Function
Bile acid receptor or farnesoid X receptor (FXR) binds bile acids, then translocates to the nucleus, forms a dimer and binds to hormone response elements (see Nuclear receptors). This causes up- or down-regulation of certain genes involved in cholesterol metabolism, lipid homeostasis and absorption of fats and vitamins. FXR ligand-binding domain (LBD) binds chenodeoxycholic acid (CDC), lithocholic acid and deoxycholic acid. [1]
See also Intracellular receptors
Disease
FXR is involved in pathophysiology of inflammatory bowel disease, colorectal cancer and type II diabetes.
Relevance
FXR and other bile acid receptors are targets for the treatment of dyslipidemia, diabetes and cardiovascular disease.
Structural highlights
of human FXR ligand-binding domain (deeppink) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry 3ruu). [2]
3D structures of bile acid receptor
Bile acid receptor 3D structures
