2bfy: Difference between revisions
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[[Image:2bfy.gif|left|200px]] | [[Image:2bfy.gif|left|200px]] | ||
'''COMPLEX OF AURORA-B WITH INCENP AND HESPERIDIN.''' | {{Structure | ||
|PDB= 2bfy |SIZE=350|CAPTION= <scene name='initialview01'>2bfy</scene>, resolution 1.80Å | |||
|SITE= <scene name='pdbsite=AC1:H1n+Binding+Site+For+Chain+B'>AC1</scene> | |||
|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> | |||
|ACTIVITY= | |||
|GENE= | |||
}} | |||
'''COMPLEX OF AURORA-B WITH INCENP AND HESPERIDIN.''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
2BFY is a [ | 2BFY is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Xenopus_laevis Xenopus laevis]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BFY OCA]. | ||
==Reference== | ==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:[http:// | 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:[http://www.ncbi.nlm.nih.gov/pubmed/15866179 15866179] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Xenopus laevis]] | [[Category: Xenopus laevis]] | ||
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[[Category: transferase complex]] | [[Category: transferase complex]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:01:26 2008'' | ||
Revision as of 17:01, 20 March 2008
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| Coordinates: | save as pdb, mmCIF, xml | ||||||
COMPLEX OF AURORA-B WITH INCENP AND HESPERIDIN.
OverviewOverview
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 StructureAbout this Structure
2BFY is a Protein complex structure of sequences from Xenopus laevis. Full crystallographic information is available from OCA.
ReferenceReference
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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