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