Prenylation is an essential post-translational modification that increases protein hydrophobicity and targets them to membranes. The 3-step process consists of initial addition of a C1 5 or C20 isoprenoid to proteins followed by the proteolytic removal of the -a1a2ipeptide by ras converting enzyme 1 (RCE1), and methylation of the C-terminal prenylcysteine by the enzyme isoprenylcysteine carboxyl methyltransferase (Icmt). Many proteins involved in signal transduction pathways are farnesyl or geranylgeranylated, including the Ras family of oncoproteins. Because mutations in the ras oncogene are responsible for ~15-20% of human cancers, inhibitors of enzymes in the prenylation pathway hold potential as anticancer agents [1,2].
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