Inhibitors of protein farnesylation 1998

Abstract

Protein farnesyltransferase (PFTase) inhibitors are being studied as mechanistically novel antitumour agents. Whilst the antiproliferative effects of PFTase inhibitors are well-documented in cell culture and rodent animal models, clinical studies which began in 1997 should soon reveal their utility in human cancer patients. This review summarises the scientific and patent literature covering PFTase inhibition that has been published since the previous two updates [1,2]. New biology with a potential impact on the utility of PFTase inhibitors is reviewed first, followed by a discussion of new PFTase inhibitors. As in earlier updates, compounds are grouped according to their kinetic mechanism of PFTase inhibition.

• PFTase
• protein farnesyltransferase
• protein farnesyltransferase inhibitors
• protein prenylation
• ras oncogene