4wuy: Difference between revisions

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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[1] Huang J, Perez-Burgos L, Placek BJ, Sengupta R, Richter M, Dorsey JA, Kubicek S, Opravil S, Jenuwein T, Berger SL. Repression of p53 activity by Smyd2-mediated methylation. Nature. 2006 Nov 30;444(7119):629-32. Epub 2006 Nov 15. PMID:17108971 doi:10.1038/nature05287

[2] Huang J, Sengupta R, Espejo AB, Lee MG, Dorsey JA, Richter M, Opravil S, Shiekhattar R, Bedford MT, Jenuwein T, Berger SL. p53 is regulated by the lysine demethylase LSD1. Nature. 2007 Sep 6;449(7158):105-8. PMID:17805299 doi:nature06092

[3] Abu-Farha M, Lambert JP, Al-Madhoun AS, Elisma F, Skerjanc IS, Figeys D. The tale of two domains: proteomics and genomics analysis of SMYD2, a new histone methyltransferase. Mol Cell Proteomics. 2008 Mar;7(3):560-72. Epub 2007 Dec 7. PMID:18065756 doi:10.1074/mcp.M700271-MCP200

[4] Saddic LA, West LE, Aslanian A, Yates JR 3rd, Rubin SM, Gozani O, Sage J. Methylation of the retinoblastoma tumor suppressor by SMYD2. J Biol Chem. 2010 Nov 26;285(48):37733-40. doi: 10.1074/jbc.M110.137612. Epub, 2010 Sep 24. PMID:20870719 doi:10.1074/jbc.M110.137612

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-'''Unreleased structure'''
+==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]] 1.63&Aring;' scene=''>
-The entry 4wuy is ON HOLD  until Paper Publication
+== 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>
-Authors: Nguyen, H., Allali-Hassani, A., Antonysamy, S., Chang, S., Chen, L.H., Curtis, C., Emtage, S., Fan, L., Gheyi, T., Li, F., Liu, S., Martin, J.R., Mendel, D., Olsen, J.B., Pelletier, L., Shatseva, T., Wu, S., Zhang, F.F., Arrowsmith, C.H., Brown, P.J., Campbell, R.M., Garcia, B.A., Barsyte-Lovejoy, D., Mader, M., Vedadi, M.
+</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>
-Description:
+</table>
-[[Category: Unreleased Structures]]
+== Function ==
-[[Category: Nguyen, H]]
+[[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>
-[[Category: Olsen, J.B]]
+== References ==
-[[Category: Wu, S]]
+<references/>
-[[Category: Vedadi, M]]
+__TOC__
-[[Category: Pelletier, L]]
+</StructureSection>
+[[Category: Allali-Hassani, A]]
+[[Category: Antonysamy, S]]
+[[Category: Arrowsmith, C H]]
+[[Category: Barsyte-Lovejoy, D]]
+[[Category: Brown, P J]]
+[[Category: Campbell, R M]]
+[[Category: Chang, S]]
+[[Category: Chen, L H]]
+[[Category: Curtis, C]]
+[[Category: Emtage, S]]
 [[Category: Fan, L]]
-[[Category: Mader, M]]
+[[Category: Garcia, B A]]
-[[Category: Curtis, C]]
+[[Category: Gheyi, T]]
 [[Category: Li, F]]
-[[Category: Garcia, B.A]]
-[[Category: Emtage, S]]
-[[Category: Allali-Hassani, A]]
-[[Category: Campbell, R.M]]
-[[Category: Arrowsmith, C.H]]
 [[Category: Liu, S]]
-[[Category: Chen, L.H]]
+[[Category: Mader, M]]
-[[Category: Brown, P.J]]
+[[Category: Martin, J R]]
+[[Category: Mendel, D]]
+[[Category: Nguyen, H]]
+[[Category: Olsen, J B]]
+[[Category: Pelletier, L]]
 [[Category: Shatseva, T]]
-[[Category: Barsyte-Lovejoy, D]]
+[[Category: Vedadi, M]]
-[[Category: Zhang, F.F]]
+[[Category: Wu, S]]
-[[Category: Martin, J.R]]
+[[Category: Zhang, F F]]
-[[Category: Chang, S]]
+[[Category: Smyd2 - lly-507]]
-[[Category: Antonysamy, S]]
+[[Category: Transferase-transferase inhibitor complex]]
-[[Category: Mendel, D]]
-[[Category: Gheyi, T]]

4wuy: Difference between revisions

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

Structural highlights

Function

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