6boz

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'''Unreleased structure'''
 
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The entry 6boz is ON HOLD until Paper Publication
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==Structure of human SETD8 in complex with covalent inhibitor MS4138==
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<StructureSection load='6boz' size='340' side='right'caption='[[6boz]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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Authors: Babault, N., Anqi, M., Jin, J.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6boz]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6BOZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6BOZ FirstGlance]. <br>
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Description: Structure of human SETD8 in complex with covalent inhibitor MS4138
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=E1J:N-(3-{[7-(2-aminoethoxy)-6-methoxy-2-(pyrrolidin-1-yl)quinazolin-4-yl]amino}propyl)prop-2-enamide'>E1J</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
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[[Category: Unreleased Structures]]
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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=6boz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6boz OCA], [http://pdbe.org/6boz PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6boz RCSB], [http://www.ebi.ac.uk/pdbsum/6boz PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6boz ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/KMT5A_HUMAN KMT5A_HUMAN]] Protein-lysine N-methyltransferase that monomethylates both histones and non-histone proteins. Specifically monomethylates 'Lys-20' of histone H4 (H4K20me1). H4K20me1 is enriched during mitosis and represents a specific tag for epigenetic transcriptional repression. Mainly functions in euchromatin regions, thereby playing a central role in the silencing of euchromatic genes. Required for cell proliferation, probably by contributing to the maintenance of proper higher-order structure of DNA during mitosis. Involved in chromosome condensation and proper cytokinesis. Nucleosomes are preferred as substrate compared to free histones. Mediates monomethylation of p53/TP53 at 'Lys-382', leading to repress p53/TP53-target genes. Plays a negative role in TGF-beta response regulation and a positive role in cell migration.<ref>PMID:12086618</ref> <ref>PMID:12121615</ref> <ref>PMID:15200950</ref> <ref>PMID:15933069</ref> <ref>PMID:15933070</ref> <ref>PMID:16517599</ref> <ref>PMID:17707234</ref> <ref>PMID:23478445</ref>
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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: Large Structures]]
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[[Category: Anqi, M]]
[[Category: Babault, N]]
[[Category: Babault, N]]
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[[Category: Anqi, M]]
 
[[Category: Jin, J]]
[[Category: Jin, J]]
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[[Category: Protein-small molecule inhibitor complex]]
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[[Category: Transferase-transferase inhibitor complex]]

Revision as of 08:41, 1 May 2019

Structure of human SETD8 in complex with covalent inhibitor MS4138

PDB ID 6boz

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