8ck5: Difference between revisions

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== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[8ck5]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Danio_rerio Danio rerio] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8CK5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8CK5 FirstGlance]. <br>
<table><tr><td colspan='2'>[[8ck5]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Danio_rerio Danio rerio] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8CK5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8CK5 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=UYO:(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-7a-methyl-1-[(2R)-6-methyl-6-nitro-heptan-2-yl]-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidene-cyclohexane-1,3-diol'>UYO</scene></td></tr>
</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>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=UYO:(1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-7a-methyl-1-[(2R)-6-methyl-6-nitro-heptan-2-yl]-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidene-cyclohexane-1,3-diol'>UYO</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8ck5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8ck5 OCA], [https://pdbe.org/8ck5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8ck5 RCSB], [https://www.ebi.ac.uk/pdbsum/8ck5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8ck5 ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8ck5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8ck5 OCA], [https://pdbe.org/8ck5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8ck5 RCSB], [https://www.ebi.ac.uk/pdbsum/8ck5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8ck5 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[https://www.uniprot.org/uniprot/VDRA_DANRE VDRA_DANRE] Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Regulates transcription of hormone sensitive genes via its association with the WINAC complex, a chromatin-remodeling complex. Plays a central role in calcium homeostasis.<ref>PMID:17218092</ref>  
[https://www.uniprot.org/uniprot/VDRA_DANRE VDRA_DANRE] Nuclear hormone receptor. Transcription factor that mediates the action of vitamin D3 by controlling the expression of hormone sensitive genes. Regulates transcription of hormone sensitive genes via its association with the WINAC complex, a chromatin-remodeling complex. Plays a central role in calcium homeostasis.<ref>PMID:17218092</ref>  
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Intense synthetic efforts have been directed towards the development of noncalcemic analogs of 1,25-dihydroxyvitamin D(3). We describe here the structural analysis and biological evaluation of two derivatives of 1,25-dihydroxyvitamin D(3) with modifications limited to the replacement of the 25-hydroxyl group by a 25-amino or 25-nitro groups. Both compounds are agonists of the vitamin D receptor. They mediate biological effects similar to 1,25-dihydroxyvitamin D(3), the 25-amino derivative being the most potent one while being less calcemic than 1,25-dihydroxyvitamin D(3). The in vivo properties of the compounds make them of potential therapeutic value.
Structural analysis and biological activities of C25-amino and C25-nitro vitamin D analogs.,Gomez-Bouzo U, Belorusova AY, Rivadulla ML, Santalla H, Verlinden L, Verstuyf A, Ferronato MJ, Curino AC, Facchinetti MM, Fall Y, Gomez G, Rochel N Bioorg Chem. 2023 Apr 6;136:106528. doi: 10.1016/j.bioorg.2023.106528. PMID:37054528<ref>PMID:37054528</ref>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 8ck5" style="background-color:#fffaf0;"></div>
== References ==
== References ==
<references/>
<references/>

Latest revision as of 06:32, 19 June 2024

VDR LBD complex with 25-nitro derivative of 1,25D3

8ck5, resolution 2.10Å

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