3dcu

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{{Seed}}
 
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[[Image:3dcu.png|left|200px]]
 
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==FXR with SRC1 and GSK8062==
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The line below this paragraph, containing "STRUCTURE_3dcu", creates the "Structure Box" on the page.
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<StructureSection load='3dcu' size='340' side='right'caption='[[3dcu]], [[Resolution|resolution]] 2.95&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3dcu]] 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=3DCU OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3DCU FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=O62:6-(4-{[3-(2,6-DICHLOROPHENYL)-5-(1-METHYLETHYL)ISOXAZOL-4-YL]METHOXY}PHENYL)NAPHTHALENE-1-CARBOXYLIC+ACID'>O62</scene></td></tr>
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{{STRUCTURE_3dcu| PDB=3dcu | SCENE= }}
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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=3dcu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3dcu OCA], [https://pdbe.org/3dcu PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3dcu RCSB], [https://www.ebi.ac.uk/pdbsum/3dcu PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3dcu 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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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/dc/3dcu_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3dcu ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a. Analog 1b also reduced the severity of cholestasis in the ANIT acute cholestatic rat model.
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===FXR with SRC1 and GSK8062===
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Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.,Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Jones SA, Kaldor I, Liu Y, Madauss KP, Marr HB, McFadyen RB, Miller AB, Iii FN, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB Bioorg Med Chem Lett. 2008 Aug 1;18(15):4339-43. Epub 2008 Jun 28. PMID:18621523<ref>PMID:18621523</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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<div class="pdbe-citations 3dcu" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_18621523}}, adds the Publication Abstract to the page
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*[[Bile acid receptor 3D structures|Bile acid receptor 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 18621523 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_18621523}}
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__TOC__
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</StructureSection>
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==About this Structure==
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3DCU is a 2 chains structure of sequences 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=3DCU OCA].
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==Reference==
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<ref group="xtra">PMID:18621523</ref><references group="xtra"/>
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[[Category: Histone acetyltransferase]]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Madauss, K P.]]
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[[Category: Large Structures]]
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[[Category: Williams, S P.]]
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[[Category: Madauss KP]]
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[[Category: Activator]]
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[[Category: Williams SP]]
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[[Category: Acyltransferase]]
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[[Category: Alpha-helical sandwich]]
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[[Category: Alternative splicing]]
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[[Category: Chromosomal rearrangement]]
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[[Category: Dna-binding]]
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[[Category: Fxr]]
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[[Category: Gw4064]]
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[[Category: Metal-binding]]
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[[Category: Nuclear receptor]]
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[[Category: Nucleus]]
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[[Category: Phosphoprotein]]
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[[Category: Polymorphism]]
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[[Category: Proto-oncogene]]
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[[Category: Receptor]]
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[[Category: Repressor]]
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[[Category: Transcription regulation]]
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[[Category: Transcription/transcription activator complex]]
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[[Category: Transferase]]
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[[Category: Ubl conjugation]]
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[[Category: Zinc]]
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[[Category: Zinc-finger]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 18 06:22:47 2009''
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Current revision

FXR with SRC1 and GSK8062

PDB ID 3dcu

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