9cr7

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Current revision (05:33, 30 July 2025) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 9cr7 is ON HOLD until Paper Publication
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==Structure of human SETD8 in complex with covalent inhibitor AM2928==
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<StructureSection load='9cr7' size='340' side='right'caption='[[9cr7]], [[Resolution|resolution]] 2.05&Aring;' scene=''>
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Authors: Babault, N., Park, K.S., Jin, J.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[9cr7]] 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=9CR7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=9CR7 FirstGlance]. <br>
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Description: Structure of human SETD8 in complex with covalent inhibitor AM2928
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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]] 2.05&#8491;</td></tr>
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[[Category: Unreleased Structures]]
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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=H81:N-(3-{[7-(2-aminoethoxy)-6-methoxy-2-(pyrrolidin-1-yl)quinazolin-4-yl]amino}propyl)prop-2-ynamide'>H81</scene></td></tr>
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[[Category: Babault, N]]
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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=9cr7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=9cr7 OCA], [https://pdbe.org/9cr7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=9cr7 RCSB], [https://www.ebi.ac.uk/pdbsum/9cr7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=9cr7 ProSAT]</span></td></tr>
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[[Category: Jin, J]]
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</table>
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[[Category: Park, K.S]]
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== Function ==
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[https://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: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Babault N]]
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[[Category: Jin J]]
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[[Category: Park KS]]

Current revision

Structure of human SETD8 in complex with covalent inhibitor AM2928

PDB ID 9cr7

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