4wuy
From Proteopedia
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| - | ''' | + | ==Crystal Structure of Protein Lysine Methyltransferase SMYD2 in complex with LLY-507, a Cell-Active, Potent and Selective Inhibitor== |
| - | + | <StructureSection load='4wuy' size='340' side='right' caption='[[4wuy]], [[Resolution|resolution]] 1.63Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[4wuy]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4WUY OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4WUY FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3UJ:5-CYANO-2-{4-[2-(3-METHYL-1H-INDOL-1-YL)ETHYL]PIPERAZIN-1-YL}-N-[3-(PYRROLIDIN-1-YL)PROPYL]BIPHENYL-3-CARBOXAMIDE'>3UJ</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SAH:S-ADENOSYL-L-HOMOCYSTEINE'>SAH</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=4wuy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4wuy OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4wuy RCSB], [http://www.ebi.ac.uk/pdbsum/4wuy PDBsum]</span></td></tr> | |
| - | + | </table> | |
| - | [[ | + | == 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> | |
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[[Category: Allali-Hassani, A]] | [[Category: Allali-Hassani, A]] | ||
| - | [[Category: | + | [[Category: Antonysamy, S]] |
| - | [[Category: Arrowsmith, C | + | [[Category: Arrowsmith, C H]] |
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[[Category: Barsyte-Lovejoy, D]] | [[Category: Barsyte-Lovejoy, D]] | ||
| - | [[Category: | + | [[Category: Brown, P J]] |
| - | [[Category: | + | [[Category: Campbell, R M]] |
[[Category: Chang, S]] | [[Category: Chang, S]] | ||
| - | [[Category: | + | [[Category: Chen, L H]] |
| - | [[Category: | + | [[Category: Curtis, C]] |
| + | [[Category: Emtage, S]] | ||
| + | [[Category: Fan, L]] | ||
| + | [[Category: Garcia, B A]] | ||
[[Category: Gheyi, T]] | [[Category: Gheyi, T]] | ||
| + | [[Category: Li, F]] | ||
| + | [[Category: Liu, S]] | ||
| + | [[Category: Mader, M]] | ||
| + | [[Category: Martin, J R]] | ||
| + | [[Category: Mendel, D]] | ||
| + | [[Category: Nguyen, H]] | ||
| + | [[Category: Olsen, J B]] | ||
| + | [[Category: Pelletier, L]] | ||
| + | [[Category: Shatseva, T]] | ||
| + | [[Category: Vedadi, M]] | ||
| + | [[Category: Wu, S]] | ||
| + | [[Category: Zhang, F F]] | ||
| + | [[Category: Smyd2 - lly-507]] | ||
| + | [[Category: Transferase-transferase inhibitor complex]] | ||
Revision as of 11:17, 8 April 2015
Crystal Structure of Protein Lysine Methyltransferase SMYD2 in complex with LLY-507, a Cell-Active, Potent and Selective Inhibitor
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Categories: Allali-Hassani, A | Antonysamy, S | Arrowsmith, C H | Barsyte-Lovejoy, D | Brown, P J | Campbell, R M | Chang, S | Chen, L H | Curtis, C | Emtage, S | Fan, L | Garcia, B A | Gheyi, T | Li, F | Liu, S | Mader, M | Martin, J R | Mendel, D | Nguyen, H | Olsen, J B | Pelletier, L | Shatseva, T | Vedadi, M | Wu, S | Zhang, F F | Smyd2 - lly-507 | Transferase-transferase inhibitor complex
