5lga
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Structural analysis and biological activities of BXL0124, a Gemini analog of Vitamin D== | |
| + | <StructureSection load='5lga' size='340' side='right' caption='[[5lga]], [[Resolution|resolution]] 2.50Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5lga]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LGA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5LGA FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6VH:(1~{R},3~{S},5~{Z})-5-[2-[(1~{R},3~{A}~{S},7~{A}~{R})-7~{A}-METHYL-1-[(6~{R})-1,1,1-TRIS(FLUORANYL)-10-METHYL-2,10-BIS(OXIDANYL)-2-(TRIFLUOROMETHYL)UNDECA-3,8-DIYN-6-YL]-2,3,3~{A},5,6,7-HEXAHYDRO-1~{H}-INDEN-4-YLIDENE]ETHYLIDENE]-4-METHYLIDENE-CYCLOHEXANE-1,3-DIOL'>6VH</scene></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=5lga FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lga OCA], [http://pdbe.org/5lga PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lga RCSB], [http://www.ebi.ac.uk/pdbsum/5lga PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lga 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 == | ||
| + | Gemini analogs of calcitriol, characterized by the extension of the C21-methyl group of calcitriol with a second chain, act as agonists of the vitamin D receptor (VDR). This second side chain of gemini is accommodated in a new cavity inside the VDR created by the structural rearrangement of the protein core. The resulting conformational change preserves the active state of the receptor and bestows gemini compounds with biological activities that exceed those of calcitriol. Of particular interest are gemini's anti-cancer properties, and in this study we demonstrate anti-proliferative and tumor-reducing abilities of BXL0124 and BXL0097, differing only by the presence or absence, respectively, of the methylene group on the A ring. BXL0124 acts as a more potent VDR agonist than its 19-nor counterpart by activating VDR-mediated transcription at lower concentrations. In a similar manner, BXL0124 is more active than BXL0097 in growth inhibition of breast cancer cells and reduction of tumor volume. Structural comparisons of BXL0097 and BXL0124, as their VDR complexes, explain the elevated activity of the latter. | ||
| - | + | Structural analysis and biological activities of BXL0124, a gemini analog of vitamin D.,Belorusova AY, Suh N, Lee HJ, So JY, Maehr H, Rochel N J Steroid Biochem Mol Biol. 2016 Sep 17. pii: S0960-0760(16)30251-5. doi:, 10.1016/j.jsbmb.2016.09.015. PMID:27650654<ref>PMID:27650654</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 5lga" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Belorusova, A Y]] | ||
| + | [[Category: Rochel, N]] | ||
| + | [[Category: Agonist]] | ||
| + | [[Category: Gemini]] | ||
| + | [[Category: Transcription]] | ||
| + | [[Category: Vitamin d nuclear receptor]] | ||
Revision as of 17:18, 19 October 2016
Structural analysis and biological activities of BXL0124, a Gemini analog of Vitamin D
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