1upv: Difference between revisions

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{{Seed}}
[[Image:1upv.png|left|200px]]


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==Crystal structure of the human Liver X receptor beta ligand binding domain in complex with a synthetic agonist==
The line below this paragraph, containing "STRUCTURE_1upv", creates the "Structure Box" on the page.
<StructureSection load='1upv' size='340' side='right'caption='[[1upv]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
You may change the PDB parameter (which sets the PDB file loaded into the applet)
== Structural highlights ==
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
<table><tr><td colspan='2'>[[1upv]] is a 1 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=1UPV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1UPV FirstGlance]. <br>
or leave the SCENE parameter empty for the default display.
</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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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=444:N-(2,2,2-TRIFLUOROETHYL)-N-{4-[2,2,2-TRIFLUORO-1-HYDROXY-1-(TRIFLUOROMETHYL)ETHYL]PHENYL}BENZENESULFONAMIDE'>444</scene></td></tr>
{{STRUCTURE_1upv|  PDB=1upv  |  SCENE=  }}
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1upv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1upv OCA], [https://pdbe.org/1upv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1upv RCSB], [https://www.ebi.ac.uk/pdbsum/1upv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1upv ProSAT]</span></td></tr>
</table>
== Function ==
[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]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/up/1upv_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</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=1upv ConSurf].
<div style="clear:both"></div>
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== Publication Abstract from PubMed ==
LXRbeta belongs to the nuclear hormone receptor superfamily of ligand-activated transcription factors. Its natural ligands are supposed to be oxidised derivatives of cholesterol. Stimulation of LXRbeta by agonists activates a number of genes that are involved in the regulation of lipid metabolism and cholesterol efflux from cells. Therefore, LXRbeta may represent a novel therapeutic target for the treatment of dyslipidemia and atherosclerosis.Here, we report the X-ray crystal structure of the LXRbeta ligand-binding domain in complex with a synthetic agonist, T-0901317. This compound occupies the ligand-binding pocket of the receptor, forms numerous lipophilic contacts with the protein and one crucial hydrogen bond to His435 and stabilises the agonist conformation of the receptor ligand-binding domain. The recruitment of the AF2-region of the protein is not achieved via direct polar interactions of the ligand with protein side-chains of this helical segment, but rather via few hydrophobic contacts and probably more importantly via indirect effects involving the pre-orientation of side-chains that surround the ligand-binding pocket and form the interface to the AF2-helix.On the basis of these results we propose a binding mode and a mechanism of action for the putative natural ligands, oxidised derivatives of cholesterol.


===CRYSTAL STRUCTURE OF THE HUMAN LIVER X RECEPTOR BETA LIGAND BINDING DOMAIN IN COMPLEX WITH A SYNTHETIC AGONIST===
Crystal structure of the human liver X receptor beta ligand-binding domain in complex with a synthetic agonist.,Hoerer S, Schmid A, Heckel A, Budzinski RM, Nar H J Mol Biol. 2003 Dec 12;334(5):853-61. PMID:14643652<ref>PMID:14643652</ref>


From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 1upv" style="background-color:#fffaf0;"></div>


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==See Also==
The line below this paragraph, {{ABSTRACT_PUBMED_14643652}}, adds the Publication Abstract to the page
*[[Liver X receptor|Liver X receptor]]
(as it appears on PubMed at http://www.pubmed.gov), where 14643652 is the PubMed ID number.
== References ==
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<references/>
{{ABSTRACT_PUBMED_14643652}}
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</StructureSection>
==About this Structure==
1UPV is a 1 chain 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=1UPV OCA].
 
==Reference==
<ref group="xtra">PMID:14643652</ref><references group="xtra"/>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Budzinski, R M.]]
[[Category: Large Structures]]
[[Category: Heckel, A.]]
[[Category: Budzinski RM]]
[[Category: Hoerer, S.]]
[[Category: Heckel A]]
[[Category: Nar, H.]]
[[Category: Hoerer S]]
[[Category: Schmid, A.]]
[[Category: Nar H]]
[[Category: Crystal structure]]
[[Category: Schmid A]]
[[Category: Ligand binding domain]]
[[Category: Liver x receptor]]
[[Category: Nuclear hormone receptor]]
[[Category: Receptor]]
[[Category: Transcription factor]]
 
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Retrieved from "https://proteopedia.org/1upv"