2bfy

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[[Image:2bfy.gif|left|200px]]
[[Image:2bfy.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2bfy |SIZE=350|CAPTION= <scene name='initialview01'>2bfy</scene>, resolution 1.80&Aring;
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The line below this paragraph, containing "STRUCTURE_2bfy", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:H1n+Binding+Site+For+Chain+B'>AC1</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=H1N:N-[2-OXO-3-((E)-PHENYL{[4-(PIPERIDIN-1-YLMETHYL)PHENYL]IMINO}METHYL)-2,6-DIHYDRO-1H-INDOL-5-YL]ETHANESULFONAMIDE'>H1N</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=
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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=
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{{STRUCTURE_2bfy| PDB=2bfy | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2bfy FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bfy OCA], [http://www.ebi.ac.uk/pdbsum/2bfy PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bfy RCSB]</span>
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}}
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'''COMPLEX OF AURORA-B WITH INCENP AND HESPERIDIN.'''
'''COMPLEX OF AURORA-B WITH INCENP AND HESPERIDIN.'''
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[[Category: Stukenberg, P T.]]
[[Category: Stukenberg, P T.]]
[[Category: Tarricone, C.]]
[[Category: Tarricone, C.]]
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[[Category: inhibition]]
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[[Category: Inhibition]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: mitosis]]
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[[Category: Mitosis]]
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[[Category: transferase complex]]
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[[Category: Transferase complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:14:13 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:05:48 2008''
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Revision as of 17:14, 3 May 2008

Template:STRUCTURE 2bfy

COMPLEX OF AURORA-B WITH INCENP AND HESPERIDIN.


Overview

Aurora family serine/threonine kinases control mitotic progression, and their deregulation is implicated in tumorigenesis. Aurora A and Aurora B, the best-characterized members of mammalian Aurora kinases, are approximately 60% identical but bind to unrelated activating subunits. The structure of the complex of Aurora A with the TPX2 activator has been reported previously. Here, we report the crystal structure of Aurora B in complex with the IN-box segment of the inner centromere protein (INCENP) activator and with the small molecule inhibitor Hesperadin. The Aurora B:INCENP complex is remarkably different from the Aurora A:TPX2 complex. INCENP forms a crown around the small lobe of Aurora B and induces the active conformation of the T loop allosterically. The structure represents an intermediate state of activation of Aurora B in which the Aurora B C-terminal segment stabilizes an open conformation of the catalytic cleft, and a critical ion pair in the kinase active site is impaired. Phosphorylation of two serines in the carboxyl terminus of INCENP generates the fully active kinase.

About this Structure

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

Reference

Mechanism of Aurora B activation by INCENP and inhibition by hesperadin., Sessa F, Mapelli M, Ciferri C, Tarricone C, Areces LB, Schneider TR, Stukenberg PT, Musacchio A, Mol Cell. 2005 Apr 29;18(3):379-91. PMID:15866179 Page seeded by OCA on Sat May 3 20:14:13 2008

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