A CEMBRANOLIDE DITERPENE FARNESYL-PROTEIN TRANSFERASE INHIBITOR FROM THE MARINE SOFT CORAL LOBOPHYTUM-CRISTAGALLI

A previously described cembranolide diterpene from Lobophytum cristaga lli was identified as a potent (IC50 0.15 mu M) inhibitor of famesyl p rotein transferase (FPT). The compound showed selectivity for FPT as c ompared to the closely related enzyme geranylgeranyl protein transfera se-1 (IC50 5.3 mu M). Kinetic evaluation suggests that this compound c ompetes with the protein/peptide farnesyl acceptor substrate, and not with farnesyl pyrophosphate for inhibition of FPT. Copyright (C) 1996 Elsevier Science Ltd