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1pq6

From Proteopedia

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[[Image:1pq6.gif|left|200px]]
 
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{{Structure
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==HUMAN LXR BETA HORMONE RECEPTOR / GW3965 COMPLEX==
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|PDB= 1pq6 |SIZE=350|CAPTION= <scene name='initialview01'>1pq6</scene>, resolution 2.40&Aring;
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<StructureSection load='1pq6' size='340' side='right'caption='[[1pq6]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND= <scene name='pdbligand=965:(3-{3-[[2-CHLORO-3-(TRIFLUOROMETHYL)BENZYL](2,2-DIPHENYLETHYL)AMINO]PROPOXY}PHENYL)ACETIC+ACID'>965</scene> and <scene name='pdbligand=IPA:ISOPROPYL ALCOHOL'>IPA</scene>
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<table><tr><td colspan='2'>[[1pq6]] 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=1PQ6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1PQ6 FirstGlance]. <br>
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|ACTIVITY=
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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]] 2.4&#8491;</td></tr>
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|GENE= NR1H2 OR LXRB OR UNR OR NER ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=965:[3-(3-{[2-CHLORO-3-(TRIFLUOROMETHYL)BENZYL](2,2-DIPHENYLETHYL)AMINO}PROPOXY)PHENYL]ACETIC+ACID'>965</scene>, <scene name='pdbligand=IPA:ISOPROPYL+ALCOHOL'>IPA</scene></td></tr>
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}}
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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=1pq6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pq6 OCA], [https://pdbe.org/1pq6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1pq6 RCSB], [https://www.ebi.ac.uk/pdbsum/1pq6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1pq6 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/pq/1pq6_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=1pq6 ConSurf].
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<div style="clear:both"></div>
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'''HUMAN LXR BETA HORMONE RECEPTOR / GW3965 COMPLEX'''
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==See Also==
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*[[Liver X receptor|Liver X receptor]]
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__TOC__
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==Overview==
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</StructureSection>
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The structures of the liver X receptor LXRbeta (NR1H2) have been determined in complexes with two synthetic ligands, T0901317 and GW3965, to 2.1 and 2.4 A, respectively. Together with its isoform LXRalpha (NR1H3) it regulates target genes involved in metabolism and transport of cholesterol and fatty acids. The two LXRbeta structures reveal a flexible ligand-binding pocket that can adjust to accommodate fundamentally different ligands. The ligand-binding pocket is hydrophobic but with polar or charged residues at the two ends of the cavity. T0901317 takes advantage of this by binding to His-435 close to H12 while GW3965 orients itself with its charged group in the opposite direction. Both ligands induce a fixed "agonist conformation" of helix H12 (also called the AF-2 domain), resulting in a transcriptionally active receptor.
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==About this Structure==
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1PQ6 is a [[Single protein]] structure of 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=1PQ6 OCA].
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==Reference==
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The three-dimensional structure of the liver X receptor beta reveals a flexible ligand-binding pocket that can accommodate fundamentally different ligands., Farnegardh M, Bonn T, Sun S, Ljunggren J, Ahola H, Wilhelmsson A, Gustafsson JA, Carlquist M, J Biol Chem. 2003 Oct 3;278(40):38821-8. Epub 2003 Jun 20. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12819202 12819202]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Single protein]]
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[[Category: Large Structures]]
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[[Category: Ahola, H.]]
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[[Category: Ahola H]]
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[[Category: Bonn, T.]]
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[[Category: Bonn T]]
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[[Category: Carlquist, M.]]
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[[Category: Carlquist M]]
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[[Category: Farnegardh, M.]]
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[[Category: Farnegardh M]]
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[[Category: Gustafsson, J A.]]
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[[Category: Gustafsson J-A]]
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[[Category: Ljunggren, J.]]
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[[Category: Ljunggren J]]
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[[Category: Sun, S.]]
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[[Category: Sun S]]
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[[Category: Wilhelmsson, A.]]
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[[Category: Wilhelmsson A]]
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[[Category: 965]]
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[[Category: IPA]]
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[[Category: lxrb+kb043546/way207380/gw3965]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 13:27:33 2008''
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Current revision

HUMAN LXR BETA HORMONE RECEPTOR / GW3965 COMPLEX

PDB ID 1pq6

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