Farnesyltransferase inhibitors as anticancer agents: Current status

Kuichun Zhu, Andrew D. Hamilton, Saïd M. Sebti

Research output: Contribution to journalReview articlepeer-review


Farnesyltransferase (FTase) is a major molecular target for the development of novel anticancer drugs that are designed to disrupt the aberrant signal transduction circuitry of tumor cells. The discovery more than a decade ago that farnesylation of Ras, one of the most prevalent oncoproteins in human cancers, is required for its cancer-causing activity was the initial stimulus to target FTase. However, it is now clear that yet to be identified farnesylated proteins other than Ras also play a pivotal role as targets for FTase inhibitors (FTIs). In this review, important mechanistic issues on the antiproliferative, pro-apoptotic and anti-angiogenic activities of FTIs, with an emphasis on potential FTI targets, will be discussed. Important clinical issues associated with translational aspects of hypotheses-driven clinical trials will also be discussed.

Original languageEnglish (US)
Pages (from-to)1428-1435
Number of pages8
JournalCurrent Opinion in Investigational Drugs
Issue number12
StatePublished - Dec 2003


  • Farnesyltransferase
  • Farnesyltransferase inhibitor
  • Prenylation
  • Ras
  • RhoB

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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