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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.
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
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