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Pharmaceutical Chemistry Journal

, Volume 47, Issue 2, pp 80–86 | Cite as

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

  • V. V. Lipson
  • M. G. Shirobokova
  • O. N. Petrova
Search for New Drugs

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.

Keywords

11β-hydroxysteroid dehydrogenase cortisol metabolic syndrome obesity drug discovery 

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Copyright information

© Springer Science+Business Media New York 2013

Authors and Affiliations

  • V. V. Lipson
    • 1
    • 3
  • M. G. Shirobokova
    • 2
  • O. N. Petrova
    • 2
  1. 1.Danilevsky Institute of Endocrine Pathology ProblemsNational Academy of Medical Sciences of UkraineKharkivUkraine
  2. 2.Institute for Single CrystalsNational Academy of Sciences of UkraineKharkivUkraine
  3. 3.Karazin Kharkiv National UniversityKharkivUkraine

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