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| | <StructureSection load='5gic' size='340' side='right'caption='[[5gic]], [[Resolution|resolution]] 2.35Å' scene=''> | | <StructureSection load='5gic' size='340' side='right'caption='[[5gic]], [[Resolution|resolution]] 2.35Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[5gic]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5GIC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5GIC FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[5gic]] 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=5GIC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5GIC FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DLC:(3R,5S)-5-{(2R,3R)-3-[(1R,2S,3Z)-3-{(2E)-2-[(3S,5R)-3,5-DIHYDROXY-2-METHYLIDENECYCLOHEXYLIDENE]ETHYLIDENE}-1,2-DIMETHYLCYCLOHEXYL]-2-METHYLBUTYL}-3-HYDROXY-3-METHYL-1-(2-PHENYLETHYL)PYRROLIDIN-2-ONE'>DLC</scene></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DLC:(3R,5S)-5-{(2R,3R)-3-[(1R,2S,3Z)-3-{(2E)-2-[(3S,5R)-3,5-DIHYDROXY-2-METHYLIDENECYCLOHEXYLIDENE]ETHYLIDENE}-1,2-DIMETHYLCYCLOHEXYL]-2-METHYLBUTYL}-3-HYDROXY-3-METHYL-1-(2-PHENYLETHYL)PYRROLIDIN-2-ONE'>DLC</scene></td></tr> |
| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5gid|5gid]], [[5gie|5gie]]</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=5gic FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5gic OCA], [https://pdbe.org/5gic PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5gic RCSB], [https://www.ebi.ac.uk/pdbsum/5gic PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5gic ProSAT]</span></td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">Vdr, Nr1i1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat])</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=5gic FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5gic OCA], [http://pdbe.org/5gic PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5gic RCSB], [http://www.ebi.ac.uk/pdbsum/5gic PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5gic ProSAT]</span></td></tr> | + | |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[http://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> | + | [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 == |
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| | | | |
| | ==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: Buffalo rat]] | + | [[Category: Homo sapiens]] |
| | [[Category: Large Structures]] | | [[Category: Large Structures]] |
| - | [[Category: Asano, L]] | + | [[Category: Rattus norvegicus]] |
| - | [[Category: Shimizu, T]] | + | [[Category: Asano L]] |
| - | [[Category: Nuclear receptor]] | + | [[Category: Shimizu T]] |
| - | [[Category: Transcription]]
| + | |
| Structural highlights
Function
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.[1]
Publication Abstract from PubMed
The active metabolite of vitamin D3 , 1alpha,25-dihydroxyvitamin D3 , acts as a ligand for the vitamin D receptor (VDR) and activates VDR-mediated gene expression. Recently, we characterized 1alpha,25-dihydroxyvitamin D3 -26,23-lactams (DLAMs), which mimic vitamin D3 metabolites, as noncalcemic VDR ligands that barely activate the receptor. In this study, we present structural insights onto the regulation of VDR function by DLAMs. X-ray crystallographic analysis revealed that DLAMs induced a large conformational change in the loop region between helices H6 and H7 in the VDR ligand-binding domain. Our structural analysis suggests that targeting of the loop region may be a new mode of VDR regulation.
Regulation of the vitamin D receptor by vitamin D lactam derivatives.,Asano L, Waku T, Abe R, Kuwabara N, Ito I, Yanagisawa J, Nagasawa K, Shimizu T FEBS Lett. 2016 Sep;590(18):3270-9. doi: 10.1002/1873-3468.12348. Epub 2016 Aug, 23. PMID:27500498[2]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Vanhooke JL, Tadi BP, Benning MM, Plum LA, DeLuca HF. New analogs of 2-methylene-19-nor-(20S)-1,25-dihydroxyvitamin D3 with conformationally restricted side chains: evaluation of biological activity and structural determination of VDR-bound conformations. Arch Biochem Biophys. 2007 Apr 15;460(2):161-5. Epub 2006 Dec 12. PMID:17227670 doi:10.1016/j.abb.2006.11.029
- ↑ Asano L, Waku T, Abe R, Kuwabara N, Ito I, Yanagisawa J, Nagasawa K, Shimizu T. Regulation of the vitamin D receptor by vitamin D lactam derivatives. FEBS Lett. 2016 Sep;590(18):3270-9. doi: 10.1002/1873-3468.12348. Epub 2016 Aug, 23. PMID:27500498 doi:http://dx.doi.org/10.1002/1873-3468.12348
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