Glucocorticoid receptor
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ContentsFunctionGlucocorticoid receptor (GCR) is the nuclear receptor binding cortisol and glucocorticoids. GCR regulates genes involved in development, metabolism and immune response. GCR interacts with nuclear receptor coactivator 2 (NCOA2) which promotes DNA transcription by acylating histones[1]. See also: RelevanceThe glucocorticoid-bound GCR can either up-regulate the expression of anti-inflammatory proteins (transactivation) or repress the expression of pro-inflammatory proteins (transrepression)[2]. DiseaseBudesonide is an agonist of GCR and is used as medication for asthma and inflammatory bowel diseases like chronic obstructive pulmonary disease[3]. Structural highlightsGCR contains 5 domains: N terminal regulatory domain; DNA-binding domain (DBD) residues 417-506; hinge region; ligand-binding domain (LBD) residues 521-777 and C terminal domain. Human glucocorticoid receptor ligand-binding domain bound to dexamethasone (1m2z). Glucocorticoid Receptor in complex with budesonide (5nfp). Budesonide binding site. Water molecule is shown as red sphere. Crystal Structure of mometasone furoate-bound glucocorticoid receptor ligand binding domain (4p6w). Mometasone furoate binding site. 3D structures of glucocorticoid receptorGlucocorticoid receptor 3D structures
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This page was last modified 10:09, 16 January 2024.