Glucocorticoid receptor (NR3C1) (NR3C1)

The Glucocorticoid Receptor (NR3C1) is a ligand-activated transcription factor belonging to the nuclear receptor superfamily [UniProt P04150, NCBI Gene 2908]. It is ubiquitously expressed and mediates the effects of cortisol and other glucocorticoids, playing a central role in regulating metabolism, development, and the immune response [StatPearls NBK532940, PubMed 28249116]. Upon ligand binding, the receptor translocates from the cytoplasm to the nucleus, where it modulates the expression of numerous genes involved in anti-inflammatory and metabolic pathways [UniProt P04150, DrugBank DB01234]. It also plays a vital role in the negative feedback loop of the hypothalamic-pituitary-adrenal (HPA) axis, which is essential for maintaining homeostasis after stress [PubMed 28249116]. In clinical practice, NR3C1 is a primary target for synthetic corticosteroids used to treat a wide range of inflammatory, allergic, and autoimmune disorders, as well as certain hematologic malignancies [StatPearls NBK532940, DrugBank DB01234]. However, chronic modulation of this target is associated with significant side effects, including metabolic dysfunction and bone loss, necessitating careful therapeutic management [StatPearls NBK532940, PubMed 28249116].

Other names

Nuclear receptor subfamily 3 group C member 1GRGCRGCCRGlucocorticoid receptor mRNAGRL

Glucocorticoid receptor agonists bind to the cytosolic receptor, causing it to translocate to the nucleus where it binds to glucocorticoid response elements (GREs) to regulate gene transcription through transactivation of anti-inflammatory genes and transrepression of pro-inflammatory factors [UniProt P04150, StatPearls NBK532940]. Antagonists like mifepristone competitively inhibit ligand binding to prevent these genomic actions [DrugBank DB00396].