Glucocorticoid receptor

Function

Glucocorticoid 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:

• Glucocorticoids
• Intracellular receptors
• Steroid Hormones and their receptors.

Relevance

The glucocorticoid-bound GCR can either up-regulate the expression of anti-inflammatory proteins (transactivation) or repress the expression of pro-inflammatory proteins (transrepression)^[2].

Disease

Budesonide is an agonist of GCR and is used as medication for asthma and inflammatory bowel diseases like chronic obstructive pulmonary disease^[3].

Structural highlights

GCR 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 receptor

Glucocorticoid receptor 3D structures