View source for 6xzv


==Structure of zVDR LBD-Calcitriol in complex with chimera 18==
<StructureSection load='6xzv' size='340' side='right'caption='[[6xzv]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[6xzv]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Danio_rerio Danio rerio] and [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6XZV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6XZV FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=G2Z:[(2~{S})-2-azanylpropyl]carbamic+acid'>G2Z</scene>, <scene name='pdbligand=MFH:[(2~{S})-2-azanyl-3-(4-hydroxyphenyl)propyl]carbamic+acid'>MFH</scene>, <scene name='pdbligand=UIA:[(2~{R})-1-azanylpropan-2-yl]carbamic+acid'>UIA</scene>, <scene name='pdbligand=URL:[(2~{S})-2-azanyl-4-methyl-pentyl]carbamic+acid'>URL</scene>, <scene name='pdbligand=URV:[(2~{S})-2-azanyl-3-methyl-butyl]carbamic+acid'>URV</scene>, <scene name='pdbligand=UZN:[(2~{S})-2-azanylhexyl]carbamic+acid'>UZN</scene>, <scene name='pdbligand=VDX:5-{2-[1-(5-HYDROXY-1,5-DIMETHYL-HEXYL)-7A-METHYL-OCTAHYDRO-INDEN-4-YLIDENE]-ETHYLIDENE}-4-METHYLENE-CYCLOHEXANE-1,3-DIOL'>VDX</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=6xzv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6xzv OCA], [https://pdbe.org/6xzv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6xzv RCSB], [https://www.ebi.ac.uk/pdbsum/6xzv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6xzv ProSAT]</span></td></tr>
</table>
== 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> 
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Efficient optimization of a peptide lead into a drug candidate frequently needs further transformation to augment properties such as bioavailability. Among the different options, foldamers, which are sequence-based oligomers with precise folded conformation, have emerged as a promising technology. We introduce oligourea foldamers to reduce the peptide character of inhibitors of protein-protein interactions (PPI). However, the precise design of such mimics is currently limited by the lack of structural information on how these foldamers adapt to protein surfaces. We report a collection of X-ray structures of peptide-oligourea hybrids in complex with ubiquitin ligase MDM2 and vitamin D receptor and show how such hybrid oligomers can be designed to bind with high affinity to protein targets. This work should enable the generation of more effective foldamer-based disruptors of PPIs in the context of peptide lead optimization.

Structural Basis for alpha-Helix Mimicry and Inhibition of Protein-Protein Interactions with Oligourea Foldamers.,Cussol L, Mauran-Ambrosino L, Buratto J, Belorusova AY, Neuville M, Osz J, Fribourg S, Fremaux J, Dolain C, Goudreau SR, Rochel N, Guichard G Angew Chem Int Ed Engl. 2020 Sep 16. doi: 10.1002/anie.202008992. PMID:32935897<ref>PMID:32935897</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 6xzv" style="background-color:#fffaf0;"></div>

==See Also==
*[[Vitamin D receptor 3D structures|Vitamin D receptor 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Danio rerio]]
[[Category: Large Structures]]
[[Category: Synthetic construct]]
[[Category: Belorusova AY]]
[[Category: Buratto J]]
[[Category: Guichard G]]
[[Category: Rochel N]]