2vgp

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|PDB= 2vgp |SIZE=350|CAPTION= <scene name='initialview01'>2vgp</scene>, resolution 1.70&Aring;
|PDB= 2vgp |SIZE=350|CAPTION= <scene name='initialview01'>2vgp</scene>, resolution 1.70&Aring;
|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>
|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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|LIGAND= <scene name='pdbligand=AD6:'>AD6</scene>
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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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|ACTIVITY= [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]
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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>
|GENE=
|GENE=
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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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|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.fli-leibniz.de/cgi-bin/ImgLib.pl?CODE=1kfv JenaLib], [http://www.rcsb.org/pdb/explore.do?structureId=2vgp RCSB]</span>
}}
}}
'''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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==Overview==
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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.
==About this Structure==
==About this Structure==
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].
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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==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]
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Non-specific serine/threonine protein kinase]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: Villa, F.]]
[[Category: Villa, F.]]
[[Category: Wan, Y.]]
[[Category: Wan, Y.]]
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[[Category: AD6]]
 
[[Category: aminothiazole]]
[[Category: aminothiazole]]
[[Category: atp-binding]]
[[Category: atp-binding]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:46:27 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Mar 26 10:03:14 2008''

Revision as of 08:03, 26 March 2008

Image:2vgp.jpg


PDB ID 2vgp

Drag the structure with the mouse to rotate
, resolution 1.70Å
Sites: and
Ligands: ,
Activity: Non-specific serine/threonine protein kinase, with EC number 2.7.11.1
Domains: S_TKc, S_TKc, INCENP_ARK-bind
Resources: FirstGlance, OCA, PDBsum, JenaLib, RCSB
Coordinates: save as pdb, mmCIF, xml



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

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