2bfx
From Proteopedia
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[[Image:2bfx.gif|left|200px]] | [[Image:2bfx.gif|left|200px]] | ||
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'''MECHANISM OF AURORA-B ACTIVATION BY INCENP AND INHIBITION BY HESPERIDIN.''' | '''MECHANISM OF AURORA-B ACTIVATION BY INCENP AND INHIBITION BY HESPERIDIN.''' | ||
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[[Category: Stukenberg, P T.]] | [[Category: Stukenberg, P T.]] | ||
[[Category: Tarricone, C.]] | [[Category: Tarricone, C.]] | ||
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| - | [[Category: | + | [[Category: Kinase]] |
| - | [[Category: | + | [[Category: Mitosis]] |
| - | [[Category: | + | [[Category: Transferase complex]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:14:10 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 17:14, 3 May 2008
MECHANISM OF AURORA-B ACTIVATION BY INCENP AND INHIBITION BY 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
2BFX 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 20:14:10 2008
