New approaches to anticancer drug design based on the inhibition of farnesyltransferase

Saïd M. Sebti, Andrew D. Hamilton

Research output: Contribution to journalReview article

Abstract

Mutated forms of the GTP-binding protein Ras are found in 30% of human cancers, with particularly high prevalence in colon and pancreatic carcinomas. Ras function in growth factor signaling requires post- translational farnesylation of a cysteine residue present as part of the CA1A2X carboxyl terminal tetrapeptide. The enzyme farnesyltransferase has become an important target for the design of potential new antitumor agents. The authors outline the major new approaches to inhibition of farnesyltransferase and describe how certain peptidomimetics have been shown to block oncogenic signaling and tumor growth in various animal models.

Original languageEnglish (US)
Pages (from-to)26-33
Number of pages8
JournalDrug Discovery Today
Volume3
Issue number1
DOIs
StatePublished - Jan 1998

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ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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