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. Author manuscript; available in PMC: 2022 Sep 1.
Published in final edited form as: Blood Rev. 2021 Mar 16;49:100825. doi: 10.1016/j.blre.2021.100825

Fig. 2.

Fig. 2.

BCR-ABL1 kinase domain mutations confer resistance to first and second generation TKIs. The crystal structure of the ABL1 kinase domain in complex with the indicated TKI (indicated in green) is shown. The P-loop is shown in yellow and the activation loop in green. Mutations at the highlighted residues confer resistance to the indicated TKI in vitro, with orange (moderate) and red (high) spheres indicating the level of resistance. Compared with imatinib, the newer inhibitors have less vulnerability to kinase domain mutations. Imatinib has a broad range of resistance mutations and a switch to a 2G TKI is indicated at in imatinib resistant disease. From O’Hare et al. Nat Rev Cancer. 2012;12(8):513–26.