2bfy
From Proteopedia
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==Overview== | ==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 .. | + | 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== | ==About this Structure== | ||
| - | 2BFY is a | + | 2BFY is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis] with H1N as [http://en.wikipedia.org/wiki/ligand ligand]. Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BFY OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transferase complex]] | [[Category: transferase complex]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 14:12:49 2007'' |
Revision as of 12:07, 5 November 2007
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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 with H1N as ligand. Structure known Active Site: AC1. 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 Mon Nov 5 14:12:49 2007
