Structural Basis for Resistance to Diverse Classes of NAMPT Inhibitors
Figure 2
Characterization of GNE-618 resistant cell lines.
a) Example IC50 of RD parent versus the resistant derivative line harboring the S165F NAMPT mutation in the absence (solid lines) or presence (dashed line) of 10 µM NA. b) Fold shifts in absolute IC50 values in resistant versus parental cell lines. Error bars represent the standard deviation of three independent runs. c-e) NAMPT S165F and S165Y were expressed in 293T cells and evaluated for response to c) GNE-618, d) APO866 and e) GMX1778. WT = wild-type NAMPT, UT = untransfected.