Is there a future for prenyltransferase inhibitors in cancer therapy?

Sarah A. Holstein, Raymond J. Hohl

Research output: Contribution to journalReview articlepeer-review

26 Scopus citations


It has been over 20 years since it was first recognized that the function of both normal and oncogenic Ras is dependent on the post-translational modification termed farnesylation. Since that time, intense effort has been expended on the development of farnesyltransferase inhibitors as novel anticancer agents. Over 70 clinical trials have now been conducted, with limited efficacy demonstrated. Here we provide an update of the most recently published clinical trials, discuss the use of the RASGRP1/APTX two-gene expression screen to select patients with acute myeloid leukemia for therapy, and report on the latest discoveries related to the targets of prenyltransferase inhibitors.

Original languageEnglish (US)
Pages (from-to)704-709
Number of pages6
JournalCurrent Opinion in Pharmacology
Issue number6
StatePublished - Dec 2012

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery


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