image
FIGURE 24-19 BCR-ABL protein kinase. (a) Origin of the Philadelphia chromosome from a translocation of the tips of chromosomes 9 and 22 and the oncogenic fusion protein formed by that translocation. (b) The BCR-ABL fusion protein is a constitutively active kinase that phosphorylates multiple signal-transducing proteins. Imatinib binds to the active site of BCR-ABL and inhibits its kinase activity. (c) Imatinib bound to the BCR-ABL active site.
[Data from B. Nagar et al., 2002, Cancer Research 62:4236, PDB ID 1iep]