2pzy

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[[Image:2pzy.jpg|left|200px]]
 
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==Structure of MK2 Complexed with Compound 76==
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The line below this paragraph, containing "STRUCTURE_2pzy", creates the "Structure Box" on the page.
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<StructureSection load='2pzy' size='340' side='right'caption='[[2pzy]], [[Resolution|resolution]] 2.90&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[2pzy]] is a 4 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=2PZY OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2PZY FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 2.9&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=B18:(4R)-N-[4-({[2-(DIMETHYLAMINO)ETHYL]AMINO}CARBONYL)-1,3-THIAZOL-2-YL]-4-METHYL-1-OXO-2,3,4,9-TETRAHYDRO-1H-BETA-CARBOLINE-6-CARBOXAMIDE'>B18</scene>, <scene name='pdbligand=STU:STAUROSPORINE'>STU</scene></td></tr>
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{{STRUCTURE_2pzy| PDB=2pzy | SCENE= }}
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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=2pzy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2pzy OCA], [https://pdbe.org/2pzy PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2pzy RCSB], [https://www.ebi.ac.uk/pdbsum/2pzy PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2pzy ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/MAPK2_HUMAN MAPK2_HUMAN] Stress-activated serine/threonine-protein kinase involved in cytokines production, endocytosis, reorganization of the cytoskeleton, cell migration, cell cycle control, chromatin remodeling, DNA damage response and transcriptional regulation. Following stress, it is phosphorylated and activated by MAP kinase p38-alpha/MAPK14, leading to phosphorylation of substrates. Phosphorylates serine in the peptide sequence, Hyd-X-R-X(2)-S, where Hyd is a large hydrophobic residue. Phosphorylates ALOX5, CDC25B, CDC25C, ELAVL1, HNRNPA0, HSF1, HSP27/HSPB1, KRT18, KRT20, LIMK1, LSP1, PABPC1, PARN, PDE4A, RCSD1, RPS6KA3, TAB3 and TTP/ZFP36. Mediates phosphorylation of HSP27/HSPB1 in response to stress, leading to dissociate HSP27/HSPB1 from large small heat-shock protein (sHsps) oligomers and impair their chaperone activities and ability to protect against oxidative stress effectively. Involved in inflammatory response by regulating tumor necrosis factor (TNF) and IL6 production post-transcriptionally: acts by phosphorylating AU-rich elements (AREs)-binding proteins ELAVL1, HNRNPA0, PABPC1 and TTP/ZFP36, leading to regulate the stability and translation of TNF and IL6 mRNAs. Phosphorylation of TTP/ZFP36, a major post-transcriptional regulator of TNF, promotes its binding to 14-3-3 proteins and reduces its ARE mRNA affinity leading to inhibition of dependent degradation of ARE-containing transcript. Also involved in late G2/M checkpoint following DNA damage through a process of post-transcriptional mRNA stabilization: following DNA damage, relocalizes from nucleus to cytoplasm and phosphorylates HNRNPA0 and PARN, leading to stabilize GADD45A mRNA. Involved in toll-like receptor signaling pathway (TLR) in dendritic cells: required for acute TLR-induced macropinocytosis by phosphorylating and activating RPS6KA3.<ref>PMID:8280084</ref> <ref>PMID:8093612</ref> <ref>PMID:8774846</ref> <ref>PMID:10383393</ref> <ref>PMID:12456657</ref> <ref>PMID:11844797</ref> <ref>PMID:12565831</ref> <ref>PMID:14499342</ref> <ref>PMID:14517288</ref> <ref>PMID:15014438</ref> <ref>PMID:15629715</ref> <ref>PMID:16456544</ref> <ref>PMID:16278218</ref> <ref>PMID:17481585</ref> <ref>PMID:18021073</ref> <ref>PMID:20932473</ref>
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/pz/2pzy_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2pzy ConSurf].
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<div style="clear:both"></div>
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'''Structure of MK2 Complexed with Compound 76'''
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==See Also==
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*[[Mitogen-activated protein kinase 3D structures|Mitogen-activated protein kinase 3D structures]]
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== References ==
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==Overview==
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<references/>
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The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a.
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__TOC__
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</StructureSection>
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==About this Structure==
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2PZY is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2PZY OCA].
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==Reference==
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The discovery of carboline analogs as potent MAPKAP-K2 inhibitors., Wu JP, Wang J, Abeywardane A, Andersen D, Emmanuel M, Gautschi E, Goldberg DR, Kashem MA, Lukas S, Mao W, Martin L, Morwick T, Moss N, Pargellis C, Patel UR, Patnaude L, Peet GW, Skow D, Snow RJ, Ward Y, Werneburg B, White A, Bioorg Med Chem Lett. 2007 Aug 15;17(16):4664-9. Epub 2007 Jun 7. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17576063 17576063]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Large Structures]]
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[[Category: Single protein]]
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[[Category: Abeywardane A]]
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[[Category: Abeywardane, A.]]
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[[Category: Andersen D]]
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[[Category: Andersen, D.]]
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[[Category: Emmanuel M]]
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[[Category: Emmanuel, M.]]
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[[Category: Gautschi E]]
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[[Category: Gautschi, E.]]
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[[Category: Goldberg DR]]
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[[Category: Goldberg, D R.]]
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[[Category: Kashem MA]]
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[[Category: Kashem, M A.]]
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[[Category: Lukas S]]
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[[Category: Lukas, S.]]
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[[Category: Mao W]]
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[[Category: Mao, W.]]
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[[Category: Martin L]]
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[[Category: Martin, L.]]
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[[Category: Morwick T]]
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[[Category: Morwick, T.]]
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[[Category: Moss N]]
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[[Category: Moss, N.]]
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[[Category: Pargellis C]]
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[[Category: Pargellis, C.]]
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[[Category: Patel UR]]
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[[Category: Patel, U R.]]
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[[Category: Patnaude L]]
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[[Category: Patnaude, L.]]
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[[Category: Peet GW]]
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[[Category: Peet, G W.]]
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[[Category: Skow D]]
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[[Category: Skow, D.]]
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[[Category: Snow RJ]]
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[[Category: Snow, R J.]]
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[[Category: Wang J]]
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[[Category: Wang, J.]]
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[[Category: Ward Y]]
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[[Category: Ward, Y.]]
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[[Category: Werneburg B]]
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[[Category: Werneburg, B.]]
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[[Category: White A]]
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[[Category: White, A.]]
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[[Category: Wu JP]]
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[[Category: Wu, J P.]]
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[[Category: Mk2]]
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[[Category: Protein kinase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:05:10 2008''
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Current revision

Structure of MK2 Complexed with Compound 76

PDB ID 2pzy

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