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5k0m

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Current revision (19:17, 20 September 2023) (edit) (undo)
 
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==Targeting the PRC2 complex through a novel protein-protein interaction inhibitor of EED==
==Targeting the PRC2 complex through a novel protein-protein interaction inhibitor of EED==
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<StructureSection load='5k0m' size='340' side='right' caption='[[5k0m]], [[Resolution|resolution]] 1.83&Aring;' scene=''>
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<StructureSection load='5k0m' size='340' side='right'caption='[[5k0m]], [[Resolution|resolution]] 1.83&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5k0m]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5K0M OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5K0M FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5k0m]] is a 1 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=5K0M OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5K0M 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=6PU:(3R,4S)-1-[(1S)-7-FLUORO-2,3-DIHYDRO-1H-INDEN-1-YL]-N,N-DIMETHYL-4-{4-[4-(METHYLSULFONYL)PIPERAZIN-1-YL]PHENYL}PYRROLIDIN-3-AMINE'>6PU</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]] 1.83&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">EED ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=6PU:(3R,4S)-1-[(1S)-7-FLUORO-2,3-DIHYDRO-1H-INDEN-1-YL]-N,N-DIMETHYL-4-{4-[4-(METHYLSULFONYL)PIPERAZIN-1-YL]PHENYL}PYRROLIDIN-3-AMINE'>6PU</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=5k0m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5k0m OCA], [http://pdbe.org/5k0m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5k0m RCSB], [http://www.ebi.ac.uk/pdbsum/5k0m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5k0m 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=5k0m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5k0m OCA], [https://pdbe.org/5k0m PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5k0m RCSB], [https://www.ebi.ac.uk/pdbsum/5k0m PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5k0m ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/EED_HUMAN EED_HUMAN]] Polycomb group (PcG) protein. Component of the PRC2/EED-EZH2 complex, which methylates 'Lys-9' and 'Lys-27' of histone H3, leading to transcriptional repression of the affected target gene. Also recognizes 'Lys-26' trimethylated histone H1 with the effect of inhibiting PRC2 complex methyltransferase activity on nucleosomal histone H3 'Lys-27', whereas H3 'Lys-27' recognition has the opposite effect, enabling the propagation of this repressive mark. The PRC2/EED-EZH2 complex may also serve as a recruiting platform for DNA methyltransferases, thereby linking two epigenetic repression systems. Genes repressed by the PRC2/EED-EZH2 complex include HOXC8, HOXA9, MYT1 and CDKN2A.<ref>PMID:9584199</ref> <ref>PMID:10581039</ref> <ref>PMID:14532106</ref> <ref>PMID:15385962</ref> <ref>PMID:15231737</ref> <ref>PMID:15225548</ref> <ref>PMID:16357870</ref> <ref>PMID:18285464</ref> <ref>PMID:20974918</ref>
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[https://www.uniprot.org/uniprot/EED_HUMAN EED_HUMAN] Polycomb group (PcG) protein. Component of the PRC2/EED-EZH2 complex, which methylates 'Lys-9' and 'Lys-27' of histone H3, leading to transcriptional repression of the affected target gene. Also recognizes 'Lys-26' trimethylated histone H1 with the effect of inhibiting PRC2 complex methyltransferase activity on nucleosomal histone H3 'Lys-27', whereas H3 'Lys-27' recognition has the opposite effect, enabling the propagation of this repressive mark. The PRC2/EED-EZH2 complex may also serve as a recruiting platform for DNA methyltransferases, thereby linking two epigenetic repression systems. Genes repressed by the PRC2/EED-EZH2 complex include HOXC8, HOXA9, MYT1 and CDKN2A.<ref>PMID:9584199</ref> <ref>PMID:10581039</ref> <ref>PMID:14532106</ref> <ref>PMID:15385962</ref> <ref>PMID:15231737</ref> <ref>PMID:15225548</ref> <ref>PMID:16357870</ref> <ref>PMID:18285464</ref> <ref>PMID:20974918</ref>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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</div>
</div>
<div class="pdbe-citations 5k0m" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 5k0m" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Polycomb complex proteins 3D structures|Polycomb complex proteins 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
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[[Category: Bigelow, L J]]
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[[Category: Large Structures]]
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[[Category: Jakob, C G]]
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[[Category: Bigelow LJ]]
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[[Category: Sun, C]]
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[[Category: Jakob CG]]
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[[Category: Zhu, H]]
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[[Category: Sun C]]
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[[Category: Protein binding]]
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[[Category: Zhu H]]
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[[Category: Wd40 prc2]]
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Current revision

Targeting the PRC2 complex through a novel protein-protein interaction inhibitor of EED

PDB ID 5k0m

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