Bile acid receptor

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<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'>
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<StructureSection load='3ruu' size='450' 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 ==
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<scene name='54/545859/Cv/2'>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>
<scene name='54/545859/Cv/2'>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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</StructureSection>
==3D structures of bile acid receptor==
==3D structures of bile acid receptor==
Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}}
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==hFXR LBD==
 
[[1osh]], [[3fli]], [[3l1b]] – hFXR LBD + non-steroidal agonist - human <br />
[[1osh]], [[3fli]], [[3l1b]] – hFXR LBD + non-steroidal agonist - human <br />

Revision as of 10:28, 30 November 2015

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

3D structures of bile acid receptor

Updated on 30-November-2015

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

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

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Michal Harel, Alexander Berchansky, Joel L. Sussman

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