Patent ID: 6083917
Filing Date: 2000-07-04
Classification: A61K,A61P,C07K,C12N

Abstract:
A farnesyltransferase inhibitor comprising a compound having a farnesyltransferase inhibitor peptide sequence within its structure, said sequence inhibiting the farnesylation of p21.sup.ras by protein farnesyltransferase without itself serving as a substrate for farnesylation by said enzyme, said farnesyltransferase inhibitor peptide sequence being defined as having the amino acids CA.sub.1 CA.sub.2 X, wherein:C=cysteine;A1=any aliphatic, aromatic or hydroxy amino acid;A2=any aromatic amino acid or amino acid incorporating one or more aromatic moieties; andX=met, ser, glu or cys;wherein said compound has an uncharged alpha nitrogen on the cysteine residue of CA.sub.1 A.sub.2 X prior to the compound being introduced intracellularly into a target cell, further wherein when said compound is introduced intracellularly into a target cell, the inhibitor is provided in a form wherein the cysteine residue of CA.sub.1 A.sub.2 X is a positively charged amino terminus of the inhibitor.