Protein Farnesyltransferase (FTase)

Protein farnesyltransferase (FTase) is a key enzyme responsible for the posttranslational modification known as farnesylation. This process involves the covalent attachment of a 15-carbon isoprenoid lipid, called a farnesyl group, to specific proteins that contain a C-terminal CaaX motif (where "C" is cysteine, "a" represents aliphatic amino acids, and "X" can be several different amino acids). The modification occurs at the cysteine residue near the protein's C-terminus and results in increased membrane association and altered protein-protein interactions. Because many oncogenic mutations require proper membrane localization via farnesylation (notably mutant Ras), FTase has become an important target for anti-cancer drug development.

Inhibition of farnesylation of target proteins