Table 1

Inhibition IC50s for FTIs and GGTIs

Peptidomimetics (Free acids/methylesters)In vitro activity (free acids)SelectivityaWhole-cell processing (methylesters)Selectivitya
FTase (nm)GGTase I (nm)Ras (μm)Rap1 (μm)
FTI-276/FTI-2770.5501000.3>30>100
FTI-2148/FTI-21531.4170012000.01>30>3000
GGTI-297/GGTI-298203554>155>3
GGTI-2154/GGTI-2166560021266>300.3>100
  • a Fold.