5kya

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<StructureSection load='5kya' size='340' side='right'caption='[[5kya]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
<StructureSection load='5kya' size='340' side='right'caption='[[5kya]], [[Resolution|resolution]] 2.60&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5kya]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5KYA OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5KYA FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5kya]] 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=5KYA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5KYA FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6Y4:[2-[(6~{R})-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOL-5-YL]-4-(TRIFLUOROMETHYL)PYRIMIDIN-5-YL]METHANOL'>6Y4</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]] 2.598&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5i4v|5i4v]]</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=6Y4:[2-[(6~{R})-2-(3-METHYLSULFONYLPHENYL)-6-PROPAN-2-YL-4,6-DIHYDROPYRROLO[3,4-C]PYRAZOL-5-YL]-4-(TRIFLUOROMETHYL)PYRIMIDIN-5-YL]METHANOL'>6Y4</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5kya FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kya OCA], [http://pdbe.org/5kya PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5kya RCSB], [http://www.ebi.ac.uk/pdbsum/5kya PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5kya 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=5kya FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5kya OCA], [https://pdbe.org/5kya PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5kya RCSB], [https://www.ebi.ac.uk/pdbsum/5kya PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5kya 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/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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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Liver X receptor (LXR) agonists have been reported to lower brain amyloid beta (Abeta) and thus to have potential for the treatment of Alzheimer's disease. Structure and property based design led to the discovery of a series of orally bioavailable, brain penetrant LXR agonists. Oral administration of compound 18 to rats resulted in significant upregulation of the expression of the LXR target gene ABCA1 in brain tissue, but no significant effect on Abeta levels was detected.
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Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.,Tice CM, Noto PB, Fan KY, Zhao W, Lotesta SD, Dong C, Marcus AP, Zheng YJ, Chen G, Wu Z, Van Orden R, Zhou J, Bukhtiyarov Y, Zhao Y, Lipinski K, Howard L, Guo J, Kandpal G, Meng S, Hardy A, Krosky P, Gregg RE, Leftheris K, McKeever BM, Singh SB, Lala D, McGeehan GM, Zhuang L, Claremon DA Bioorg Med Chem Lett. 2016 Aug 29. pii: S0960-894X(16)30921-0. doi:, 10.1016/j.bmcl.2016.08.089. PMID:27599745<ref>PMID:27599745</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 5kya" style="background-color:#fffaf0;"></div>
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==See Also==
==See Also==
*[[Liver X receptor|Liver X receptor]]
*[[Liver X receptor|Liver X receptor]]
*[[Retinoid X receptor 3D structures|Retinoid X receptor 3D structures]]
*[[Retinoid X receptor 3D structures|Retinoid X receptor 3D structures]]
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== References ==
 
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<references/>
 
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Chen, G]]
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[[Category: Chen G]]
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[[Category: McKeever, B M]]
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[[Category: McKeever BM]]
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[[Category: Chemical modulator]]
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[[Category: Dna binding protein]]
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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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Current revision

Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core

PDB ID 5kya

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