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Is there a future for prenyltransferase inhibitors in cancer therapy?

Sarah A Holstein1, Raymond J Hohl

  • 1Department of Internal Medicine, University of Iowa, C32 GH, Iowa City, IA 52242, USA.

Current Opinion in Pharmacology
|July 24, 2012
PubMed

Insights

Farnesyltransferase inhibitors show limited efficacy in cancer trials. New research explores patient selection for acute myeloid leukemia and novel prenyltransferase inhibitor targets.

Area of Science:

  • Biochemistry
  • Oncology
  • Pharmacology

Background:

  • Ras protein function, crucial in normal and cancer cells, relies on farnesylation.
  • Farnesyltransferase inhibitors (FTIs) were developed as anticancer agents based on this dependency.
  • Despite extensive research and over 70 clinical trials, FTIs have shown limited therapeutic efficacy.

Purpose of the Study:

  • To review recent clinical trial data on farnesyltransferase inhibitors.
  • To discuss the application of the RASGRP1/APTX gene expression screen for patient selection in acute myeloid leukemia.
  • To present recent findings on the targets of prenyltransferase inhibitors.

Main Methods:

  • Review of recently published clinical trial results.
  • Analysis of the RASGRP1/APTX two-gene expression screen for patient stratification.
  • Summary of recent discoveries concerning prenyltransferase inhibitor targets.

Main Results:

  • Clinical trials of farnesyltransferase inhibitors have demonstrated limited efficacy.
  • The RASGRP1/APTX screen shows potential for selecting acute myeloid leukemia patients for therapy.
  • New insights into prenyltransferase inhibitor targets are emerging.

Conclusions:

  • Farnesyltransferase inhibitors have not met expectations for broad anticancer efficacy.
  • Biomarker-guided therapy, such as the RASGRP1/APTX screen, may improve outcomes in specific cancers like AML.
  • Ongoing research into prenyltransferase inhibitor targets could lead to more effective therapies.

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