1pq9

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[[Image:1pq9.gif|left|200px]]
 
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{{Structure
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==HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317 COMPLEX==
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|PDB= 1pq9 |SIZE=350|CAPTION= <scene name='initialview01'>1pq9</scene>, resolution 2.10&Aring;
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<StructureSection load='1pq9' size='340' side='right'caption='[[1pq9]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND= <scene name='pdbligand=44B:1,1,1,3,3,3-HEXAFLUORO-2-{4-[(2,2,2-TRIFLUOROETHYL)AMINO]PHENYL}PROPAN-2-OL'>44B</scene>, <scene name='pdbligand=BNS:HYDROSULFONYLBENZENE'>BNS</scene>
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<table><tr><td colspan='2'>[[1pq9]] 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=1PQ9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1PQ9 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]] 2.1&#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=44B:1,1,1,3,3,3-HEXAFLUORO-2-{4-[(2,2,2-TRIFLUOROETHYL)AMINO]PHENYL}PROPAN-2-OL'>44B</scene>, <scene name='pdbligand=BNS:BENZENESULFONIC+ACID'>BNS</scene></td></tr>
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|DOMAIN=
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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=1pq9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pq9 OCA], [https://pdbe.org/1pq9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1pq9 RCSB], [https://www.ebi.ac.uk/pdbsum/1pq9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1pq9 ProSAT]</span></td></tr>
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|RELATEDENTRY=[[1pq6|1pq6]]
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</table>
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1pq9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pq9 OCA], [http://www.ebi.ac.uk/pdbsum/1pq9 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1pq9 RCSB]</span>
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== Function ==
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}}
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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/1pq9_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=1pq9 ConSurf].
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<div style="clear:both"></div>
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'''HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317 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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1PQ9 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=1PQ9 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: lxrb+t0901317 split]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:03:05 2008''
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Current revision

HUMAN LXR BETA HORMONE RECEPTOR COMPLEXED WITH T0901317 COMPLEX

PDB ID 1pq9

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