A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli
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.
Coval, SJ; Patton, RW; Petrin, JM; James, L; Rothofsky, ML; Lin, SL; Patel, M; Reed, JK; McPhail, AT; Bishop, WR
Volume / Issue
Start / End Page
International Standard Serial Number (ISSN)
Digital Object Identifier (DOI)