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Active site variability of type 1 11beta-hydroxysteroid dehydrogenase revealed by selective inhibitors and cross-species comparisons.

Abstract:

The NADPH-dependent enzyme type 1 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) activates in a tissue-specific manner circulating pro-glucocorticoid hormones (cortisone in humans) to the 11beta-OH ligand (cortisol in humans), which is able to bind to its cognate receptor and regulate gene transcription. Modulation of this pre-receptor activation mechanism by selective enzyme inhibitors is a desirable goal in the treatment of insulin resistance and related metabolic disorders. Like most ot...

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Publication status:
Published

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Publisher copy:
10.1016/j.mce.2005.11.043

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Journal:
Molecular and cellular endocrinology
Volume:
248
Issue:
1-2
Pages:
26-33
Publication date:
2006-03-01
DOI:
EISSN:
1872-8057
ISSN:
0303-7207
Source identifiers:
108336

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