4rak
From Proteopedia
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| - | ''' | + | ==Crystal structure of nuclear receptor subfamily 1, group h, member 2 (lxrb) complexed with partial agonist== |
| + | <StructureSection load='4rak' size='340' side='right' caption='[[4rak]], [[Resolution|resolution]] 2.04Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4rak]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4RAK OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4RAK FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=652:2-{2-[2-(2-CHLOROPHENYL)PROPAN-2-YL]-1-[3-(METHYLSULFONYL)BIPHENYL-4-YL]-1H-IMIDAZOL-4-YL}PROPAN-2-OL'>652</scene>, <scene name='pdbligand=BU1:1,4-BUTANEDIOL'>BU1</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=4rak FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4rak OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4rak RCSB], [http://www.ebi.ac.uk/pdbsum/4rak PDBsum]</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). | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | A series of biaryl pyrazole and imidazole Liver X Receptor (LXR) partial agonists has been synthesized displaying LXRbeta selectivity. The LXRbeta selective partial agonist 18 was identified with potent induction of ATP binding transporters ABCA1 and ABCG1 in human whole blood (EC50=1.2muM, 55% efficacy). In mice 18 displayed peripheral induction of ABCA1 at 3 and 10mpk doses with no significant elevation of plasma or hepatic triglycerides at these doses, showing an improved profile compared to a full pan-agonist. | ||
| - | + | Liver X Receptor (LXR) partial agonists: Biaryl pyrazoles and imidazoles displaying a preference for LXRbeta.,Kick E, Martin R, Xie Y, Flatt B, Schweiger E, Wang TL, Busch B, Nyman M, Gu XH, Yan G, Wagner B, Nanao M, Nguyen L, Stout T, Plonowski A, Schulman I, Ostrowski J, Kirchgessner T, Wexler R, Mohan R Bioorg Med Chem Lett. 2015 Jan 15;25(2):372-7. doi: 10.1016/j.bmcl.2014.11.029., Epub 2014 Nov 15. PMID:25435151<ref>PMID:25435151</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| - | + | <references/> | |
| + | __TOC__ | ||
| + | </StructureSection> | ||
[[Category: Nanao, M]] | [[Category: Nanao, M]] | ||
| + | [[Category: Ligand binding domain]] | ||
| + | [[Category: Lxr-b]] | ||
| + | [[Category: Lxrb]] | ||
| + | [[Category: Ner]] | ||
| + | [[Category: Ner-i]] | ||
| + | [[Category: Nhr]] | ||
| + | [[Category: Nr1h2]] | ||
| + | [[Category: Nuclear hormone receptor]] | ||
| + | [[Category: Rip15]] | ||
| + | [[Category: Rxr]] | ||
| + | [[Category: Transcription-agonist complex]] | ||
| + | [[Category: Unr]] | ||
Revision as of 14:45, 31 December 2014
Crystal structure of nuclear receptor subfamily 1, group h, member 2 (lxrb) complexed with partial agonist
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Categories: Nanao, M | Ligand binding domain | Lxr-b | Lxrb | Ner | Ner-i | Nhr | Nr1h2 | Nuclear hormone receptor | Rip15 | Rxr | Transcription-agonist complex | Unr
