3l0e

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{{Seed}}
 
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[[Image:3l0e.jpg|left|200px]]
 
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==X-ray crystal structure of a Potent Liver X Receptor Modulator==
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The line below this paragraph, containing "STRUCTURE_3l0e", creates the "Structure Box" on the page.
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<StructureSection load='3l0e' size='340' side='right'caption='[[3l0e]], [[Resolution|resolution]] 2.30&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'>[[3l0e]] 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=3L0E OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3L0E 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]] 2.3&#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=G58:N-(2-CHLORO-6-FLUOROBENZYL)-1-METHYL-N-{[3-(METHYLSULFONYL)BIPHENYL-4-YL]METHYL}-1H-IMIDAZOLE-4-SULFONAMIDE'>G58</scene></td></tr>
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{{STRUCTURE_3l0e| PDB=3l0e | 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=3l0e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3l0e OCA], [https://pdbe.org/3l0e PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3l0e RCSB], [https://www.ebi.ac.uk/pdbsum/3l0e PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3l0e ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/NR1H2_HUMAN NR1H2_HUMAN] Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (By similarity).
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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/l0/3l0e_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=3l0e 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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Tertiary sulfonamides were identified in a HTS as dual liver X receptor (LXR, NR1H2, and NR1H3) ligands, and the binding affinity of the series was increased through iterative analogue synthesis. A ligand-bound cocrystal structure was determined which elucidated key interactions for high binding affinity. Further characterization of the tertiary sulfonamide series led to the identification of high affinity LXR antagonists. GSK2033 (17) is the first potent cell-active LXR antagonist described to date. 17 may be a useful chemical probe to explore the cell biology of this orphan nuclear receptor.
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===X-ray crystal structure of a Potent Liver X Receptor Modulator===
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Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists.,Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM J Med Chem. 2010 Mar 26. PMID:20345102<ref>PMID:20345102</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 3l0e" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_20345102}}, adds the Publication Abstract to the page
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*[[Liver X receptor|Liver X receptor]]
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(as it appears on PubMed at http://www.pubmed.gov), where 20345102 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_20345102}}
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__TOC__
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</StructureSection>
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==About this Structure==
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3L0E is a 2 chains structure with 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=3L0E OCA].
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==Reference==
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<ref group="xtra">PMID:20345102</ref><references group="xtra"/>
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Jr., R T.Gampe.]]
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[[Category: Large Structures]]
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[[Category: Acetylation]]
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[[Category: Gampe Jr RT]]
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[[Category: Activator]]
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[[Category: Dna-binding]]
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[[Category: Hlxr-beta]]
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[[Category: Human liver x receptor-beta]]
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[[Category: Metal-binding]]
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[[Category: Nucleus]]
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[[Category: Phosphoprotein]]
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[[Category: Polymorphism]]
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[[Category: Receptor]]
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[[Category: Sulfonamide modulator]]
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[[Category: Transcription]]
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[[Category: Transcription regulation]]
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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 Apr 7 10:36:00 2010''
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Current revision

X-ray crystal structure of a Potent Liver X Receptor Modulator

PDB ID 3l0e

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