Inhibitors of protein farnesylation

In this article, we update the progress reported towards developing an inhibitor of protein farnesyltransferase (PFTase) as a new type of cancer therapy. For the rationale behind this undertaking, please refer to the review published in this journal in December 1995 [1], and other reviews [2,3]. A few experiments bearing on the utility of PFTase inhibitors as antitumour agents are considered first, including biological results obtained with compounds described in our earlier review. Finally, new compounds described in the scientific and patent literature in the past year are reported. As in the previous review, these are grouped according to their kinetic mechanism of inhibition of PFTase.