3rjw

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'''Unreleased structure'''
 
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The entry 3rjw is ON HOLD
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==Crystal structure of histone lysine methyltransferase g9a with an inhibitor==
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<StructureSection load='3rjw' size='340' side='right'caption='[[3rjw]], [[Resolution|resolution]] 2.56&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3rjw]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=3nni 3nni]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RJW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RJW FirstGlance]. <br>
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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]] 2.56&#8491;</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=CIQ:2-CYCLOHEXYL-6-METHOXY-N-[1-(1-METHYLETHYL)PIPERIDIN-4-YL]-7-(3-PYRROLIDIN-1-YLPROPOXY)QUINAZOLIN-4-AMINE'>CIQ</scene>, <scene name='pdbligand=SAH:S-ADENOSYL-L-HOMOCYSTEINE'>SAH</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</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'>[https://proteopedia.org/fgij/fg.htm?mol=3rjw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rjw OCA], [https://pdbe.org/3rjw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rjw RCSB], [https://www.ebi.ac.uk/pdbsum/3rjw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rjw ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/EHMT2_HUMAN EHMT2_HUMAN] Histone methyltransferase that specifically mono- and dimethylates 'Lys-9' of histone H3 (H3K9me1 and H3K9me2, respectively) in euchromatin. H3K9me represents a specific tag for epigenetic transcriptional repression by recruiting HP1 proteins to methylated histones. Also mediates monomethylation of 'Lys-56' of histone H3 (H3K56me1) in G1 phase, leading to promote interaction between histone H3 and PCNA and regulating DNA replication. Also weakly methylates 'Lys-27' of histone H3 (H3K27me). Also required for DNA methylation, the histone methyltransferase activity is not required for DNA methylation, suggesting that these 2 activities function independently. Probably targeted to histone H3 by different DNA-binding proteins like E2F6, MGA, MAX and/or DP1. May also methylate histone H1. In addition to the histone methyltransferase activity, also methylates non-histone proteins: mediates dimethylation of 'Lys-373' of p53/TP53. Also methylates CDYL, WIZ, ACIN1, DNMT1, HDAC1, ERCC6, KLF12 and itself.<ref>PMID:8457211</ref> <ref>PMID:11316813</ref> <ref>PMID:18438403</ref> <ref>PMID:20118233</ref> <ref>PMID:22387026</ref>
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Authors: Dong, A., Wasney, G.A., Tempel, W., Liu, F., Barsyte, D., Allali-Hassani, A., Chen, X., Chau, I., Hajian, T., Senisterra, G., Chavda, N., Arora, K., Siarheyeva, A., Kireev, D.B., Herold, J.M., Bochkarev, A., Bountra, C., Weigelt, J., Edwards, A.M., Frye, S.V., Arrowsmith, C.H., Brown, P.J., Jin, J., Vedadi, M., Structural Genomics Consortium (SGC)
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==See Also==
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*[[Histone methyltransferase 3D structures|Histone methyltransferase 3D structures]]
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Description: Crystal structure of histone lysine methyltransferase g9a with an inhibitor
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Allali-Hassani A]]
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[[Category: Arora K]]
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[[Category: Arrowsmith CH]]
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[[Category: Barsyte D]]
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[[Category: Bochkarev A]]
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[[Category: Bountra C]]
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[[Category: Brown PJ]]
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[[Category: Chau I]]
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[[Category: Chavda N]]
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[[Category: Chen X]]
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[[Category: Dong A]]
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[[Category: Edwards AM]]
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[[Category: Frye SV]]
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[[Category: Hajian T]]
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[[Category: Herold JM]]
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[[Category: Jin J]]
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[[Category: Kireev DB]]
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[[Category: Liu F]]
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[[Category: Senisterra G]]
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[[Category: Siarheyeva A]]
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[[Category: Tempel W]]
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[[Category: Vedadi M]]
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[[Category: Wasney GA]]
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[[Category: Weigelt J]]

Current revision

Crystal structure of histone lysine methyltransferase g9a with an inhibitor

PDB ID 3rjw

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