Farnesyltransferase inhibitors versus Ras inhibitors.
Over the past few years, the idea that farnesyl-protein transferase (FPTase) inhibitors might be effective antiproliferative/antitumor agents has been realized in studies of cultured cells and in rodent models of cancer. Most of the studies with FPTase inhibitors have focused on inhibiting the growth of ras-transformed cells in vitro or the growth of ras-dependent tumors in mice. More recently, it has been recognized that the antiproliferative effect of FPTase inhibitors may extend beyond ras-driven tumors. It now seems likely that the ability of FPTase inhibitors to reverse the malignant phenotype results, at least in part, from inhibiting the farnesylation of proteins other than Ras.
Gibbs
J B
JB
Merck Research Laboratories, West Point, PA 19486, USA. jay_gibbs@merck.com
Graham
S L
SL
Hartman
G D
GD
Koblan
K S
KS
Kohl
N E
NE
Omer
C A
CA
Oliff
A
A
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000970:Antineoplastic Agents / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry*; D051231:Farnesyltranstransferase; D011905:Genes, ras / Q000187:drug effects*; D006801:Humans
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase