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| [[Image:2bfy.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_2bfy| PDB=2bfy | SCENE= }} | | {{STRUCTURE_2bfy| PDB=2bfy | SCENE= }} |
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| '''COMPLEX OF AURORA-B WITH INCENP AND HESPERIDIN.'''
| | ===COMPLEX OF AURORA-B WITH INCENP AND HESPERIDIN.=== |
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| ==Overview==
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| 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.
| | The line below this paragraph, {{ABSTRACT_PUBMED_15866179}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 15866179 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_15866179}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Mitosis]] | | [[Category: Mitosis]] |
| [[Category: Transferase complex]] | | [[Category: Transferase complex]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:14:13 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 04:46:35 2008'' |
