Bile acid receptor

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(New page: <StructureSection load='3ruu' size='350' side='right' caption='Structure of human FXR ligand-binding domain complex with non-steroidal agonist and nuclear receptor coactivator 1 peptide (...)
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<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'>
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<StructureSection load='3ruu' size='350' side='right' caption='Structure of human FXR ligand-binding domain complex with non-steroidal agonist and nuclear receptor coactivator 1 peptide (PDB entry [[3ruu]])' scene=''>
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== Function ==
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'''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.
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'''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>
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==3D structures of bile acid receptor==
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See also [[Intracellular receptors]]
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Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
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== Disease ==
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FXR is involved in pathophysiology of inflammatory bowel disease, colorectal cancer and type II diabetes.
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== Relevance ==
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FXR and other bile acid receptors are targets for the treatment of dyslipidemia, diabetes and cardiovascular disease.
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== Structural highlights ==
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<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>
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==3D structures of bile acid receptor==
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[[Bile acid receptor 3D structures]]
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===hFXR LBD===
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</StructureSection>
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[[1osh]], [[3fli]], [[3l1b]] – hFXR LBD + non-steroidal agonist - human <br />
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== References ==
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[[1osv]] – hFXR LBD + CDC derivative + nuclear receptor coactivator 2 peptide<br />
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<references/>
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[[3bej]], [[3dct]], [[3dcu]], [[3hc5]], [[3hc6]], [[3rut]], [[3ruu]], [[3rvf]] – hFXR LBD + non-steroidal agonist + nuclear receptor coactivator 1 peptide<br />
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[[Category:Topic Page]]
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[[3fxv]], [[3gd2]], [[3okh]], [[3oki]], [[3olf]], [[3omk]], [[3omm]], [[3oof]], [[3ook]], [[3p88]], [[3p89]] – hFXR LBD (mutant) + non-steroidal agonist + nuclear receptor coactivator 1 peptide<br />
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[[1ot7]] – hFXR LBD + CDC derivative + RPGR-interacting protein peptide<br />
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Current revision

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)

Drag the structure with the mouse to rotate

References

  1. ↑ Schaap FG, Trauner M, Jansen PL. Bile acid receptors as targets for drug development. Nat Rev Gastroenterol Hepatol. 2014 Jan;11(1):55-67. doi:, 10.1038/nrgastro.2013.151. Epub 2013 Aug 27. PMID:23982684 doi:http://dx.doi.org/10.1038/nrgastro.2013.151
  2. ↑ Akwabi-Ameyaw A, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, Miller AB, Navas F 3rd, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB. Conformationally constrained farnesoid X receptor (FXR) agonists: Alternative replacements of the stilbene. Bioorg Med Chem Lett. 2011 Aug 11. PMID:21890356 doi:10.1016/j.bmcl.2011.08.034

Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky, Joel L. Sussman

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