Target intelligence / Profile preview

Glucocorticoid receptor (GR)

Target
GR
Molecular classification
Nuclear receptor, Steroid hormone receptor, Transcription factor
01

Overview

The glucocorticoid receptor is a ligand-activated nuclear receptor encoded by the NR3C1 gene. It is the primary mediator of glucocorticoid (e.g., cortisol) action in mammals and regulates transcription of target genes involved in metabolism, immune response, inflammation, and the stress response. Upon binding cortisol or synthetic glucocorticoids, GR dissociates from cytoplasmic chaperones, translocates to the nucleus, and binds specific DNA elements to activate or repress gene transcription. GR signaling is critical in managing inflammation, autoimmunity, metabolic disease, and is targeted by a range of anti-inflammatory and immunosuppressive drugs.

Other names
NR3C1GCRglucocorticoid receptor alpha (GRα)glucocorticoid receptor beta (GRβ)nuclear receptor subfamily 3 group C member 1
02

Mechanism of action

Agonists: Bind to GR, resulting in transactivation/repression of target genes, anti-inflammatory and immunosuppressive effects. Antagonists: Block cortisol/glucocorticoid binding, inhibiting receptor-mediated gene activation

03

Biological functions

Regulation of metabolismImmune response modulationRegulation of inflammationStress response signalingTranscriptional regulation
04

Disease associations

CancerInflammationAutoimmune diseaseNeuropsychiatric disordersMetabolic syndromeCushing syndromeAdrenal insufficiency
05

Safety considerations

ImmunosuppressionHyperglycemia/diabetesOsteoporosisAdrenal suppressionDyslipidemiaPsychiatric effects
06

Interacting drugs

Cortisol (hydrocortisone, endogenous ligand)

5 more in the full profile.

07

Biomarkers

NR3C1 gene expression or mutationsCortisol levels (in blood/saliva/urine)GRα/GRβ isoform expression

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