5h1e
From Proteopedia
(Difference between revisions)
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| - | '''Unreleased structure''' | ||
| - | + | ==Interaction between vitamin D receptor and coactivator peptide SRC2-3== | |
| + | <StructureSection load='5h1e' size='340' side='right' caption='[[5h1e]], [[Resolution|resolution]] 2.60Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5h1e]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5H1E OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5H1E FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5h1e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5h1e OCA], [http://pdbe.org/5h1e PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5h1e RCSB], [http://www.ebi.ac.uk/pdbsum/5h1e PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5h1e ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Disease == | ||
| + | [[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation. | ||
| + | == 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> [[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.<ref>PMID:9430642</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Vitamin D receptor (VDR) is a member of the nuclear receptor superfamily and regulates the expression of target genes through ligand binding. To express the target gene, coactivator binding to the VDR/ligand complex is essential. Although there are many coactivators in living cells, precise interactions between coactivators and VDR have not been clarified. Here, we synthesized two coactivator peptides, DRIP205-2 and SRC2-3, evaluated their affinity for the ligand-binding domain (LBD) of VDR using 1alpha,25-dihydroxyvitamin D3, partial agonist 1, and antagonist 2 by surface plasmon resonance (SPR), and assessed their interaction modes with VDR-LBD using X-ray crystallographic analysis. This study showed that the SRC2-3 peptide is more sensitive to the ligands (agonist, partial agonist, and antagonist) and shows more intimate interactions with VDR-LBD than DRIP205-2 peptide. | ||
| - | + | SRC2-3 binds to vitamin D receptor with high sensitivity and strong affinity.,Egawa D, Itoh T, Kato A, Kataoka S, Anami Y, Yamamoto K Bioorg Med Chem. 2017 Jan 15;25(2):568-574. doi: 10.1016/j.bmc.2016.11.020. Epub , 2016 Nov 14. PMID:27890450<ref>PMID:27890450</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | <div class="pdbe-citations 5h1e" style="background-color:#fffaf0;"></div> | |
| - | + | == References == | |
| - | + | <references/> | |
| + | __TOC__ | ||
| + | </StructureSection> | ||
[[Category: Anami, Y]] | [[Category: Anami, Y]] | ||
| + | [[Category: Egawa, D]] | ||
[[Category: Itoh, T]] | [[Category: Itoh, T]] | ||
| + | [[Category: Kataoka, S]] | ||
[[Category: Kato, A]] | [[Category: Kato, A]] | ||
| + | [[Category: Yamamoto, K]] | ||
| + | [[Category: Co-factor]] | ||
| + | [[Category: Rxr]] | ||
| + | [[Category: Tif2]] | ||
| + | [[Category: Transcription]] | ||
| + | [[Category: Vdre]] | ||
| + | [[Category: Vitamin d3]] | ||
Revision as of 16:26, 18 January 2017
Interaction between vitamin D receptor and coactivator peptide SRC2-3
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Categories: Anami, Y | Egawa, D | Itoh, T | Kataoka, S | Kato, A | Yamamoto, K | Co-factor | Rxr | Tif2 | Transcription | Vdre | Vitamin d3
