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11β-Hydroxysteroid Dehydrogenase (11β-HSD)
- Target
- 11β-HSD
- Molecular classification
- Enzyme, Short-chain dehydrogenases/reductases superfamily
01
Overview
11β-Hydroxysteroid dehydrogenase (11β-HSD) refers to a family of enzymes that catalyze the interconversion between active and inactive glucocorticoids, specifically converting cortisone to cortisol, and vice versa. This regulation is crucial for controlling local glucocorticoid action at the tissue level. There are two main isozymes, type 1 (HSD11B1) and type 2 (HSD11B2), with distinct tissue expression and functions. Type 1 primarily acts as a reductase, converting cortisone to cortisol, while type 2 functions mainly as a dehydrogenase, converting cortisol to cortisone. Altered expression or function has been implicated in several conditions, including obesity, metabolic syndrome, and hypertension. Inhibitors targeting these enzymes are being explored for therapeutic potential against age-related diseases and metabolic disorders.
- Other names
- HSD-11βHSD11B1HSD11B2CORTRD2HDLSDR26C1
02
Mechanism of action
Inhibition of 11β-HSD enzymes, modulating local glucocorticoid concentrations and downstream receptor activation.
03
Biological functions
Regulation of glucocorticoid activityInterconversion of cortisol and cortisoneRegulation of mineralocorticoid receptor activationMetabolism of bile acidsMetabolism of neurosteroidsMetabolism of xenobioticsMetabolism of oxysterols
04
Disease associations
ObesityMetabolic syndromeHypertensionApparent mineralocorticoid excess syndromeAge-related diseases
05
Safety considerations
Potential for off-target effects due to broad substrate specificity.Disruption of normal glucocorticoid homeostasis.
06
Interacting drugs
Glycyrrhizinic acid (licorice)
1 more in the full profile.
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