11β-Hydroxysteroid dehydrogenase type 1, a target for development of oral antidiabetic drugs (Review)

11β-Hydroxysteroid dehydrogenase (11β-HSD1) is an enzyme that catalyses the transformation of the inactive glucocorticoid cortisone into active cortisol. A chronically elevated level of cortisol as a result of 11β-HSD1 hyperexpression in the liver and fatty tissue leads to the development of metabol...

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Bibliographic Details
Published in:Pharmaceutical chemistry journal 2013-05, Vol.47 (2), p.80-86
Main Authors: Lipson, V. V., Shirobokova, M. G., Petrova, O. N.
Format: Article
Language:English
Subjects:
Adipose tissues
Cortisone
Development and progression
Enzymes
Hypoglycemic agents
Medicine
Obesity
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Search for New Drugs
Type 2 diabetes
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Summary:11β-Hydroxysteroid dehydrogenase (11β-HSD1) is an enzyme that catalyses the transformation of the inactive glucocorticoid cortisone into active cortisol. A chronically elevated level of cortisol as a result of 11β-HSD1 hyperexpression in the liver and fatty tissue leads to the development of metabolic syndrome, obesity, insulin-resistance, type 2 diabetes mellitus (DM2), and cardiovascular complications. Inhibition of 11β-HSD1 is recognized as a promising strategy for reducing the activity of glucocorticoids on a tissue-specific level. Herein inhibitors 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.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-013-0900-y