Figure 7 - full size

 

Figure 7.
FIG. 7. STI-571 binding and interactions with c-Kit kinase. A, chemical structure of STI-571 and F[obs] - F[calc] omit difference electron density calculated prior to building the inhibitor into the co-crystal structure, contoured at 3 (blue) and 6 (red). Key hydrogen bonds are depicted. B, stereo view of STI-571 (purple) binding to c-Kit showing key hydrogen bonds formed with the hinge residue Cys673, gatekeeper residue Thr670, and conserved residue Glu640. The polypeptide surrounding Trp557 from the virgin autoinhibited c-Kit structure is shown superimposed on the STI-571 complex structure.

The above figure is reprinted by permission from the ASBMB: J Biol Chem (2004, 279, 31655-31663) copyright 2004.