4fhh

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<StructureSection load='4fhh' size='340' side='right'caption='[[4fhh]], [[Resolution|resolution]] 2.33&Aring;' scene=''>
<StructureSection load='4fhh' size='340' side='right'caption='[[4fhh]], [[Resolution|resolution]] 2.33&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4fhh]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Brachidanio_rerio Brachidanio rerio]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FHH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4FHH FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4fhh]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Danio_rerio Danio rerio] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4FHH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4FHH FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0U3:N-HYDROXY-2-{4-[3-(4-{[(2S)-2-HYDROXY-3,3-DIMETHYLBUTYL]OXY}-3-METHYLPHENYL)PENTAN-3-YL]-2-METHYLPHENOXY}ACETAMIDE'>0U3</scene></td></tr>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0U3:N-HYDROXY-2-{4-[3-(4-{[(2S)-2-HYDROXY-3,3-DIMETHYLBUTYL]OXY}-3-METHYLPHENYL)PENTAN-3-YL]-2-METHYLPHENOXY}ACETAMIDE'>0U3</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[4fhi|4fhi]]</div></td></tr>
 
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">vdra, nr1i1a, vdr ([https://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'>[https://proteopedia.org/fgij/fg.htm?mol=4fhh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fhh OCA], [https://pdbe.org/4fhh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4fhh RCSB], [https://www.ebi.ac.uk/pdbsum/4fhh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4fhh ProSAT]</span></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=4fhh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4fhh OCA], [https://pdbe.org/4fhh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4fhh RCSB], [https://www.ebi.ac.uk/pdbsum/4fhh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4fhh ProSAT]</span></td></tr>
</table>
</table>
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== Disease ==
 
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[[https://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 ==
== Function ==
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[[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> [[https://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>
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[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;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Brachidanio rerio]]
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[[Category: Danio rerio]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Fischer, J]]
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[[Category: Fischer J]]
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[[Category: Gleason, J L]]
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[[Category: Gleason JL]]
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[[Category: Kaldre, D]]
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[[Category: Kaldre D]]
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[[Category: Moras, D]]
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[[Category: Moras D]]
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[[Category: Rochel, N]]
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[[Category: Rochel N]]
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[[Category: Wang, T T]]
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[[Category: Wang TT]]
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[[Category: White, J H]]
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[[Category: White JH]]
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[[Category: Adn coregulator]]
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[[Category: Alpha helical sandwich]]
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[[Category: Apha helical sandwich]]
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[[Category: Ligand binding domain]]
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[[Category: Nucleus]]
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[[Category: Phosphorylation and hdac inhibitor]]
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[[Category: Transcription factor]]
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[[Category: Transcription-protein binding-inhibitor complex]]
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Revision as of 10:40, 14 December 2022

Development of synthetically accessible non-secosteroidal hybrid molecules combining vitamin D receptor agonism and histone deacetylase inhibition

PDB ID 4fhh

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