1pq9

<StructureSection load='1pq9' size='340' side='right' caption='[[1pq9]], [[Resolution|resolution]] 2.10&Aring;' scene=''>

<table><tr><td colspan='2'>[[1pq9]] 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=1PQ9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1PQ9 FirstGlance]. <br>

</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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>

<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">NR1H2 OR LXRB OR UNR OR NER ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=1pq9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pq9 OCA], [http://pdbe.org/1pq9 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=1pq9 RCSB], [http://www.ebi.ac.uk/pdbsum/1pq9 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=1pq9 ProSAT]</span></td></tr>

[[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).

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== Publication Abstract from PubMed ==

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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== References ==

[[Category: Human]]

[[Category: Ahola, H]]

[[Category: Bonn, T]]

[[Category: Carlquist, M]]

[[Category: Farnegardh, M]]

[[Category: Gustafsson, J A]]

[[Category: Ljunggren, J]]

[[Category: Sun, S]]

[[Category: Wilhelmsson, A]]

[[Category: Transcription regulation]]