Author/Authors :
Stephen J. Coval، نويسنده , , Robert W. Patton، نويسنده , , Joanne M. Petrin، نويسنده , , Linda James-Myers، نويسنده , , Marnie L. Rothofsky، نويسنده , , Stanley L. Lin، نويسنده , , Mahesh Patel، نويسنده , , John K. Reed، نويسنده , , Andrew T. McPhail، نويسنده , , W. Robert Bishop، نويسنده ,
Abstract :
A previously described cembranolide diterpene from Lobophytum cristagalli was identified as a potent (IC50 0.15 μM) inhibitor of farnesyl protein transferase (FPT). The compound showed selectivity for FPT as compared to the closely related enzyme geranylgeranyl protein transferase-1 (IC50 5.3 μM). Kinetic evaluation suggests that this compound competes with the protein/peptide farnesyl acceptor substrate, and not with farnesyl pyrophosphate for inhibition of FPT.
