3kfc: Difference between revisions

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 ==Complex Structure of LXR with an agonist==
-<StructureSection load='3kfc' size='340' side='right' caption='[[3kfc]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
+<StructureSection load='3kfc' size='340' side='right'caption='[[3kfc]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[3kfc]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3KFC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3KFC FirstGlance]. <br>
+<table><tr><td colspan='2'>[[3kfc]] is a 4 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=3KFC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3KFC FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=61X:4-{3-[3-(METHYLSULFONYL)PHENOXY]PHENYL}-8-(TRIFLUOROMETHYL)QUINOLINE'>61X</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.4&#8491;</td></tr>
-<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">NR1H2, LXRB, NER, UNR ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=61X:4-{3-[3-(METHYLSULFONYL)PHENOXY]PHENYL}-8-(TRIFLUOROMETHYL)QUINOLINE'>61X</scene></td></tr>
-<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=3kfc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3kfc OCA], [http://pdbe.org/3kfc PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3kfc RCSB], [http://www.ebi.ac.uk/pdbsum/3kfc PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3kfc ProSAT]</span></td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3kfc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3kfc OCA], [https://pdbe.org/3kfc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3kfc RCSB], [https://www.ebi.ac.uk/pdbsum/3kfc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3kfc ProSAT]</span></td></tr>
 </table>
 == Function ==
-[[http://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).
+[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).
 == Evolutionary Conservation ==
 [[Image:Consurf_key_small.gif|200px|right]]
@@ Line 20: / Line 20: @@
 </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=3kfc ConSurf].
 <div style="clear:both"></div>
-<div style="background-color:#fffaf0;">
-== Publication Abstract from PubMed ==
-A series of 4-(3-aryloxyaryl)quinolines with sulfone substituents on the terminal aryl ring (7) was prepared as LXR agonists. High affinity LXR ligands with excellent agonist potency and efficacy in functional assays of LXR activity were identified. In general, these sulfone agonists were equal to or superior to previously described alcohol and amide analogs in terms of affinity, functional potency, and microsomal stability. Many of the sulfones had LXRbeta binding IC(50) values &lt;10nM while the most potent compounds in an ABCA1 mRNA induction assay in J774 mouse cells had EC(50) values &lt;10nM and were as efficacious as T0901317.
--(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.,Bernotas RC, Singhaus RR, Kaufman DH, Travins JM, Ullrich JW, Unwalla R, Quinet E, Evans M, Nambi P, Olland A, Kauppi B, Wilhelmsson A, Goos-Nilsson A, Wrobel J Bioorg Med Chem Lett. 2010 Jan 1;20(1):209-12. Epub 2009 Oct 31. PMID:19932617<ref>PMID:19932617</ref>
-From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-</div>
-<div class="pdbe-citations 3kfc" style="background-color:#fffaf0;"></div>
 ==See Also==
 *[[Liver X receptor|Liver X receptor]]
-== References ==
-<references/>
 __TOC__
 </StructureSection>
-[[Category: Human]]
+[[Category: Homo sapiens]]
-[[Category: Bernotas, R C]]
+[[Category: Large Structures]]
-[[Category: Olland, A]]
+[[Category: Bernotas RC]]
-[[Category: Unwalla, R]]
+[[Category: Olland A]]
-[[Category: Dna-binding]]
+[[Category: Unwalla R]]
-[[Category: Liver x receptor]]
-[[Category: Lxr]]
-[[Category: Lxr agonist]]
-[[Category: Lxr ligand]]
-[[Category: Metal-binding]]
-[[Category: Nuclear receptor]]
-[[Category: Nucleus]]
-[[Category: Receptor]]
-[[Category: Transcription]]
-[[Category: Transcription regulation]]
-[[Category: Zinc-finger]]