Bile acid receptor
From Proteopedia
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| - | <StructureSection load=' | + | <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 == | == 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. <ref>PMID:23982684</ref> | + | '''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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| + | See also [[Intracellular receptors]] | ||
== Disease == | == Disease == | ||
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== Structural highlights == | == Structural highlights == | ||
| - | <scene name='54/545859/Cv/ | + | <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> |
| - | </StructureSection> | ||
==3D structures of bile acid receptor== | ==3D structures of bile acid receptor== | ||
| + | [[Bile acid receptor 3D structures]] | ||
| - | + | </StructureSection> | |
| - | [[1osh]], [[3fli]], [[3l1b]] – hFXR LBD + non-steroidal agonist - human <br /> | ||
| - | [[1osv]] – hFXR LBD + CDC derivative + nuclear receptor coactivator 2 peptide<br /> | ||
| - | [[4wvd]] - hFXR LBD + nuclear receptor corepressor peptide<br /> | ||
| - | [[3bej]], [[3dct]], [[3dcu]], [[3hc5]], [[3hc6]], [[3rut]], [[3ruu]], [[3rvf]] – hFXR LBD + non-steroidal agonist + nuclear receptor coactivator 1 peptide<br /> | ||
| - | [[4qe6]] – hFXR LBD + CDC + nuclear receptor coactivator 2 peptide<br /> | ||
| - | [[4qe8]] – hFXR LBD + DM175 + nuclear receptor coactivator 2 peptide<br /> | ||
| - | [[5iaw]] - hFXR LBD + nuclear receptor coactivator 2 peptide + modulator<br /> | ||
| - | [[5q0x]], [[5q0y]], [[5q0z]], [[5q10]], [[5q11]], [[5q12]], [[5q13]], [[5q14]], [[5q16]], [[5q18]], [[5q19]], [[5q1a]], [[5q1b]], [[5q1c]], [[5q1d]], [[5q1e]], [[5q1f]], [[5q1g]], [[5q1h]], [[5q1i]], [[5q01]], [[5q0j]], [[5q0k]], [[5q0l]], [[5q0m]], [[5q0n]], [[5q0o]], [[5q0p]], [[5q0r]], [[5q0q]], [[5q0s]], [[5q0t]], [[5q0u]], [[5q0v]], [[5q0w]], [[5q17]] - hFXR LBD + coactivator peptide SRC-1 HD3 + ligand<br /> | ||
| - | [[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 /> | ||
| - | [[4oiv]] – hFXR LBD + antagonist <br /> | ||
== References == | == References == | ||
<references/> | <references/> | ||
[[Category:Topic Page]] | [[Category:Topic Page]] | ||
Current revision
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References
- ↑ 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
- ↑ 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
