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ABSTRACT:
SUBMITTER: Elkins JM
PROVIDER: S-EPMC3621106 | biostudies-literature | 2012 Sep
REPOSITORIES: biostudies-literature
Elkins Jonathan M JM Santaguida Stefano S Musacchio Andrea A Knapp Stefan S
Journal of medicinal chemistry 20120904 17
We present the structure of the human Aurora B kinase domain in complex with the C-terminal Aurora-binding region of human INCENP and the Aurora kinase inhibitor VX-680. The structure unexpectedly reveals a dimeric arrangement of the Aurora B:INCENP complex, which was confirmed to exist in solution by analytical ultracentrifugation. The dimerization involves a domain swap of the activation loop, resulting in a different conformation of the DFG motif as compared to that seen in other kinase compl ...[more]