4ynd
From Proteopedia
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| - | ''' | + | ==The Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2== |
| - | + | <StructureSection load='4ynd' size='340' side='right' caption='[[4ynd]], [[Resolution|resolution]] 2.79Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[4ynd]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4YND OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4YND FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=4GQ:N-CYCLOHEXYL-N~3~-[2-(3,4-DICHLOROPHENYL)ETHYL]-N-(2-{[(2R)-2-HYDROXY-2-(3-OXO-3,4-DIHYDRO-2H-1,4-BENZOXAZIN-8-YL)ETHYL]AMINO}ETHYL)-BETA-ALANINAMIDE'>4GQ</scene>, <scene name='pdbligand=SAM:S-ADENOSYLMETHIONINE'>SAM</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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ynd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ynd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ynd RCSB], [http://www.ebi.ac.uk/pdbsum/4ynd PDBsum]</span></td></tr> | |
| - | + | </table> | |
| - | [[Category: | + | == Function == |
| + | [[http://www.uniprot.org/uniprot/SMYD2_HUMAN SMYD2_HUMAN]] Protein-lysine N-methyltransferase that methylates both histones and non-histone proteins. Specifically methylates histone H3 'Lys-4' (H3K4me) and dimethylates histone H3 'Lys-36' (H3K36me2). Has also methyltransferase activity toward non-histone proteins such as p53/TP53 and RB1. Monomethylates 'Lys-370' of p53/TP53, leading to decreased DNA-binding activity and subsequent transcriptional regulation activity of p53/TP53. Monomethylates 'Lys-860' of RB1/RB.<ref>PMID:17108971</ref> <ref>PMID:17805299</ref> <ref>PMID:18065756</ref> <ref>PMID:20870719</ref> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Algire, M]] | ||
| + | [[Category: Arrowsmith, C H]] | ||
| + | [[Category: Brown, P J]] | ||
| + | [[Category: Chiang, G C]] | ||
[[Category: Guo, J]] | [[Category: Guo, J]] | ||
| - | [[Category: | + | [[Category: Jakob, C G]] |
| - | [[Category: | + | [[Category: Kennedy, S]] |
[[Category: Li, F]] | [[Category: Li, F]] | ||
| + | [[Category: Pappano, W N]] | ||
| + | [[Category: Soni, N B]] | ||
| + | [[Category: Sweis, R F]] | ||
| + | [[Category: Vedadi, M]] | ||
[[Category: Wang, Z]] | [[Category: Wang, Z]] | ||
| - | [[Category: | + | [[Category: Epigenetic]] |
| - | [[Category: | + | [[Category: H3k36]] |
| - | [[Category: | + | [[Category: Lysine]] |
| - | [[Category: | + | [[Category: Methyltransferase]] |
| - | [[Category: | + | [[Category: P53]] |
| - | [[Category: | + | [[Category: Smyd2]] |
| - | [[Category: | + | [[Category: Tranferase-transferase inhibitor complex]] |
| - | + | ||
Revision as of 12:20, 20 May 2015
The Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2
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Categories: Algire, M | Arrowsmith, C H | Brown, P J | Chiang, G C | Guo, J | Jakob, C G | Kennedy, S | Li, F | Pappano, W N | Soni, N B | Sweis, R F | Vedadi, M | Wang, Z | Epigenetic | H3k36 | Lysine | Methyltransferase | P53 | Smyd2 | Tranferase-transferase inhibitor complex
