5kyj

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==Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core==
==Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core==
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<StructureSection load='5kyj' size='340' side='right' caption='[[5kyj]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
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<StructureSection load='5kyj' size='340' side='right'caption='[[5kyj]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5kyj]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KYJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5KYJ FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5kyj]] 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=5KYJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5KYJ FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6Y8:(6~{R})-5-(5-FLUORANYL-2-METHOXY-PYRIMIDIN-4-YL)-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOLE'>6Y8</scene></td></tr>
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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]] 2.8&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5i4v|5i4v]], [[5kya|5kya]]</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=6Y8:(6~{R})-5-(5-FLUORANYL-2-METHOXY-PYRIMIDIN-4-YL)-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOLE'>6Y8</scene></td></tr>
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<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=5kyj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kyj OCA], [http://pdbe.org/5kyj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5kyj RCSB], [http://www.ebi.ac.uk/pdbsum/5kyj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5kyj ProSAT]</span></td></tr>
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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=5kyj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kyj OCA], [https://pdbe.org/5kyj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5kyj RCSB], [https://www.ebi.ac.uk/pdbsum/5kyj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5kyj ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[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). [[http://www.uniprot.org/uniprot/RXRB_HUMAN RXRB_HUMAN]] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 (By similarity). Specifically binds 9-cis retinoic acid (9C-RA).
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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).
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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</div>
</div>
<div class="pdbe-citations 5kyj" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 5kyj" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Liver X receptor|Liver X receptor]]
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*[[Retinoid X receptor 3D structures|Retinoid X receptor 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Chen, G]]
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[[Category: Homo sapiens]]
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[[Category: McKeever, B M]]
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[[Category: Large Structures]]
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[[Category: Chemical modulator]]
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[[Category: Chen G]]
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[[Category: Dna binding protein]]
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[[Category: McKeever BM]]
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[[Category: Liver x receptor]]
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[[Category: Lxrbeta-lbd/rxrbeta-lbd heterodimer]]
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[[Category: Nuclear receptor]]
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[[Category: Retinoic acid x receptor]]
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Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core

PDB ID 5kyj

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