Relevant bibliographies by topics / 11Β-Hsd1 Inhibitors

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  1. Journal articles
  2. Dissertations / Theses
  3. Book chapters
  4. Conference papers

Academic literature on the topic '11Β-Hsd1 Inhibitors'

Author: Grafiati
Published: 2 June 2025
Last updated: 31 July 2025

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

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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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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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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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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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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 >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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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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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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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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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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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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Dissertations / Theses on the topic "11Β-Hsd1 Inhibitors"

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Leiva, Martínez Rosana. "Polycyclic group optimization in 11β-HSD1 inhibitors and their pharmacological evaluation". Doctoral thesis, Universitat de Barcelona, 2017. http://hdl.handle.net/10803/457770.

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The present PhD Thesis evolves around the design, synthesis and pharmacological evaluation of novel 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors. Given that the enzyme active site includes a hydrophobic pocket to accommodate bulky lipophilic scaffolds, the main objective was focused on the study of new 11β-HSD1 inhibitors exploring different hydrophobic polycyclic substituents. 11β-HSD1 catalyzes the cortisol regeneration from its inactive form cortisone in tissues mainly expressing glucocorticoid (GC) receptors, such as liver, adipose and brain. GCs are well known hormones t
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Adie, Jillian E. "Structure-based drug design of 11β-hydroxysteroid dehydrogenase type 1 inhibitors". Thesis, University of Edinburgh, 2010. http://hdl.handle.net/1842/4673.

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The enzyme 11β-Hydroxysteroid Dehydrogenase 1 (11β-HSD1) catalyses the intracellular biosynthesis of the active glucocorticoid cortisol. Tissue specific dysregulation of the enzyme has been implicated in the development of metabolic syndrome and other associated diseases. Experiments with transgenic mice and prototype inhibitors show that inhibition of 11β-HSD1 in visceral adipose tissue and liver leads to a resistance of diet-induced hyperglycemia and a favourable lipid and lipoprotein profile as compared to controls. 11β-HSD1 inhibition has thus been proposed as an effective strategy to decr
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Book chapters on the topic "11Β-Hsd1 Inhibitors"

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Scott*, James S., and Jasen Chooramun. "Chapter 5. 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors in Development." In Drug Discovery. Royal Society of Chemistry, 2012. http://dx.doi.org/10.1039/9781849735322-00109.

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Paderes, Genevieve D., Klaus Dress, Buwen Huang, Jeff Elleraas, Paul A. Rejto, and Tom Pauly. "Structure-Based and Property-Compliant Library Design of 11β-HSD1 Adamantyl Amide Inhibitors." In Methods in Molecular Biology. Humana Press, 2010. http://dx.doi.org/10.1007/978-1-60761-931-4_10.

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Edwards, Christopher. "Perspective Chapter: A New View of the Endocrinology of Pregnancy and Parturition – Lessons from the Literature." In New Perspectives in Human Embryology [Working Title]. IntechOpen, 2024. http://dx.doi.org/10.5772/intechopen.1005047.

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Human and sheep parturition are more akin than currently recognised. In both glucocorticoids are key. The difference being mechanisms controlling glucocorticoid levels. Sheep have low cortisol during pregnancy which rise at term: humans control local glucocorticoid levels via the fetal adrenal and DHEA-sulphate. This increases 11β-HSD2 expression protecting the fetus from maternal cortisol by converting this to cortisone. During pregnancy DHEA inhibits placental and fetal membrane 11β-HSD1 expression. This plus hexose-6-phosphate dehydrogenase inhibition decreases 11β-HSD1 oxido-reductase/incr
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Fuerst-Recktenwald, Sabine, Markus Abt, and Wiebke Arlt. "Effects of Two 11β-HSD1 Inhibitors on the Hypothalamo-Pituitary-Adrenal Axis of Male and Female Type 2 Diabetic Patients." In CLINICAL - MODY & More. The Endocrine Society, 2011. http://dx.doi.org/10.1210/endo-meetings.2011.part4.or11.or39-4.

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Conference papers on the topic "11Β-Hsd1 Inhibitors"

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Nikmaturrohana, Qurin, Sri Rahayu Lestari та Betty Lukiati. "Potential of single bulb garlic (Allium sativum) active compound as an 11β-HSD1 inhibitor in obesity through in silico method". У PROCEEDINGS OF THE 3RD INTERNATIONAL SEMINAR ON METALLURGY AND MATERIALS (ISMM2019): Exploring New Innovation in Metallurgy and Materials. AIP Publishing, 2020. http://dx.doi.org/10.1063/5.0002532.

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