced micein vitroandin vivo, this study presented a novel curcumin analog, LG13, as a potent selective 11β-HSD1 inhibitor.In vivo, Type 2 diabetic mice were treated with LG13 for 42 days to assess the pharmacological benefits of 11β-H

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2

Walker, Brian R. "Extra-adrenal regeneration of glucocorticoids by 11β-hydroxysteroid dehydrogenase type 1: physiological regulator and pharmacological target for energy partitioning". Proceedings of the Nutrition Society 66, № 1 (2007): 1–8. http://dx.doi.org/10.1017/s002966510700523x.

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The major glucocorticoid in man, cortisol, plays important roles in regulating fuel metabolism, energy partitioning and body fat distribution. In addition to the control of cortisol levels in blood by the hypothalamic–pituitary–adrenal axis, intracellular cortisol levels within target tissues can be controlled by local enzymes. 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyses the regeneration of active cortisol from inert cortisone, thereby amplifying cortisol levels and glucocorticoid receptor activation in adipose tissue, liver and other tissues. 11β-HSD1 is under complex tissue-

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3

Liu, Haifeng, Lingyu Li, Chunlei Zhang та ін. "11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor Development by Lentiviral Screening Based on Computational Modeling". Pharmacology 102, № 3-4 (2018): 169–79. http://dx.doi.org/10.1159/000491397.

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In this study, rat and human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have been cloned by lentiviral transduction and expressed by CHO-K1 cells. The results showed that recombinant plasmids contained R11bhsd1 or H11bhsd1 have been constructed, which is consistent with the gene bank respectively. A clone cell was selected with G418 and cultivated to express 11β-HSD1. 11β-HSD1 catalytic activity of rat and human were 99.5 and 98.7%, respectively, determined by scanning radiometer. And the cloned CHO-K1 cells expressed the protein of 11β-HSD1 in a long-term and stable manner, which make

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4

Arampatzis, Spyridon, Bert Kadereit, Daniela Schuster та ін. "Comparative enzymology of 11β-hydroxysteroid dehydrogenase type 1 from six species". Journal of Molecular Endocrinology 35, № 1 (2005): 89–101. http://dx.doi.org/10.1677/jme.1.01736.

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11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1), catalyzing the intracellular activation of cortisone to cortisol, is currently considered a promising target to treat patients with metabolic syndrome; hence, there is considerable interest in the development of selective inhibitors. For preclinical tests of such inhibitors, the characteristics of 11β-HSD1 from the commonly used species have to be known. Therefore, we determined differences in substrate affinity and inhibitor effects for 11β-HSD1 from six species. The differences in catalytic activities with cortisone and 11-dehydrocorticoste

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5

Harno, Erika, Elizabeth C. Cottrell, Alice Yu та ін. "11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors Still Improve Metabolic Phenotype in Male 11β-HSD1 Knockout Mice Suggesting Off-Target Mechanisms". Endocrinology 154, № 12 (2013): 4580–93. http://dx.doi.org/10.1210/en.2013-1613.

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The enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is a target for novel type 2 diabetes and obesity therapies based on the premise that lowering of tissue glucocorticoids will have positive effects on body weight, glycemic control, and insulin sensitivity. An 11β-HSD1 inhibitor (compound C) inhibited liver 11β-HSD1 by &gt;90% but led to only small improvements in metabolic parameters in high-fat diet (HFD)–fed male C57BL/6J mice. A 4-fold higher concentration produced similar enzyme inhibition but, in addition, reduced body weight (17%), food intake (28%), and glucose (22%). We

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6

Di Vincenzo, Mariangela, Pamela Pellegrino, Genny Schiappa та ін. "Role of 11β-Hydroxysteroid Dehydrogenase and Mineralocorticoid Receptor on Alzheimer’s Disease Onset: A Systematic Review". International Journal of Molecular Sciences 26, № 3 (2025): 1357. https://doi.org/10.3390/ijms26031357.

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The role of 11β-HSD1 in Alzheimer’s disease (AD) has garnered significant attention due to its involvement in glucocorticoid metabolism, neuroinflammation, and cognitive decline. This review explores the current understanding of 11β-HSD1 in AD, examining genetic, preclinical, and clinical research. Genetic studies have identified 11β-HSD1 polymorphisms that may influence AD risk, although findings remain inconsistent. Mechanistically, 11β-HSD1 promotes neurodegeneration through the dysregulation of glucocorticoid activity, contributing to hippocampal atrophy, amyloid plaque formation, and tau

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7

Cooper, Mark S., та Paul M. Stewart. "11β-Hydroxysteroid Dehydrogenase Type 1 and Its Role in the Hypothalamus-Pituitary-Adrenal Axis, Metabolic Syndrome, and Inflammation". Molecular Endocrinology 23, № 11 (2009): 1934. http://dx.doi.org/10.1210/mend.23.11.9999.

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ABSTRACT Context 11β-Hydroxysteroid dehydrogenase (11β-HSD) enzymes are now appreciated to be important regulators of hormone action at a tissue level. 11β-HSD1 is widely expressed and increases glucocorticoid action through its unique ability to convert inactive glucocorticoids (cortisone in man, 11-dehydrocorticosterone in rodents) to their active forms (cortisol and corticosterone, respectively). The enzyme has roles in the normal hypothalamus-pituitary-adrenal (HPA) axis, has been implicated in metabolic syndrome, and may modulate various aspects of the immune response. Evidence Acquisitio

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8

Lee, Jong Han, Zhanguo Gao та Jianping Ye. "Regulation of 11β-HSD1 expression during adipose tissue expansion by hypoxia through different activities of NF-κB and HIF-1α". American Journal of Physiology-Endocrinology and Metabolism 304, № 10 (2013): E1035—E1041. http://dx.doi.org/10.1152/ajpendo.00029.2013.

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11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) is involved in the pathogenesis of type 2 diabetes by generating active glucocorticoids (cortisol and corticosterone) that are strong inhibitors of angiogenesis. However, the mechanism of 11β-HSD1 gene expression and its relationship to adipose angiogenesis are largely unknown. To address this issue, we examined 11β-HSD1 expression in visceral and subcutaneous adipose tissue (AT) of diet-induced obese (DIO) mice during weight gain and investigated the gene regulation by hypoxia in vitro. 11β-HSD1 mRNA was reduced in the adipose tissues during

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9

Wang, Hong, Jianmin Sang, Zhongyao Ji та ін. "Bisphenol A Analogues Inhibit Human and Rat 11β-Hydroxysteroid Dehydrogenase 1 Depending on Its Lipophilicity". Molecules 28, № 13 (2023): 4894. http://dx.doi.org/10.3390/molecules28134894.

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Bisphenol A (BPA) analogues substituted on the benzene ring are widely used in a variety of industrial and consumer materials. However, their effects on the glucocorticoid-metabolizing enzyme 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) remain unclear. The inhibitory effects of 6 BPA analogues on the inhibition of human and rat 11β-HSD1 were investigated. The potencies of inhibition on human 11β-HSD1 were bisphenol H (IC50, 0.75 µM) > bisphenol G (IC50, 5.06 µM) > diallyl bisphenol A (IC50, 13.36 µM) > dimethyl bisphenol A (IC50, 30.18 µM) > bisphenol A dimethyl ether (IC50, 33.08

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10

Abrahams, Lianne, Nina M. Semjonous, Phil Guest та ін. "Biomarkers of hypothalamic–pituitary–adrenal axis activity in mice lacking 11β-HSD1 and H6PDH". Journal of Endocrinology 214, № 3 (2012): 367–72. http://dx.doi.org/10.1530/joe-12-0178.

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Glucocorticoid concentrations are a balance between production under the negative feedback control and diurnal rhythm of the hypothalamic–pituitary–adrenal (HPA) axis and peripheral metabolism, for example by the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which catalyses the reduction of inactive cortisone (11-dehydrocorticosterone (11-DHC) in mice) to cortisol (corticosterone in mice). Reductase activity is conferred upon 11β-HSD1 by hexose-6-phosphate dehydrogenase (H6PDH). 11β-HSD1 is implicated in the development of obesity, and selective 11β-HSD1 inhibitors are currently u

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Ishii-Yonemoto, Takako, Hiroaki Masuzaki, Shintaro Yasue та ін. "Glucocorticoid reamplification within cells intensifies NF-κB and MAPK signaling and reinforces inflammation in activated preadipocytes". American Journal of Physiology-Endocrinology and Metabolism 298, № 5 (2010): E930—E940. http://dx.doi.org/10.1152/ajpendo.00320.2009.

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Increased expression and activity of the intracellular glucocorticoid-reactivating enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) contribute to dysfunction of adipose tissue. Although the pathophysiological role of 11β-HSD1 in mature adipocytes has long been investigated, its potential role in preadipocytes still remains obscure. The present study demonstrates that the expression of 11β-HSD1 in preadipocyte-rich stromal vascular fraction (SVF) cells in fat depots from ob/ob and diet-induced obese mice was markedly elevated compared with lean control. In 3T3-L1 preadipocytes, the lev

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12

Tiganescu, Ana, Melanie Hupe, Yoshikazu Uchida, Theodora Mauro, Peter M. Elias, and Walter M. Holleran. "Increased glucocorticoid activation during mouse skin wound healing." Journal of Endocrinology 221, no. 1 (2014): 51–61. http://dx.doi.org/10.1530/joe-13-0420.

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Glucocorticoid (GC) excess inhibits wound healing causing increased patient discomfort and infection risk. 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) activates GCs (converting 11-dehydrocorticosterone to corticosterone in rodents) in many tissues including skin, wherede novosteroidogenesis from cholesterol has also been reported. To examine the regulation of 11β-HSD1 and steroidogenic enzyme expression during wound healing, 5 mm wounds were generated in female SKH1 mice and compared at days 0, 2, 4, 8, 14, and 21 relative to unwounded skin. 11β-HSD1 expression (mRNA and protein) and en

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13

Singh, Rahul, Vijay Kumar Bhardwaj, Pralay Das та Rituraj Purohit. "Identification of 11β-HSD1 inhibitors through enhanced sampling methods". Chemical Communications 58, № 32 (2022): 5005–8. http://dx.doi.org/10.1039/d1cc06894f.

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14

Morris, David J., Syed A. Latif, Michael D. Rokaw, Charles O. Watlington, and John P. Johnson. "A second enzyme protecting mineralocorticoid receptors from glucocorticoid occupancy." American Journal of Physiology-Cell Physiology 274, no. 5 (1998): C1245—C1252. http://dx.doi.org/10.1152/ajpcell.1998.274.5.c1245.

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We have confirmed that A6 cells (derived from kidney of Xenopus laevis), which contain both mineralocorticoid and glucocorticoid receptors, do not normally possess 11β-hydroxysteroid dehydroxgenase (11β-HSD1 or 11β-HSD2) enzymatic activity and so are without apparent “protective” enzymes. A6 cells do not convert the glucocorticoid corticosterone to 11-dehydrocorticosterone but do, however, possess steroid 6β-hydroxylase that transforms corticosterone to 6β-hydroxycorticosterone. This hydroxylase is cytochrome P-450 3A (CYP3A). We have now determined the effects of 3α,5β-tetrahydroprogesterone

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15

Park, Ji Seon, Su Jung Bae, Sik-Won Choi та ін. "A novel 11β-HSD1 inhibitor improves diabesity and osteoblast differentiation". Journal of Molecular Endocrinology 52, № 2 (2014): 191–202. http://dx.doi.org/10.1530/jme-13-0177.

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Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential as treatment for osteoporosis as well as metabolic syndrome including type 2 diabetes mellitus. Here, we investigated the anti-diabetic, anti-adipogenic, and anti-osteoporotic activity of KR-67500, as a novel selective 11β-HSD1 inhibitor. Cellular 11β-HSD1 activity was tested based on a homogeneous time-resolved fluorescence method. Oral glucose tolerance test (OGTT) and insulin tolerance test (ITT) levels were measured in diet-induced obese (DIO)-C57BL/6 mice administered KR-67500 (50 mg/kg

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Han, Mei-Ling, Yu Shen, Guo-Cai Wang, Ying Leng, Hua Zhang та Jian-Min Yue. "11β-HSD1 Inhibitors from Walsura cochinchinensis". Journal of Natural Products 76, № 7 (2013): 1319–27. http://dx.doi.org/10.1021/np400260g.

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17

Wang, Minghan. "Glucocorticoid antagonists and 11β-HSD1 inhibitors". Drug Discovery Today: Therapeutic Strategies 4, № 2 (2007): 117–22. http://dx.doi.org/10.1016/j.ddstr.2007.10.001.

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18

Sooy, Karen, June Noble, Andrew McBride та ін. "Cognitive and Disease-Modifying Effects of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibition in Male Tg2576 Mice, a Model of Alzheimer's Disease". Endocrinology 156, № 12 (2015): 4592–603. http://dx.doi.org/10.1210/en.2015-1395.

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Chronic exposure to elevated levels of glucocorticoids has been linked to age-related cognitive decline and may play a role in Alzheimer's disease. In the brain, 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) amplifies intracellular glucocorticoid levels. We show that short-term treatment of aged, cognitively impaired C57BL/6 mice with the potent and selective 11β-HSD1 inhibitor UE2316 improves memory, including after intracerebroventricular drug administration to the central nervous system alone. In the Tg2576 mouse model of Alzheimer's disease, UE2316 treatment of mice aged 14 months for

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19

Osman, Doaa A., Mario A. Macías, Lamya H. Al-Wahaibi та ін. "Structural Insights and Docking Analysis of Adamantane-Linked 1,2,4-Triazole Derivatives as Potential 11β-HSD1 Inhibitors". Molecules 26, № 17 (2021): 5335. http://dx.doi.org/10.3390/molecules26175335.

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The solid-state structural analysis and docking studies of three adamantane-linked 1,2,4-triazole derivatives are presented. Crystal structure analyses revealed that compound 2 crystallizes in the triclinic P-1 space group, while compounds 1 and 3 crystallize in the same monoclinic P21/c space group. Since the only difference between them is the para substitution on the aryl group, the electronic nature of these NO2 and halogen groups seems to have no influence over the formation of the solid. However, a probable correlation with the size of the groups is not discarded due to the similar inter

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Hardy, Rowan S., Hannah Botfield, Keira Markey та ін. "11βHSD1 Inhibition with AZD4017 Improves Lipid Profiles and Lean Muscle Mass in Idiopathic Intracranial Hypertension". Journal of Clinical Endocrinology & Metabolism 106, № 1 (2020): 174–87. http://dx.doi.org/10.1210/clinem/dgaa766.

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Abstract Background The enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) determines prereceptor metabolism and activation of glucocorticoids within peripheral tissues. Its dysregulation has been implicated in a wide array of metabolic diseases, leading to the development of selective 11β-HSD1 inhibitors. We examined the impact of the reversible competitive 11β-HSD1 inhibitor, AZD4017, on the metabolic profile in an overweight female cohort with idiopathic intracranial hypertension (IIH). Methods We conducted a UK multicenter phase II randomized, double-blind, placebo-controlled trial

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Hassan, Abdullahi M., Abdullahi H. Sadiya, Kuje E. Jafaru та Haruna G. Sunday. "In-silico Investigation of Potential Inhibitors of 11-β-Hydroxysteroid Dehydrogenase". Asian Journal of Biochemistry, Genetics and Molecular Biology 15, № 2 (2023): 10–23. http://dx.doi.org/10.9734/ajbgmb/2023/v15i2329.

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Diabetes mellitus is a chronic disease plagued with insufficient insulin production or insulin resistance. New targets and disease pathways are emerging and one such is the 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) which catalyses the intracellular conversion of inert cortisone to physiologically active cortisol, functioning to enhance local cortisol action beyond what would be predicted based on simple plasma exposures. This study aimed at exploring the anti-diabetic potential of the bioactive compounds found in Carica papaya. In this study, 59 natural compounds were obtained from li

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Chapman, Karen, Megan Holmes та Jonathan Seckl. "11β-Hydroxysteroid Dehydrogenases: Intracellular Gate-Keepers of Tissue Glucocorticoid Action". Physiological Reviews 93, № 3 (2013): 1139–206. http://dx.doi.org/10.1152/physrev.00020.2012.

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Glucocorticoid action on target tissues is determined by the density of “nuclear” receptors and intracellular metabolism by the two isozymes of 11β-hydroxysteroid dehydrogenase (11β-HSD) which catalyze interconversion of active cortisol and corticosterone with inert cortisone and 11-dehydrocorticosterone. 11β-HSD type 1, a predominant reductase in most intact cells, catalyzes the regeneration of active glucocorticoids, thus amplifying cellular action. 11β-HSD1 is widely expressed in liver, adipose tissue, muscle, pancreatic islets, adult brain, inflammatory cells, and gonads. 11β-HSD1 is selec

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Sunak, Neera, Daphne F. Green, Lalantha R. Abeydeera, Lisa M. Thurston та Anthony E. Michael. "Implication of cortisol and 11β-hydroxysteroid dehydrogenase enzymes in the development of porcine (Sus scrofa domestica) ovarian follicles and cysts". Reproduction 133, № 6 (2007): 1149–58. http://dx.doi.org/10.1530/rep-07-0003.

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This study investigated cortisol inactivation by 11β-hydroxysteroid dehydrogenase (11β HSD) enzymes in porcine granulosa cells from antral follicles at different developmental stages and in ovarian cysts. In granulosa cells, cortisol oxidation increased threefold with antral follicle diameter (P < 0.001). This trend was paralleled by a threefold increase in NADP+-dependent 11β-dehydrogenase activity in granulosa cell homogenates with follicle diameter. Intact granulosa cells from ovarian cysts exhibited significantly lower enzyme activities than cells from large antral follicles. Neither in

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Bini, Jason, Jean-Dominique Gallezot, Songye Li та ін. "RF12 | PSUN106 Quantifying Liver and Brain Levels of 11β-hydroxysteroid Dehydrogenase Type 1 in Obesity Using Positron Emission Tomography Imaging". Journal of the Endocrine Society 6, Supplement_1 (2022): A29—A30. http://dx.doi.org/10.1210/jendso/bvac150.062.

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Abstract Objectives Cortisol is known to promote adipocyte differentiation and maturation, and prolonged exposure to excess cortisol contributes to the development of obesity and metabolic dysregulation. The intracellular 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme catalyzes the conversion of inactive cortisone to active cortisol. Recently, we demonstrated reduced brain 11β-HSD1 levels in vivo with increasing body mass index (BMI), using positron emission tomography (PET) radioligands [11C]- and [18F]AS2471907(1). PET imaging can simultaneously quantify uptake in multiple organs

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Quiroga, Diego. "Employing Molecular Docking Calculations for the Design of Alkyl (2-Alcoxy-2-Hydroxypropanoyl)-L-Tryptophanate Derivatives as Potential Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)". Reactions 4, № 1 (2023): 108–16. http://dx.doi.org/10.3390/reactions4010006.

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In this paper, we presented the design by computational tools of novel alkyl (2-alcoxy-2-hydroxypropanoyl)-L-tryptophanate derivatives, which can be potential inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The molecular structure optimization of a group of 36 compounds was performed employing DFT-B3LYP calculations at the level 6-311G(d,p). Then, molecular docking calculations were performed using Autodock tools software, employing the Lamarckian genetic algorithm (LGA). Four parameters (binding, intermolecular and Van Der Waals hydrogen bonding desolvation energies, and HOM

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Almeida, Cristiana, Cristina Monteiro та Samuel Silvestre. "Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 as Potential Drugs for Type 2 Diabetes Mellitus—A Systematic Review of Clinical and In Vivo Preclinical Studies". Scientia Pharmaceutica 89, № 1 (2021): 5. http://dx.doi.org/10.3390/scipharm89010005.

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Diabetes mellitus is a pathology with increasing frequency in society, being one of the main causes of death worldwide. For this reason, new therapeutic targets have been studied over the years. 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is an enzyme responsible for reducing cortisone to its active form cortisol, which can lead to metabolic changes such as insulin resistance and hyperglycemia. Therefore, 11β-HSD1 inhibition may offer a new therapeutic approach for type 2 diabetes mellitus. This work intends to systematically review the available scientific evidence on this subject. For

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Shah, Unmesh, Craig D. Boyle, Samuel Chackalamannil та ін. "Azabicyclic sulfonamides as potent 11β-HSD1 inhibitors". Bioorganic & Medicinal Chemistry Letters 20, № 5 (2010): 1551–54. http://dx.doi.org/10.1016/j.bmcl.2010.01.082.

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Kupczyk, Daria, Rafał Bilski, Mariusz Kozakiewicz та ін. "11β-HSD as a New Target in Pharmacotherapy of Metabolic Diseases". International Journal of Molecular Sciences 23, № 16 (2022): 8984. http://dx.doi.org/10.3390/ijms23168984.

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Glucocorticoids (GCs), which are secreted by the adrenal cortex, are important regulators in the metabolism of carbohydrates, lipids, and proteins. For the proper functioning of the body, strict control of their release is necessary, as increased GCs levels may contribute to the development of obesity, type 2 diabetes mellitus, hypertension, cardiovascular diseases, and other pathological conditions contributing to the development of metabolic syndrome. 11β-hydroxysteroid dehydrogenase type I (11β-HSD1) locally controls the availability of the active glucocorticoid, namely cortisol and cortico

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Yu, Jin-Hai, Yu Shen, Yan Wu, Ying Leng, Hua Zhang та Jian-Min Yue. "Ricinodols A–G: new tetracyclic triterpenoids as 11β-HSD1 inhibitors from Ricinodendron heudelotii". RSC Advances 5, № 34 (2015): 26777–84. http://dx.doi.org/10.1039/c5ra01857a.

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Donarska, Beata, Joanna Cytarska, Dominika Kołodziej-Sobczak та ін. "Synthesis of Carborane–Thiazole Conjugates as Tyrosinase and 11β-Hydroxysteroid Dehydrogenase Inhibitors: Antiproliferative Activity and Molecular Docking Studies". Molecules 29, № 19 (2024): 4716. http://dx.doi.org/10.3390/molecules29194716.

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The presented study depicts the synthesis of 11 carborane–thiazole conjugates with anticancer activity, as well as an evaluation of their biological activity as inhibitors of two enzymes: tyrosinase and 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The overexpression of tyrosinase results in the intracellular accumulation of melanin and can be observed in melanoma. The overexpression of 11β-HSD1 results in an elevation of glucocorticoid levels and has been associated with the aggravation of metabolic disorders such as type II diabetes mellitus and obesity. Recently, as the comorbidity of

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Kupczyk, Daria, Renata Studzińska, Rafał Bilski та Alina Woźniak. "Application of ELISA Technique and Human Microsomes in the Search for 11β-Hydroxysteroid Dehydrogenase Inhibitors". BioMed Research International 2019 (12 травня 2019): 1–8. http://dx.doi.org/10.1155/2019/5747436.

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The metabolic syndrome is defined by impaired carbohydrate metabolism and lipid disorders and often accompanied by hypertension, all of which will lead to obesity and insulin resistance. Glucocorticoids play a regulatory role in the metabolism of proteins, lipids, and carbohydrates. There is growing evidence for a role of glucocorticoids in the development of the metabolic syndrome. The most important factor that regulates the access of endogenous glucocorticoids to receptors after release of glucocorticoids and their diffusion into the cytoplasm of target cells is the steroid metabolism invol

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Yeh, Vince S. C., Ravi Kurukulasuriya, Steven Fung та ін. "Discovery of orally active butyrolactam 11β-HSD1 inhibitors". Bioorganic & Medicinal Chemistry Letters 16, № 21 (2006): 5555–60. http://dx.doi.org/10.1016/j.bmcl.2006.08.034.

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Scott, James S., Frederick W. Goldberg та Andrew V. Turnbull. "Medicinal Chemistry of Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)". Journal of Medicinal Chemistry 57, № 11 (2013): 4466–86. http://dx.doi.org/10.1021/jm4014746.

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Kotha, Sambasivarao, and Sunil Pulletikurti. "Synthesis of propellanes containing a bicyclo[2.2.2]octene unitviathe Diels–Alder reaction and ring-closing metathesis as key steps." RSC Advances 8, no. 27 (2018): 14906–15. http://dx.doi.org/10.1039/c8ra02687d.

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A simple and convenient method to synthesize propellane derivatives containing a bicyclo[2.2.2]octene unit which are structurally similar to 11β-HSD1 inhibitors by sequential usage of the Diels–Alder reaction, C-allylation and ring-closing metathesis (RCM) is reported.

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Lipson, V. V., V. V. Borodina, R. G. Redkin, N. V. Svetlichnaya, and T. A. Zubatyuk. "THE SCREENING IN SILICO OF POTENTIAL 11-HYDROXYSTEROIDDEHYDROGENASE 1 INHIBITORS." Problems of Endocrine Pathology 55, no. 1 (2016): 56–62. http://dx.doi.org/10.21856/j-pep.2016.1.08.

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It was conducted the virtual screening by molecular docking with the program AutoDoc 4.2. for 27 000 structures of nitrogen and sulfur containing heterocyclic compounds has been carried out in order to identify of the enzyme 11β-hydroxysteroiddehydrogenase (11β-HSD1) inhibitors among them. It was established that spiro(pyrrolidin-3,2’-oxindoles), molecules of which have the residues of sulfurcontaining amino acids have been demonstrated in silico the greatest affinity to the specified target. We concluded of the expediency of these substances synthesis, and their anti-diabetic properties were

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Mostefaoui, L., F. Mesli, M. Merad та S. Ghalem. "Virtual screening of triazoles inhibitors of 11β-hydroxysteroid dehydrogenaseenzymes using -ADME-moleculardocking, and molecular dynamics simulation studies". Journal of Fundamental and Applied Sciences 12, № 2 (2023): 712–27. http://dx.doi.org/10.4314/jfas.v12i2.13.

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Hypertension, or elevated arterial blood pressure, is a substantial public health problem. The two 11β hydroxysteroid dehydrogenase (11β HSD) isozymes catalyze the interconversion of cortisol and cortisone. Our research consists in studying the inhibition of the enzymes with some derivatives of 1,2,4 triazoles by means of molecular docking and dynamics approaches. The interactions between the studied inhibitors and our target were further explored through molecular docking and molecular dynamics simulations, in the presence of water molecules. The molecular dynamics study was done for the best

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37

Yuan, Chester, David J. St. Jean, Qingyian Liu та ін. "The discovery of 2-anilinothiazolones as 11β-HSD1 inhibitors". Bioorganic & Medicinal Chemistry Letters 17, № 22 (2007): 6056–61. http://dx.doi.org/10.1016/j.bmcl.2007.09.070.

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Lee, Jin Hee, Nam Sook Kang та Sung-Eun Yoo. "Docking-based 3D-QSAR study for 11β-HSD1 inhibitors". Bioorganic & Medicinal Chemistry Letters 18, № 7 (2008): 2479–90. http://dx.doi.org/10.1016/j.bmcl.2008.02.042.

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Ghalem, Said, Mostefaoui Larbi, Meriem Merad та Benmiloud kamal. "Molecular docking of 11β-HSD1 with (1,2,4-triazole derivatives) inhibitors in a solvated medium". SDRP Journal of Computational Chemistry & Molecular Modelling 2, № 2 (2018): 1–8. http://dx.doi.org/10.25177/jccmm.2.2.1.

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Mi, Yabing, Wangsheng Wang, Jiangwen Lu, et al. "Proteasome-mediated degradation of collagen III by cortisol in amnion fibroblasts." Journal of Molecular Endocrinology 60, no. 2 (2018): 45–54. http://dx.doi.org/10.1530/jme-17-0215.

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Rupture of fetal membranes (ROM) can initiate parturition at both term and preterm. Collagen III in the compact layer of the amnion contributes to the tensile strength of fetal membranes. However, the upstream signals triggering collagen III degradation remain mostly elusive. In this study, we investigated the role of cortisol regenerated by 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) in collagen III degradation in human amnion fibroblasts with an aim to seek novel targets for the prevention of preterm premature ROM (pPROM)-elicited preterm birth. Human amnion tissue and cultured amnion tiss

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Yu, Jin-Hai, Yu Shen, Hong-Bing Liu, Ying Leng, Hua Zhang та Jian-Min Yue. "Dammarane-type triterpenoids as 11β-HSD1 inhibitors from Homonoia riparia". Org. Biomol. Chem. 12, № 26 (2014): 4716–22. http://dx.doi.org/10.1039/c4ob00807c.

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Neelamkavil, Santhosh F., Craig D. Boyle, Samuel Chackalamannil, William J. Greenlee, Lili Zhang та Giuseppe Terracina. "The discovery of azepane sulfonamides as potent 11β-HSD1 inhibitors". Bioorganic & Medicinal Chemistry Letters 19, № 16 (2009): 4563–65. http://dx.doi.org/10.1016/j.bmcl.2009.07.003.

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Cheng, Hengmiao, Jacqui Hoffman, Phuong Le та ін. "The development and SAR of pyrrolidine carboxamide 11β-HSD1 inhibitors". Bioorganic & Medicinal Chemistry Letters 20, № 9 (2010): 2897–902. http://dx.doi.org/10.1016/j.bmcl.2010.03.032.

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Webster, Scott P., Peter Ward, Margaret Binnie та ін. "Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors". Bioorganic & Medicinal Chemistry Letters 17, № 10 (2007): 2838–43. http://dx.doi.org/10.1016/j.bmcl.2007.02.057.

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Wang, Guo-Cai, Jin-Hai Yu, Yu Shen, Ying Leng, Hua Zhang та Jian-Min Yue. "Limonoids and Triterpenoids as 11β-HSD1 Inhibitors from Walsura robusta". Journal of Natural Products 79, № 4 (2016): 899–906. http://dx.doi.org/10.1021/acs.jnatprod.5b00952.

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Tice, Colin M., Wei Zhao, Paula M. Krosky та ін. "Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1". Bioorganic & Medicinal Chemistry Letters 20, № 22 (2010): 6725–29. http://dx.doi.org/10.1016/j.bmcl.2010.08.142.

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Yan, Xuelei, Zhulun Wang, Athena Sudom та ін. "The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors". Bioorganic & Medicinal Chemistry Letters 20, № 23 (2010): 7071–75. http://dx.doi.org/10.1016/j.bmcl.2010.09.097.

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Morgan, Stuart A., Zaki K. Hassan-Smith, Craig L. Doig, Mark Sherlock, Paul M. Stewart та Gareth G. Lavery. "Glucocorticoids and 11β-HSD1 are major regulators of intramyocellular protein metabolism". Journal of Endocrinology 229, № 3 (2016): 277–86. http://dx.doi.org/10.1530/joe-16-0011.

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The adverse metabolic effects of prescribed and endogenous glucocorticoid excess, ‘Cushing’s syndrome’, create a significant health burden. While skeletal muscle atrophy and resultant myopathy is a clinical feature, the molecular mechanisms underpinning these changes are not fully defined. We have characterized the impact of glucocorticoids upon key metabolic pathways and processes regulating muscle size and mass including: protein synthesis, protein degradation, and myoblast proliferation in both murine C2C12 and human primary myotube cultures. Furthermore, we have investigated the role of pr

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Sun, Daqing, Zhulun Wang, Yongmei Di та ін. "Discovery and Initial SAR of Arylsulfonylpiperazine Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1)". Bioorganic & Medicinal Chemistry Letters 18, № 12 (2008): 3513–16. http://dx.doi.org/10.1016/j.bmcl.2008.05.025.

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Chen, Xuan-Qin, Li-Dong Shao, Mahesh Pal та ін. "Hupehenols A–E, Selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors from Viburnum hupehense". Journal of Natural Products 78, № 2 (2015): 330–34. http://dx.doi.org/10.1021/np500896n.

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