6g5n

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==Crystal structure of human SP100 in complex with bromodomain-focused fragment XS039818e 1-(3-Phenyl-1,2,4-oxadiazol-5-yl)methanamine==
==Crystal structure of human SP100 in complex with bromodomain-focused fragment XS039818e 1-(3-Phenyl-1,2,4-oxadiazol-5-yl)methanamine==
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<StructureSection load='6g5n' size='340' side='right' caption='[[6g5n]], [[Resolution|resolution]] 1.77&Aring;' scene=''>
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<StructureSection load='6g5n' size='340' side='right'caption='[[6g5n]], [[Resolution|resolution]] 1.77&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[6g5n]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6G5N OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6G5N FirstGlance]. <br>
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<table><tr><td colspan='2'>[[6g5n]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6G5N OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6G5N FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=ENK:(3-phenyl-1,2,4-oxadiazol-5-yl)methanamine'>ENK</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.765&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5pwc|5pwc]]</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=ENK:(3-phenyl-1,2,4-oxadiazol-5-yl)methanamine'>ENK</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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<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=6g5n FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6g5n OCA], [http://pdbe.org/6g5n PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6g5n RCSB], [http://www.ebi.ac.uk/pdbsum/6g5n PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6g5n ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6g5n FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6g5n OCA], [https://pdbe.org/6g5n PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6g5n RCSB], [https://www.ebi.ac.uk/pdbsum/6g5n PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6g5n ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/SP100_HUMAN SP100_HUMAN]] Together with PML, this tumor suppressor is a major constituent of the PML bodies, a subnuclear organelle involved in a large number of physiological processes including cell growth, differentiation and apoptosis. Functions as a transcriptional coactivator of ETS1 and ETS2 according to PubMed:11909962. Under certain conditions, it may also act as a corepressor of ETS1 preventing its binding to DNA according to PubMed:15247905. Through the regulation of ETS1 it may play a role in angiogenesis, controlling endothelial cell motility and invasion. Through interaction with the MRN complex it may be involved in the regulation of telomeres lengthening. May also regulate TP53-mediated transcription and through CASP8AP2, regulate FAS-mediated apoptosis. Also plays a role in infection by viruses, including human cytomegalovirus and Epstein-Barr virus, through mechanisms that may involve chromatin and/or transcriptional regulation.<ref>PMID:11909962</ref> <ref>PMID:14647468</ref> <ref>PMID:15247905</ref> <ref>PMID:15592518</ref> <ref>PMID:15767676</ref> <ref>PMID:16177824</ref> <ref>PMID:17245429</ref> <ref>PMID:21274506</ref> <ref>PMID:21880768</ref>
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[https://www.uniprot.org/uniprot/SP100_HUMAN SP100_HUMAN] Together with PML, this tumor suppressor is a major constituent of the PML bodies, a subnuclear organelle involved in a large number of physiological processes including cell growth, differentiation and apoptosis. Functions as a transcriptional coactivator of ETS1 and ETS2 according to PubMed:11909962. Under certain conditions, it may also act as a corepressor of ETS1 preventing its binding to DNA according to PubMed:15247905. Through the regulation of ETS1 it may play a role in angiogenesis, controlling endothelial cell motility and invasion. Through interaction with the MRN complex it may be involved in the regulation of telomeres lengthening. May also regulate TP53-mediated transcription and through CASP8AP2, regulate FAS-mediated apoptosis. Also plays a role in infection by viruses, including human cytomegalovirus and Epstein-Barr virus, through mechanisms that may involve chromatin and/or transcriptional regulation.<ref>PMID:11909962</ref> <ref>PMID:14647468</ref> <ref>PMID:15247905</ref> <ref>PMID:15592518</ref> <ref>PMID:15767676</ref> <ref>PMID:16177824</ref> <ref>PMID:17245429</ref> <ref>PMID:21274506</ref> <ref>PMID:21880768</ref>
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Arrowsmith, C H]]
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[[Category: Homo sapiens]]
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[[Category: Bountra, C]]
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[[Category: Large Structures]]
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[[Category: Brandao-Neto, J]]
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[[Category: Arrowsmith CH]]
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[[Category: Brennan, P E]]
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[[Category: Bountra C]]
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[[Category: Burgess-Brown, N]]
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[[Category: Brandao-Neto J]]
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[[Category: Collins, P]]
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[[Category: Brennan PE]]
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[[Category: Delft, F von]]
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[[Category: Burgess-Brown N]]
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[[Category: Douangamath, A]]
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[[Category: Collins P]]
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[[Category: Edwards, A M]]
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[[Category: Douangamath A]]
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[[Category: Fairhead, M]]
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[[Category: Edwards AM]]
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[[Category: Huber, K]]
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[[Category: Fairhead M]]
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[[Category: Knapp, S]]
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[[Category: Huber K]]
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[[Category: Krojer, T]]
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[[Category: Knapp S]]
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[[Category: MacLean, E]]
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[[Category: Krojer T]]
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[[Category: Ng, J]]
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[[Category: MacLean E]]
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[[Category: Nunez-Alonso, G]]
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[[Category: Ng J]]
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[[Category: Pearce, N M]]
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[[Category: Nunez-Alonso G]]
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[[Category: Szykowska, A]]
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[[Category: Pearce NM]]
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[[Category: Tallant, C]]
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[[Category: Szykowska A]]
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[[Category: Talon, R P.H]]
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[[Category: Tallant C]]
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[[Category: Wright, N]]
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[[Category: Talon RPH]]
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[[Category: Bromodomain]]
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[[Category: Wright N]]
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[[Category: Diamond i04-1]]
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[[Category: Von Delft F]]
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[[Category: Epigenetic]]
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[[Category: Fragment screening]]
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[[Category: Pandda]]
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[[Category: Sgc]]
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[[Category: Structural genomic]]
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[[Category: Transcription]]
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[[Category: Xchem]]
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[[Category: Xchemexplorer]]
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Current revision

Crystal structure of human SP100 in complex with bromodomain-focused fragment XS039818e 1-(3-Phenyl-1,2,4-oxadiazol-5-yl)methanamine

PDB ID 6g5n

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OCA

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