3p88

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==FXR bound to isoquinolinecarboxylic acid==
==FXR bound to isoquinolinecarboxylic acid==
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<StructureSection load='3p88' size='340' side='right' caption='[[3p88]], [[Resolution|resolution]] 2.95&Aring;' scene=''>
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<StructureSection load='3p88' size='340' side='right'caption='[[3p88]], [[Resolution|resolution]] 2.95&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3p88]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3P88 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3P88 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3p88]] 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=3P88 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3P88 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=P88:7-(4-{[3-(2,6-DIMETHYLPHENYL)-5-(1-METHYLETHYL)ISOXAZOL-4-YL]METHOXY}PHENYL)ISOQUINOLINE-3-CARBOXYLIC+ACID'>P88</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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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]] 2.95&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3p89|3p89]]</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=P88:7-(4-{[3-(2,6-DIMETHYLPHENYL)-5-(1-METHYLETHYL)ISOXAZOL-4-YL]METHOXY}PHENYL)ISOQUINOLINE-3-CARBOXYLIC+ACID'>P88</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">hCG_20893, NR1H4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]), BHLHE74, NCOA1, SRC1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=3p88 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3p88 OCA], [https://pdbe.org/3p88 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3p88 RCSB], [https://www.ebi.ac.uk/pdbsum/3p88 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3p88 ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3p88 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3p88 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3p88 RCSB], [http://www.ebi.ac.uk/pdbsum/3p88 PDBsum]</span></td></tr>
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</table>
</table>
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<div style="background-color:#fffaf0;">
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== Function ==
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== Publication Abstract from PubMed ==
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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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To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability parameters relative to 1b. In addition, analog 1c lowered body weight gain and serum glucose in a DIO mouse model of diabetes.
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Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.,Bass JY, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Mills WY, Navas F 3rd, Parks DJ, Smalley TL Jr, Spearing PK, Todd D, Williams SP, Wisely GB Bioorg Med Chem Lett. 2011 Feb 15;21(4):1206-13. Epub 2010 Dec 23. PMID:21256005<ref>PMID:21256005</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==See Also==
==See Also==
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*[[Bile acid receptor|Bile acid receptor]]
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*[[Bile acid receptor 3D structures|Bile acid receptor 3D structures]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Deaton, D N]]
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[[Category: Large Structures]]
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[[Category: Madauss, K P]]
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[[Category: Deaton DN]]
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[[Category: Williams, S P]]
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[[Category: Madauss KP]]
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[[Category: Nuclear recptor fxr]]
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[[Category: Williams SP]]
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[[Category: Transcription-inhibitor complex]]
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Current revision

FXR bound to isoquinolinecarboxylic acid

PDB ID 3p88

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