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3wt5

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'''Unreleased structure'''
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==A mixed population of antagonist and agonist binding conformers in a single crystal explains partial agonism against vitamin D receptor: Active vitamin D analogues with 22R-alkyl group==
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<StructureSection load='3wt5' size='340' side='right' caption='[[3wt5]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3wt5]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3WT5 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3WT5 FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=YA1:(1R,3R,7E,17BETA)-17-[(2R,3R)-3-BUTYL-6-HYDROXY-6-METHYLHEPTAN-2-YL]-2-METHYLIDENE-9,10-SECOESTRA-5,7-DIENE-1,3-DIOL'>YA1</scene><br>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3wt6|3wt6]], [[3wt7|3wt7]]</td></tr>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3wt5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3wt5 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3wt5 RCSB], [http://www.ebi.ac.uk/pdbsum/3wt5 PDBsum]</span></td></tr>
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<table>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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We are continuing to study the structural basis of vitamin D receptor (VDR) agonism and antagonism by using 22S-alkyl vitamin D analogues. Here we report the synthesis and biological evaluation of 22R-alkyl analogues and the X-ray crystallographic analysis of vitamin D receptor ligand-binding domain (VDR-LBD) complexed with a 22R-analogue. VDR-LBD complexed with the partial agonist 8a showed that 8a binds to VDR-LBD with two conformations, one of which is the antagonist/VDR-LBD complex structure and the other is the agonist/VDR-LBD complex structure. The results indicate that the partial agonist activity of 8a depends on the sum of antagonistic and agonistic activities caused by the antagonist and agonist binding conformers, respectively. The structural basis observed here must be applicable to the partial agonism of other ligand-dependent nuclear receptors. This is the first report describing the trapping of a conformational subset of the ligand and the nuclear receptor in a single crystal.
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The entry 3wt5 is ON HOLD
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A Mixed Population of Antagonist and Agonist Binding Conformers in a Single Crystal Explains Partial Agonism against Vitamin D Receptor: Active Vitamin D Analogues with 22R-Alkyl Group.,Anami Y, Itoh T, Egawa D, Yoshimoto N, Yamamoto K J Med Chem. 2014 May 22;57(10):4351-67. doi: 10.1021/jm500392t. Epub 2014 Apr 29. PMID:24742174<ref>PMID:24742174</ref>
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Authors: Anami, Y., Itoh, T., Yamamoto, K.
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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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Description: A mixed population of antagonist and agonist binding conformers in a single crystal explains partial agonism against vitamin D receptor: Active vitamin D analogues with 22R-alkyl group
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Anami, Y.]]
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[[Category: Itoh, T.]]
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[[Category: Yamamoto, K.]]
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[[Category: Co-factor]]
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[[Category: Nuclear]]
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[[Category: Rxr]]
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[[Category: Transcription]]
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[[Category: Vdre]]
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[[Category: Vitamin d3]]

Revision as of 08:45, 11 June 2014

A mixed population of antagonist and agonist binding conformers in a single crystal explains partial agonism against vitamin D receptor: Active vitamin D analogues with 22R-alkyl group

3wt5, resolution 1.90Å

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