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Figure 3.
Fig. 3. STI-571 exploits the unique conformation of the
activation loop in the down-regulated form of Abl. Conformation
of the activation loops of Abl and the Src kinases Lck (active)
(16) and Hck (inactive) (11). Also shown is a space-filling
model of the Abl-specific inhibitor. The figure was generated by
superimposing the catalytic segments of the displayed kinases.
The structures of Lck and Hck are representative for the active
and the inactive state of Src-family tyrosine kinases,
respectively. The active form of Abl is expected to resemble
that of Lck. The activation loop is magenta, the catalytic
segment green. The conserved side chains of the Asp-Phe-Gly
motif and the tyrosine residue in the activation loop are shown
in a ball-and-stick representation.
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