2vgp

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[[Image:2vgp.jpg|left|200px]]
[[Image:2vgp.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2vgp |SIZE=350|CAPTION= <scene name='initialview01'>2vgp</scene>, resolution 1.70&Aring;
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The line below this paragraph, containing "STRUCTURE_2vgp", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Ad6+Binding+Site+For+Chain+A'>AC1</scene> and <scene name='pdbsite=AC2:Ad6+Binding+Site+For+Chain+B'>AC2</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=AD6:4-[(5-BROMO-1,3-THIAZOL-2-YL)AMINO]-N-METHYLBENZAMIDE'>AD6</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=<span class='plainlinks'>[http://www.ncbi.nlm.nih.gov/Structure/cdd/cddsrv.cgi?uid=smart00220 S_TKc], [http://www.ncbi.nlm.nih.gov/Structure/cdd/cddsrv.cgi?uid=cd00180 S_TKc], [http://www.ncbi.nlm.nih.gov/Structure/cdd/cddsrv.cgi?uid=pfam03941 INCENP_ARK-bind]</span>
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{{STRUCTURE_2vgp| PDB=2vgp | SCENE= }}
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|RELATEDENTRY=[[2bfx|2BFX]], [[2bfy|2BFY]], [[2vgo|2VGO]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2vgp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vgp OCA], [http://www.ebi.ac.uk/pdbsum/2vgp PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2vgp RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF AURORA B KINASE IN COMPLEX WITH A AMINOTHIAZOLE INHIBITOR'''
'''CRYSTAL STRUCTURE OF AURORA B KINASE IN COMPLEX WITH A AMINOTHIAZOLE INHIBITOR'''
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[[Category: Villa, F.]]
[[Category: Villa, F.]]
[[Category: Wan, Y.]]
[[Category: Wan, Y.]]
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[[Category: aminothiazole]]
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[[Category: Aminothiazole]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: aurora b]]
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[[Category: Aurora b]]
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[[Category: cancer]]
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[[Category: Cancer]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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[[Category: cell division]]
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[[Category: Cell division]]
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[[Category: centromere]]
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[[Category: Centromere]]
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[[Category: coiled coil]]
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[[Category: Coiled coil]]
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[[Category: incenp]]
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[[Category: Incenp]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: magnesium]]
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[[Category: Magnesium]]
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[[Category: metal-binding]]
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[[Category: Metal-binding]]
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[[Category: microtubule]]
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[[Category: Microtubule]]
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[[Category: mitosis]]
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[[Category: Mitosis]]
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[[Category: nucleotide-binding]]
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[[Category: Nucleotide-binding]]
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[[Category: nucleus]]
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[[Category: Nucleus]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 18:46:35 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:12:02 2008''
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Revision as of 15:46, 4 May 2008

Image:2vgp.jpg

Template:STRUCTURE 2vgp

CRYSTAL STRUCTURE OF AURORA B KINASE IN COMPLEX WITH A AMINOTHIAZOLE INHIBITOR


Overview

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.

About this Structure

2VGP is a Protein complex structure of sequences from Xenopus laevis. Full crystallographic information is available from OCA.

Reference

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 Page seeded by OCA on Sun May 4 18:46:35 2008

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