Ras protein is a key signal transducer in the pathway from the out membrane to the nucleus in cell. ras oncogene is particularly attractive as a target for the development of new anti-tumor drug since mutated ras genes was found about 30% in human cancers. Ras proteins are produced as precursor proteins and require their association with the plasma membrane to acquire biological activity. This is achieved by posttranslational modifications including the farnesylation onto cysteine at the C-terminal end of Ras by farnesyl protein transferase (FPTase). Recent work has demonstrated that specific inhibitors of the FPTase might be interesting chemical leads to develop effective therapeutic agents for the treatment of cancer.

Many research teams try to identify a potent and selective inhibitor of FPTase from herbal medicine extracts. A couple of FPTase inhibitors, isolated from herbal medicines, inhibited the membrane association of Ras protein. It is suggested that the inhibition of FPTase activity was closely related with the inhibition of Ras membrane association and the alteration of Ras localization. However, many flavonoids did not alter the intracellular localization of Ras, even though they inhibited the FPTase in in vitro assay. In this review article, we summarize the FPTase structure and biological activities.