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5ij7
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | The entry | + | ==Structure of Hs/AcPRC2 in complex with a pyridone inhibitor== |
| + | <StructureSection load='5ij7' size='340' side='right'caption='[[5ij7]], [[Resolution|resolution]] 2.62Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5ij7]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Anolis_carolinensis Anolis carolinensis] 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=5IJ7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5IJ7 FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.62Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6BN:5,8-DICHLORO-2-[(4-ETHYL-6-METHYL-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL]-7-({1-[(2R)-2-HYDROXYPROPANOYL]PIPERIDIN-4-YL}OXY)-3,4-DIHYDROISOQUINOLIN-1(2H)-ONE'>6BN</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></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=5ij7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ij7 OCA], [https://pdbe.org/5ij7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5ij7 RCSB], [https://www.ebi.ac.uk/pdbsum/5ij7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5ij7 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Disease == | ||
| + | [https://www.uniprot.org/uniprot/EZH2_HUMAN EZH2_HUMAN] Weaver syndrome. The disease is caused by mutations affecting the gene represented in this entry. | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/EZH2_HUMAN EZH2_HUMAN] Polycomb group (PcG) protein. Catalytic subunit of the PRC2/EED-EZH2 complex, which methylates 'Lys-9' (H3K9me) and 'Lys-27' (H3K27me) of histone H3, leading to transcriptional repression of the affected target gene. Able to mono-, di- and trimethylate 'Lys-27' of histone H3 to form H3K27me1, H3K27me2 and H3K27me3, respectively. Compared to EZH2-containing complexes, it is more abundant in embryonic stem cells and plays a major role in forming H3K27me3, which is required for embryonic stem cell identity and proper differentiation. 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, CDKN2A and retinoic acid target genes. EZH2 can also methylate non-histone proteins such as the transcription factor GATA4 and the nuclear receptor RORA.<ref>PMID:14532106</ref> <ref>PMID:15385962</ref> <ref>PMID:15231737</ref> <ref>PMID:15225548</ref> <ref>PMID:16179254</ref> <ref>PMID:16618801</ref> <ref>PMID:16357870</ref> <ref>PMID:16936726</ref> <ref>PMID:17210787</ref> <ref>PMID:17344414</ref> <ref>PMID:19026781</ref> <ref>PMID:18285464</ref> <ref>PMID:20935635</ref> <ref>PMID:23063525</ref> [https://www.uniprot.org/uniprot/G1KPH4_ANOCA G1KPH4_ANOCA] | ||
| - | + | ==See Also== | |
| - | + | *[[Polycomb complex proteins 3D structures|Polycomb complex proteins 3D structures]] | |
| - | + | == References == | |
| - | [[Category: | + | <references/> |
| - | [[Category: | + | __TOC__ |
| - | [[Category: Brooun | + | </StructureSection> |
| + | [[Category: Anolis carolinensis]] | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Brooun A]] | ||
| + | [[Category: Deng Y-L]] | ||
| + | [[Category: Gajiwala KS]] | ||
| + | [[Category: Liu W]] | ||
Current revision
Structure of Hs/AcPRC2 in complex with a pyridone inhibitor
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