Protein Prenyltransferase Inhibitors: Small Molecules and Peptides

Protein prenyltransferases are enzymes that transfer isoprenoid lipids (such as farnesyl or geranylgeranyl groups) to acceptor molecules. The attachment of these groups is known as prenylation. Farnesyltransferase (FTase) and geranylgeranyltransferase type 1 (GGTase 1) catalyze this modification, which takes place at a conserved cysteine residue in a CaaX motif in the protein substrate (in which 'C' is cysteine, 'a' is an aliphatic amino acid, and 'X' is variable). The ...