Target intelligence / Profile preview

Corticosteroid 11-beta-dehydrogenase (11-beta-HSD) (11-beta-HSD)

Target
11-beta-HSD
Molecular classification
Enzyme, Oxidoreductase, Short-chain dehydrogenase/reductase family
01

Overview

Corticosteroid 11-beta-dehydrogenase, also known as 11-beta-hydroxysteroid dehydrogenase (11-beta-HSD), is a family of enzymes that catalyze the interconversion of active glucocorticoids, such as cortisol, and their inactive 11-keto metabolites, such as cortisone (Source: UniProt P28845). There are two primary isoforms: Type 1 (11-beta-HSD1), which acts mainly as a reductase to regenerate cortisol in the liver and adipose tissue, and Type 2 (11-beta-HSD2), which acts as a dehydrogenase to inactivate cortisol in the kidney (Source: PubMed PMID: 23510150). This enzymatic activity is essential for regulating local glucocorticoid concentrations and protecting the mineralocorticoid receptor from inappropriate activation by cortisol (Source: StatPearls, 'Apparent Mineralocorticoid Excess'). Dysregulation of these enzymes is strongly linked to metabolic disorders, including obesity and type 2 diabetes, as well as cardiovascular conditions like hypertension (Source: NIH, PMC3010339). Pharmacological research focuses on selective 11-beta-HSD1 inhibitors to improve insulin sensitivity and reduce adiposity, while non-selective inhibition is associated with electrolyte imbalances (Source: PubChem). These enzymes serve as critical gatekeepers for tissue-specific steroid hormone action.

Other names
11-beta-hydroxysteroid dehydrogenaseHSD11BCortisone reductase11-oxoreductase
02

Mechanism of action

Inhibition of the enzymatic conversion between active cortisol and inactive cortisone to modulate local glucocorticoid concentrations and prevent inappropriate receptor activation.

03

Biological functions

Steroid metabolismGlucocorticoid regulationMineralocorticoid receptor protectionMetabolic homeostasis
04

Disease associations

Type 2 diabetesObesityMetabolic syndromeHypertensionAlzheimer's diseaseCushing's syndrome
05

Safety considerations

HypokalemiaHypertensionAdrenal insufficiencySodium retentionEdema
06

Interacting drugs

Carbenoxolone

6 more in the full profile.

07

Biomarkers

Urinary cortisol/cortisone ratioPlasma cortisol/cortisone ratioUrinary tetrahydrocortisol/tetrahydrocortisone ratio

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