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

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Pharmaceutical Chemistry Journal Aims and scope

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.

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Authors and Affiliations

  1. Danilevsky Institute of Endocrine Pathology Problems, National Academy of Medical Sciences of Ukraine, 61002, Kharkiv, Ukraine

    V. V. Lipson

  2. Institute for Single Crystals, National Academy of Sciences of Ukraine, 61001, Kharkiv, Ukraine

    M. G. Shirobokova & O. N. Petrova

  3. Karazin Kharkiv National University, 61002, Kharkiv, Ukraine

    V. V. Lipson

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  1. V. V. Lipson
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  2. M. G. Shirobokova
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  3. O. N. Petrova
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Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 47, No. 2, pp. 12 – 18, February, 2013.

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Lipson, V.V., Shirobokova, M.G. & Petrova, O.N. 11β-Hydroxysteroid dehydrogenase type 1, a target for development of oral antidiabetic drugs (Review). Pharm Chem J 47, 80–86 (2013). https://doi.org/10.1007/s11094-013-0900-y

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