Bile acid receptor: Difference between revisions

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<StructureSection load='3ruu' size='350' side='right' caption='Structure of human FXR ligand-binding domain (grey) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (green) and sulfate ions (PDB entry [[3ruu]])' scene=''>
<StructureSection load='' size='350' side='right' caption='Structure of human FXR ligand-binding domain (magenta) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry [[3ruu]])' scene='54/545859/Cv/1'>
    
    
== 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.  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.
'''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. <ref>PMID:23982684</ref>
 
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 ==
 
<scene name='54/545859/Cv/3'>Structure</scene> of human FXR ligand-binding domain (deeppink) complex with non-steroidal agonist, nuclear receptor coactivator 1 peptide (cyan) and sulfate ions (PDB entry [[3ruu]]). <ref>PMID:21890356</ref>


==3D structures of bile acid receptor==
==3D structures of bile acid receptor==
[[Bile acid receptor 3D structures]]


Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
</StructureSection>
 
===hFXR LBD===


[[1osh]], [[3fli]], [[3l1b]] – hFXR LBD + non-steroidal agonist - human <br />
== References ==
[[1osv]] – hFXR LBD + CDC derivative + nuclear receptor coactivator 2 peptide<br />
<references/>
[[3bej]], [[3dct]], [[3dcu]], [[3hc5]], [[3hc6]], [[3rut]], [[3ruu]], [[3rvf]] – hFXR LBD + non-steroidal agonist + nuclear receptor coactivator 1 peptide<br />
[[Category:Topic Page]]
[[3fxv]], [[3gd2]], [[3okh]], [[3oki]], [[3olf]], [[3omk]], [[3omm]], [[3oof]], [[3ook]], [[3p88]], [[3p89]] – hFXR LBD (mutant) + non-steroidal agonist + nuclear receptor coactivator 1 peptide<br />
[[1ot7]] – hFXR LBD + CDC derivative + RPGR-interacting protein peptide<br />

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky, Joel L. Sussman
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