Carbonyl reductase 1 catalyzes 20β-reduction of glucocorticoids, modulating receptor activation and metabolic complications of obesity

Sci Rep. 2017 Sep 6;7(1):10633. doi: 10.1038/s41598-017-10410-1.

Abstract

Carbonyl Reductase 1 (CBR1) is a ubiquitously expressed cytosolic enzyme important in exogenous drug metabolism but the physiological function of which is unknown. Here, we describe a role for CBR1 in metabolism of glucocorticoids. CBR1 catalyzes the NADPH- dependent production of 20β-dihydrocortisol (20β-DHF) from cortisol. CBR1 provides the major route of cortisol metabolism in horses and is up-regulated in adipose tissue in obesity in horses, humans and mice. We demonstrate that 20β-DHF is a weak endogenous agonist of the human glucocorticoid receptor (GR). Pharmacological inhibition of CBR1 in diet-induced obesity in mice results in more marked glucose intolerance with evidence for enhanced hepatic GR signaling. These findings suggest that CBR1 generating 20β-dihydrocortisol is a novel pathway modulating GR activation and providing enzymatic protection against excessive GR activation in obesity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbonyl Reductase (NADPH) / genetics
  • Carbonyl Reductase (NADPH) / metabolism*
  • Disease Models, Animal
  • Energy Metabolism*
  • Female
  • Gene Expression
  • Genetic Association Studies
  • Genetic Variation
  • Glucocorticoids / chemistry
  • Glucocorticoids / metabolism*
  • Glucocorticoids / urine
  • Horses
  • Humans
  • Hydrocortisone / metabolism
  • Hydroxycorticosteroids / metabolism
  • Hydroxycorticosteroids / urine
  • Liver / metabolism
  • Male
  • Mice
  • Models, Molecular
  • Molecular Conformation
  • Obesity / genetics
  • Obesity / metabolism*
  • Phenotype
  • Protein Binding
  • Receptors, Glucocorticoid / agonists
  • Receptors, Glucocorticoid / chemistry
  • Receptors, Glucocorticoid / metabolism*
  • Structure-Activity Relationship

Substances

  • Glucocorticoids
  • Hydroxycorticosteroids
  • Receptors, Glucocorticoid
  • Carbonyl Reductase (NADPH)
  • Hydrocortisone