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Free keywords:
PROTEIN TRANSFERASE; CANCER CHEMOTHERAPEUTICS; RAS; FARNESYL; TRANSFORMATION; GENES; ACIDS
Chemistry; bioorganic chemistry; enzyme inhibitors; pepticinnamin E; signal transduction;
Abstract:
The farnesyltransferase inhibitor pepticinnamin E was synthesized and shown to have the S configuration at the central, non-proteinogenic amino acid. Using a recombinant yeast farnesyltransferase the biological activity of the natural product and structural analogues was determined. It was shown that pepticinnamin E is a bisubstrate inhibitor. Furthermore, several structural parameters were identified that decisively influence inhibition of the farnesyl transfer.
