Structural Basis for Resistance to Diverse Classes of NAMPT Inhibitors
Figure 4
Nampt inhibitors evaluated for potency on mutant NAMPT enzymes.
a) Chemical structures of NAMPT inhibitors, compound 1 is GNE-618, compound 9 is GMX1778, compound 11 is APO866. b) Fold change in IC50 of NAMPT inhibitors on purified mutant NAMPT proteins compared to wild-type enzyme. c) Fold change in IC50 values for S165Y/F mutants compared to wild-type. * fold-change assuming IC50 = maximum concentration tested (5 µM). Actual fold-change is likely larger than that depicted.