Bile acid receptor

<StructureSection load='3ruu' size='450' side='right' caption='Structure of human FXR ligand-binding domain (deeppink) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry 3ruu)' scene='54/545859/Cv/1'>

FunctionFunction

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. 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.

DiseaseDisease

FXR is involved in pathophysiology of inflammatory bowel disease, colorectal cancer and type II diabetes.

RelevanceRelevance

FXR and other bile acid receptors are targets for the treatment of dyslipidemia, diabetes and cardiovascular disease.

Structural highlightsStructural 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).

3D structures of bile acid receptor3D structures of bile acid receptor

Updated on 18-November-2015

hFXR LBDhFXR LBD

1osh, 3fli, 3l1b – hFXR LBD + non-steroidal agonist - human
1osv – hFXR LBD + CDC derivative + nuclear receptor coactivator 2 peptide
4ii6, 4wvd - hFXR LBD + nuclear receptor corepressor peptide
3bej, 3dct, 3dcu, 3hc5, 3hc6, 3rut, 3ruu, 3rvf – hFXR LBD + non-steroidal agonist + nuclear receptor coactivator 1 peptide
3fxv, 3gd2, 3okh, 3oki, 3olf, 3omk, 3omm, 3oof, 3ook, 3p88, 3p89 – hFXR LBD (mutant) + non-steroidal agonist + nuclear receptor coactivator 1 peptide
1ot7 – hFXR LBD + CDC derivative + RPGR-interacting protein peptide