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==Crystal Structure of Rat VDR Ligand Binding Domain in Complex with Novel Nonsecosteroidal Ligands== | ==Crystal Structure of Rat VDR Ligand Binding Domain in Complex with Novel Nonsecosteroidal Ligands== | ||
<StructureSection load='3w0h' size='340' side='right' caption='[[3w0h]], [[Resolution|resolution]] 1.80Å' scene=''> | <StructureSection load='3w0h' size='340' side='right'caption='[[3w0h]], [[Resolution|resolution]] 1.80Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[3w0h]] is a 2 chain structure with sequence from [ | <table><tr><td colspan='2'>[[3w0h]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3W0H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3W0H FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=W12:(2S)-3-{4-[4-(4-{[(2R)-2-HYDROXY-3,3-DIMETHYLBUTYL]OXY}PHENYL)HEPTAN-4-YL]PHENOXY}PROPANE-1,2-DIOL'>W12</scene> | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.8Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=W12:(2S)-3-{4-[4-(4-{[(2R)-2-HYDROXY-3,3-DIMETHYLBUTYL]OXY}PHENYL)HEPTAN-4-YL]PHENOXY}PROPANE-1,2-DIOL'>W12</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=3w0h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3w0h OCA], [https://pdbe.org/3w0h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3w0h RCSB], [https://www.ebi.ac.uk/pdbsum/3w0h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3w0h ProSAT]</span></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | |||
</table> | </table> | ||
== Function == | == Function == | ||
[ | [https://www.uniprot.org/uniprot/VDR_RAT VDR_RAT] 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. Recruited to promoters via its interaction with the WINAC complex subunit BAZ1B/WSTF, which mediates the interaction with acetylated histones, an essential step for VDR-promoter association. Plays a central role in calcium homeostasis.<ref>PMID:17227670</ref> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
| Line 22: | Line 21: | ||
==See Also== | ==See Also== | ||
*[[Vitamin D receptor|Vitamin D receptor]] | *[[Vitamin D receptor 3D structures|Vitamin D receptor 3D structures]] | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: Asano | [[Category: Large Structures]] | ||
[[Category: Ito | [[Category: Rattus norvegicus]] | ||
[[Category: Kuwabara | [[Category: Asano L]] | ||
[[Category: Miyachi | [[Category: Ito I]] | ||
[[Category: Shimizu | [[Category: Kuwabara N]] | ||
[[Category: Waku | [[Category: Miyachi H]] | ||
[[Category: Yanagisawa | [[Category: Shimizu T]] | ||
[[Category: Waku T]] | |||
[[Category: Yanagisawa J]] | |||
Latest revision as of 15:44, 8 November 2023
Crystal Structure of Rat VDR Ligand Binding Domain in Complex with Novel Nonsecosteroidal LigandsCrystal Structure of Rat VDR Ligand Binding Domain in Complex with Novel Nonsecosteroidal Ligands
Structural highlights
FunctionVDR_RAT 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. Recruited to promoters via its interaction with the WINAC complex subunit BAZ1B/WSTF, which mediates the interaction with acetylated histones, an essential step for VDR-promoter association. Plays a central role in calcium homeostasis.[1] Publication Abstract from PubMedNon-secosteroidal ligands for vitamin D receptor (VDR) have been developed for the agonist with non-calcemic profiles. Here, we provide the structural mechanism of VDR agonism by novel non-secosteroidal ligands. All ligands had the similar efficacy, while two had the higher potency. Crystallographic analyses revealed that all ligands interacted with helix H10 and the loop between helices H6 and H7 in a similar manner, but also that the two ligands with higher potency had different interaction modes. This study suggests that distinct ligand potency depend upon differences in the formation and rearrangement of hydrogen-bond networks induced by each ligand. Structural basis for vitamin D receptor agonism by novel non-secosteroidal ligands.,Asano L, Ito I, Kuwabara N, Waku T, Yanagisawa J, Miyachi H, Shimizu T FEBS Lett. 2013 Apr 2;587(7):957-63. doi: 10.1016/j.febslet.2013.02.028. Epub, 2013 Feb 24. PMID:23462137[2] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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