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Farnesyltransferase (FTase)

Target: FTase
Molecular classification: Enzyme, Transferase

Overview

Farnesyltransferase (FTase) is an enzyme that catalyzes the post-translational modification of proteins by attaching a farnesyl lipid group to a cysteine residue near the C-terminus of target proteins. This process, known as farnesylation, is essential for the function and membrane localization of many signaling proteins, most notably members of the Ras superfamily. Inhibition of FTase is a potential therapeutic strategy for cancer.

Mechanism of action

Farnesyltransferase inhibitors bind to the active site of FTase, preventing the transfer of a farnesyl group from farnesyl pyrophosphate (FPP) to target proteins with a CaaX motif.

Biological functions

Protein farnesylationMembrane targetingSignal transductionCell growth regulation

Disease associations

Cancer

Safety considerations

Redundancy with other prenylation enzymes (e.g., GGT1)Potential for cross-prenylation

Interacting drugs

Farnesyltransferase inhibitors (FTIs)

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