4nvq

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{{STRUCTURE_4nvq| PDB=4nvq | SCENE= }}
 
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===Human G9a in Complex with Inhibitor A-366===
 
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==Function==
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==Human G9a in Complex with Inhibitor A-366==
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[[http://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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<StructureSection load='4nvq' size='340' side='right'caption='[[4nvq]], [[Resolution|resolution]] 2.03&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4nvq]] 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=4NVQ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4NVQ 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]] 2.03&#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=2OD:5-METHOXY-6-[3-(PYRROLIDIN-1-YL)PROPOXY]SPIRO[CYCLOBUTANE-1,3-INDOL]-2-AMINE'>2OD</scene>, <scene name='pdbligand=SAH:S-ADENOSYL-L-HOMOCYSTEINE'>SAH</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=4nvq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nvq OCA], [https://pdbe.org/4nvq PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4nvq RCSB], [https://www.ebi.ac.uk/pdbsum/4nvq PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4nvq 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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==About this Structure==
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==See Also==
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[[4nvq]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NVQ OCA].
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*[[Histone methyltransferase 3D structures|Histone methyltransferase 3D structures]]
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== References ==
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==Reference==
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<references/>
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<references group="xtra"/><references/>
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__TOC__
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[[Category: Brown, P J.]]
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</StructureSection>
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[[Category: Chiang, G G.]]
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[[Category: Homo sapiens]]
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[[Category: Guo, J.]]
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[[Category: Large Structures]]
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[[Category: Li, F.]]
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[[Category: Brown PJ]]
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[[Category: Maag, D.]]
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[[Category: Chiang GG]]
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[[Category: Michaelides, M R.]]
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[[Category: Guo J]]
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[[Category: Pappano, W N.]]
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[[Category: Li F]]
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[[Category: Petros, A M.]]
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[[Category: Maag D]]
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[[Category: Pliushchev, M.]]
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[[Category: Michaelides MR]]
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[[Category: Soni, N B.]]
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[[Category: Pappano WN]]
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[[Category: Sweis, R F.]]
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[[Category: Petros AM]]
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[[Category: Tse, C.]]
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[[Category: Pliushchev M]]
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[[Category: Vedadi, M.]]
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[[Category: Soni NB]]
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[[Category: Lysine methyl transferase]]
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[[Category: Sweis RF]]
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[[Category: Transferase-transferase inhibitor complex]]
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[[Category: Tse C]]
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[[Category: Vedadi M]]

Current revision

Human G9a in Complex with Inhibitor A-366

PDB ID 4nvq

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