11-Beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors in Type 2 diabetes mellitus and obesity

@article{Hughes200811BetahydroxysteroidDT,
  title={11-Beta-hydroxysteroid dehydrogenase type 1 (11$\beta$-HSD1) inhibitors in Type 2 diabetes mellitus and obesity},
  author={Katherine A. Hughes and Scott Peter Webster and Brian R. Walker},
  journal={Expert Opinion on Investigational Drugs},
  year={2008},
  volume={17},
  pages={481 - 496}
}
Background: Glucocorticoids such as cortisol are important regulators of fuel metabolism during starvation and stress. Chronic glucocorticoid excess induces obesity with multiple features of the metabolic syndrome. Objective: In this article, we review the importance of glucocorticoids in metabolic syndrome and the approaches that have been explored to reduce glucocorticoid action as the basis for novel therapy of Type 2 diabetes and obesity. Method: We focus on the enzyme 11-beta… 
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11β-Hydroxysteroid dehydrogenase type 1, a target for development of oral antidiabetic drugs (Review)
TLDR
Inhibition of 11β-HSD1, representatives of several types of N-containing heterocycles at various research stages, are reviewed as potential drugs influencing metabolic syndrome, DM2, and obesity.
11β-hydroxysteroid dehydrogenase type 1 inhibitors: a review of recent patents
TLDR
This review covers the recent 11β-HSD1 patent literature and clinical activity ranging from late 2007 through the end of 2008, as a number of structural classes have been reported by several pharmaceutical companies over the past 16 months.
11β-Hydroxysteroid dehydrogenase type 1 is an important regulator at the interface of obesity and inflammation
  • C. A. Staab, E. Maser
  • Biology, Medicine
    The Journal of Steroid Biochemistry and Molecular Biology
  • 2010
Obesity and corticosteroids: 11β-Hydroxysteroid type 1 as a cause and therapeutic target in metabolic disease
  • N. Morton
  • Biology, Medicine
    Molecular and Cellular Endocrinology
  • 2010
Discovery of novel inhibitors of human 11β-hydroxysteroid dehydrogenase type 1
11β-Hydroxysteroid Dehydrogenase Type 1 and the Metabolic Syndrome
TLDR
Evidence is being gathered not only on the relevance of such enzymes to GC physiological actions but also on their involvement in the pathophysiology of certain chronic disease states, in which circulating GC levels are not necessarily altered.
11-Dehydrocorticosterone causes metabolic syndrome, which is prevented when 11β-HSD1 is knocked out in livers of male mice.
Metabolic syndrome is growing in importance with the rising levels of obesity, type 2 diabetes, and insulin resistance. Metabolic syndrome shares many characteristics with Cushing's syndrome, which…
Overexpression of 11β-Hydroxysteroid Dehydrogenase Type 1 in Hepatic and Visceral Adipose Tissue is Associated with Metabolic Disorders in Morbidly Obese Patients
TLDR
The observed correlations between hepatic and VAT 11β-HSD1 expression with dyslipidemia and insulin resistance suggest that this enzyme might have a pathogenic role in obesity and related metabolic disorders.
The role of 11β-hydroxysteroid dehydrogenase type 1 in bile acid homeostasis
TLDR
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 11 β- HSD1 function.
Selective inhibition of 11β-hydroxysteroid dehydrogenase 1 by 18α-glycyrrhetinic acid but not 18β-glycyrrhetinic acid
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References

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TLDR
This patent review focuses on the large number of patents published since 2005 and 11β-HSD1, an important target for the treatment of the metabolic syndrome and cognitive impairment, with many companies pursuing the development of inhibitors.
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TLDR
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TLDR
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TLDR
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TLDR
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