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2bfy

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[[Category: transferase complex]]
[[Category: transferase complex]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 14:12:49 2007''
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Revision as of 15:31, 5 November 2007

Image:2bfy.gif

2bfy, resolution 1.80Å

Drag the structure with the mouse to rotate

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

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