View source for 6fob


==Vitamin D receptor complex 5==
<StructureSection load='6fob' size='340' side='right' caption='[[6fob]], [[Resolution|resolution]] 2.75&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[6fob]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Brachidanio_rerio Brachidanio rerio]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6FOB OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6FOB FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DZW:(1~{R},3~{S},5~{Z})-4-methylidene-5-[(~{E})-3-[3-(6-methyl-6-oxidanyl-heptyl)phenyl]dec-2-enylidene]cyclohexane-1,3-diol'>DZW</scene></td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">vdra, nr1i1a, vdr ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=7955 Brachidanio rerio])</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=6fob FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6fob OCA], [http://pdbe.org/6fob PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6fob RCSB], [http://www.ebi.ac.uk/pdbsum/6fob PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6fob ProSAT]</span></td></tr>
</table>
== Function ==
[[http://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 ==
1We report the design, synthesis, biological evaluation and structural analysis of a new class of vitamin D analogs that possess an aromatic m-phenylene D-ring and an alkyl chain replacing the C-ring. A key feature of the synthetic strategy is a stereoselective Pd-catalyzed construction of the triene system in aqueous medium that allows the rapid preparation of small amounts of VDR ligands for biological screening. Analogs with the shorter (2a) and longer (2d, 2e) side chains attached to the triene system have no calcemic activity. Compound 2a binds to VDR with the same order of magnitude than calcipotriol and oxacalcitriol. It also reduces proliferation in normal and tumor cells similarly to the natural hormone 1a,25-dihydroxyvitamin D3, calcipotriol and oxacalcitriol, suggesting preclinical studies related to hyperproliferative disorders such as psoriasis and cancer.

Aromatic-Based Design of Highly Active and Noncalcemic Vitamin D Receptor Agonists.,Gogoi P, Seoane S, Sigueiro R, Guiberteau T, Maestro MA, Perez-Fernandez R, Rochel N, Mourino A J Med Chem. 2018 May 7. doi: 10.1021/acs.jmedchem.8b00337. PMID:29733645<ref>PMID:29733645</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 6fob" style="background-color:#fffaf0;"></div>
== References ==
<references/>
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</StructureSection>
[[Category: Brachidanio rerio]]
[[Category: Rochel, N]]
[[Category: Gene regulation]]