Human glucocorticoid receptor (GR)

The human glucocorticoid receptor is an intracellular, ligand-activated transcription factor belonging to the nuclear receptor superfamily. It is encoded by the NR3C1 gene on chromosome 5 and is ubiquitously expressed across tissues. Structurally, it is a modular protein with distinct domains for transcriptional regulation, DNA binding, and ligand binding. Upon binding glucocorticoid hormones (such as cortisol or synthetic analogs), the receptor dissociates from cytoplasmic chaperones, translocates to the nucleus, and regulates the transcription of genes involved in inflammation, metabolism, cell proliferation, and immune responses. The glucocorticoid receptor is a major pharmacological target in the treatment of inflammatory, autoimmune, and some neoplastic diseases, but its therapeutic potential is limited by resistance mechanisms and undesirable systemic effects that arise from extended or high-dose use

Other names

Glucocorticoid receptorNuclear receptor subfamily 3 group C member 1NR3C1GRL

Agonists bind the receptor, activate nuclear translocation, and promote or repress expression of glucocorticoid-responsive genes by binding to glucocorticoid response elements (GREs) Antagonists block ligand binding and downstream transcriptional activity Partial agonists or modulators alter receptor conformation and downstream gene expression patterns