Peptidomimetic inhibitors of p21ras farnesyltransferase: Hydrophobic functionalization leads to disruption of p21ras membrane association in whole cells

Abstract In this paper we describe the synthesis of several hydrophobic inhibitors of p21ras farnesyltransferase. These peptidomimetic structures, containing cysteine and methionine residues separated by an aromatic spacer, are functionalized as their methyl esters and N,S-bis-benzyloxycarbonyl (Cbz) derivatives and are shown to penetrate NIH 3T3 cells to disrupt p21 ras plasma membrane association.