Figure 6 | Leukemia

Figure 6

From: ABL fusion oncogene transformation and inhibitor sensitivity are mediated by the cellular regulator RIN1

Figure 6

Model of RIN1 effect on BCR-ABL1 activity and imatinib sensitivity. BCR-ABL1 equilibrates between active and inactive conformations, favoring the active form (open to substrate (S)) relative to ABL1. Right: RIN1 binds to ABL1 SH3 and SH2 domains, alleviating residual autoinhibition and stabilizing a high activity conformation. RIN1 is also a RAS effector.28, 56 Left: Imatinib (IM) preferentially binds and stabilizes the inactive conformation of the ABL1 catalytic site.35 RIN1 overexpression shifts equilibrium to right; RIN1 silencing shifts equilibrium to left.

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