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. 2021 Jul 8;7(9):1–8. doi: 10.1001/jamaoncol.2021.2086

Figure 1. Type I Inhibitor PLX9486 Binds to Mutant KITD816V With High Atomic Efficiency.

Figure 1.

The aspartate to valine substitution in KITD816V promotes hydrophobic packing between V816 and Y646, locking the activation look (A-loop) in an extended, aspartate-phenylalanine-glycine–-in conformation conducive to adenosine triphosphate and substrate binding.