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Figure 1.
Figure 1. Structure and Inhibitor of the Extended Kinase
Domain of Bub1
(A) Domain architecture of human Bub1. TPR,
tetratricopeptide repeat; GLEBS, Gle2-binding sequence; KEN,
lysine-glutamate-asparagine.
(B) Ribbon drawing of the
crystal structure of the extended kinase domain of Bub1. The
N-terminal extension is colored yellow. The substrate-binding
P+1 loop is shown in green, while the rest of the activation
segment is in blue. The catalytic loop is shown in red. ATP is
shown as sticks. The Mg^2+ ion is shown as a gray sphere. The N
and C termini are indicated. All structure figures were
generated with PyMOL (http://pymol.sourceforge.net/).
(C)
The ATP-binding site of Bub1. ATP is shown as sticks. The extra
pocket is indicated.
(D) The chemical structure of
2OH-BNPP1.
(E) Determination of the IC[50] values of
2OH-BNPP1 against Aurora B, p38, Bub1C, and Bub1.
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