Figure 1
(a) Schematic diagram showing the relationship between Abl and Bcr-Abl (top), the constructs used for crystallography (middle) and the amino-acid numbers for structural elements mentioned in the text (bottom). The breakpoint cluster region (Bcr) is shown in red and the Abl gene is shown in light blue. The green segment shows the Abl-SH2-binding region of Bcr that, when phosphorylated, is necessary for the activation of the Abl tyrosine kinase (yellow boxes). The blue segment shows the region of the Abl gene that is lost during the reciprocal translocation, which is involved in the down-regulation of the Abl kinase. (b) Chemical structures of compounds mentioned in the text. 1, NVP-AFN941; 2, imatinib; 3, NVP-AFG210; 4, PD180970; 5, NVP-AEG082; 6, nilotinib. |