Author: ["Nancy E. Kohl","Charles A. Omer","Michael W. Conner","Neville J. Anthony","Joseph P. Davide","S. Jane Desolms","Elizabeth A. Giuliani","Robert P. Gomez","Samuel L. Graham","Kelly Hamilton","Laurence K. Handt","George D. Hartman","Kenneth S. Koblan","Astrid M. Kral","Patricia J. Miller","Scott D. Mosser","Timothy J. O'Neill","Elaine Rands","Michael D. Schaber","Jackson B. Gibbs","Allen Oliff"]
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Abstract
For Ras oncoproteins to transform mammalian cells, they must be post-translationally modified with a farnesyl group in a reaction catalysed by the enzyme farnesyl-protein transferase (FPTase). Inhibitors of FPTase have therefore been proposed as anti-cancer agents. We show that L-744,832, which mimics the CaaX motif to which the farnesyl group is added, is a potent and selective inhibitor of FPTase. In MMTV-v-Ha-ras mice bearing palpable tumours, daily administration of L-744,832 caused tumour regression. Following cessation of treatment, tumours reappeared, the majority of which regressed upon retreatment. No systemic toxicity was found upon necropsy of L-744,832-treated mice. This first demonstration of anti-FPTase-mediated tumour regression suggests that FPTase inhibitors may be safe and effective anti-tumour agents in some cancers.Cite this article
Kohl, N., Omer, C., Conner, M. et al. Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice. Nat Med 1, 792–797 (1995). https://doi.org/10.1038/nm0895-792 