2vgp

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{{Seed}}
 
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[[Image:2vgp.png|left|200px]]
 
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==Crystal structure of Aurora B kinase in complex with a aminothiazole inhibitor==
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The line below this paragraph, containing "STRUCTURE_2vgp", creates the "Structure Box" on the page.
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<StructureSection load='2vgp' size='340' side='right'caption='[[2vgp]], [[Resolution|resolution]] 1.70&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'>[[2vgp]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VGP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2VGP 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]] 1.7&#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=AD6:4-[(5-BROMO-1,3-THIAZOL-2-YL)AMINO]-N-METHYLBENZAMIDE'>AD6</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
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{{STRUCTURE_2vgp| PDB=2vgp | 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=2vgp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vgp OCA], [https://pdbe.org/2vgp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2vgp RCSB], [https://www.ebi.ac.uk/pdbsum/2vgp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2vgp ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/AUKBA_XENLA AUKBA_XENLA] Serine/threonine-protein kinase component of the chromosomal passenger complex (CPC), a complex that acts as a key regulator of mitosis. The CPC complex has essential functions at the centromere in ensuring correct chromosome alignment and segregation and is required for chromatin-induced microtubule stabilization and spindle assembly. Involved in the bipolar attachment of spindle microtubules to kinetochores and is a key regulator for the onset of cytokinesis during mitosis. Required for central/midzone spindle assembly and cleavage furrow formation. Phosphorylates 'Ser-10' of histone H3 during mitosis.<ref>PMID:12221116</ref> <ref>PMID:11350965</ref> <ref>PMID:17199039</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/vg/2vgp_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=2vgp ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Aurora family kinases regulate important events during mitosis including centrosome maturation and separation, mitotic spindle assembly, and chromosome segregation. Misregulation of Aurora kinases due to genetic amplification and protein overexpression results in aneuploidy and may contribute to tumorigenesis. Here we report the discovery of new small molecule aminothiazole inhibitors of Aurora kinases with exceptional kinase selectivity and report a 1.7 A cocrystal structure with the Aurora B:INCENP complex from Xenopus laevis. The compounds recapitulate the hallmarks of Aurora kinase inhibition, including decreased histone H3 serine 10 phosphorylation, failure to complete cytokinesis, and endoreduplication.
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===CRYSTAL STRUCTURE OF AURORA B KINASE IN COMPLEX WITH A AMINOTHIAZOLE INHIBITOR===
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Discovery of selective aminothiazole aurora kinase inhibitors.,Andersen CB, Wan Y, Chang JW, Riggs B, Lee C, Liu Y, Sessa F, Villa F, Kwiatkowski N, Suzuki M, Nallan L, Heald R, Musacchio A, Gray NS ACS Chem Biol. 2008 Mar 20;3(3):180-92. Epub 2008 Feb 29. PMID:18307303<ref>PMID:18307303</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 2vgp" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_18307303}}, adds the Publication Abstract to the page
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*[[Centromere protein 3D structure|Centromere protein 3D structure]]
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(as it appears on PubMed at http://www.pubmed.gov), where 18307303 is the PubMed ID number.
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*[[Serine/threonine protein kinase 3D structures|Serine/threonine protein kinase 3D structures]]
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== References ==
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{{ABSTRACT_PUBMED_18307303}}
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<references/>
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__TOC__
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==About this Structure==
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</StructureSection>
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2VGP is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2VGP OCA].
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[[Category: Large Structures]]
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==Reference==
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Discovery of selective aminothiazole aurora kinase inhibitors., Andersen CB, Wan Y, Chang JW, Riggs B, Lee C, Liu Y, Sessa F, Villa F, Kwiatkowski N, Suzuki M, Nallan L, Heald R, Musacchio A, Gray NS, ACS Chem Biol. 2008 Mar 20;3(3):180-92. Epub 2008 Feb 29. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/18307303 18307303]
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Protein complex]]
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[[Category: Xenopus laevis]]
[[Category: Xenopus laevis]]
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[[Category: Andersen, C B.]]
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[[Category: Andersen CB]]
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[[Category: Chang, J W.]]
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[[Category: Chang JW]]
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[[Category: Gray, N S.]]
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[[Category: Gray NS]]
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[[Category: Lee, C.]]
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[[Category: Lee C]]
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[[Category: Liu, Y.]]
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[[Category: Liu Y]]
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[[Category: Musacchio, A.]]
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[[Category: Musacchio A]]
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[[Category: Nallan, L.]]
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[[Category: Nallan L]]
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[[Category: Sessa, F.]]
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[[Category: Sessa F]]
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[[Category: Villa, F.]]
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[[Category: Villa F]]
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[[Category: Wan, Y.]]
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[[Category: Wan Y]]
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[[Category: Aminothiazole]]
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[[Category: Atp-binding]]
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[[Category: Aurora b]]
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[[Category: Cancer]]
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[[Category: Cell cycle]]
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[[Category: Cell division]]
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[[Category: Centromere]]
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[[Category: Coiled coil]]
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[[Category: Incenp]]
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[[Category: Kinase]]
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[[Category: Magnesium]]
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[[Category: Metal-binding]]
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[[Category: Microtubule]]
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[[Category: Mitosis]]
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[[Category: Nucleotide-binding]]
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[[Category: Nucleus]]
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[[Category: Phosphorylation]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 20:36:18 2008''
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Current revision

Crystal structure of Aurora B kinase in complex with a aminothiazole inhibitor

PDB ID 2vgp

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