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3okh

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(New page: '''Unreleased structure''' The entry 3okh is ON HOLD Authors: Rudolph, M.G. Description: Discovery of novel, selective and orally active FXR agonists for the potential treatment of dis...)
Current revision (11:17, 21 February 2024) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 3okh is ON HOLD
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==Crystal structure of human FXR in complex with 2-(4-chlorophenyl)-1-[(1S)-1-cyclohexyl-2-(cyclohexylamino)-2-oxoethyl]-1H-benzimidazole-6-carboxylic acid==
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<StructureSection load='3okh' size='340' side='right'caption='[[3okh]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3okh]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3OKH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3OKH FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.5&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=OKH:2-(4-CHLOROPHENYL)-1-[(1S)-1-CYCLOHEXYL-2-(CYCLOHEXYLAMINO)-2-OXOETHYL]-1H-BENZIMIDAZOLE-6-CARBOXYLIC+ACID'>OKH</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3okh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3okh OCA], [https://pdbe.org/3okh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3okh RCSB], [https://www.ebi.ac.uk/pdbsum/3okh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3okh ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/NR1H4_HUMAN NR1H4_HUMAN] Ligand-activated transcription factor. Receptor for bile acids such as chenodeoxycholic acid, lithocholic acid and deoxycholic acid. Represses the transcription of the cholesterol 7-alpha-hydroxylase gene (CYP7A1) through the induction of NR0B2 or FGF19 expression, via two distinct mechanisms. Activates the intestinal bile acid-binding protein (IBABP). Activates the transcription of bile salt export pump ABCB11 by directly recruiting histone methyltransferase CARM1 to this locus.<ref>PMID:10334992</ref> <ref>PMID:10334993</ref> <ref>PMID:12815072</ref> <ref>PMID:15471871</ref> <ref>PMID:12718892</ref> <ref>PMID:18621523</ref> <ref>PMID:19410460</ref> <ref>PMID:19586769</ref>
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Authors: Rudolph, M.G.
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==See Also==
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*[[Bile acid receptor 3D structures|Bile acid receptor 3D structures]]
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Description: Discovery of novel, selective and orally active FXR agonists for the potential treatment of dislipidemia & diabetes
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== References ==
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<references/>
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Sep 1 09:37:32 2010''
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Rudolph MG]]

Current revision

Crystal structure of human FXR in complex with 2-(4-chlorophenyl)-1-[(1S)-1-cyclohexyl-2-(cyclohexylamino)-2-oxoethyl]-1H-benzimidazole-6-carboxylic acid

PDB ID 3okh

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