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Farnesyltransferase inhibitors: antineoplastic mechanism and clinical prospects

G C Prendergast1

  • 1Glenolden Laboratory, DuPont Pharmaceuticals Company, Wistar Institute, Glenolden, Philadelphia, PA 19036, USA. george. c.prendergast@dupontpharma.com

Current Opinion in Cell Biology
|March 14, 2000
PubMed

Insights

Farnesyltransferase inhibitors fight cancer by altering RhoB isoprenylation, not Ras. This finding offers new strategies for cancer treatment and wider clinical applications.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • Farnesyltransferase inhibitors (FTIs) are investigated for cancer treatment.
  • Previous research focused on FTIs inhibiting Ras isoprenylation, but this mechanism is now questioned.
  • Emerging evidence points to RhoB isoprenylation as a key target for FTIs.

Purpose of the Study:

  • To re-evaluate the mechanism of action for farnesyltransferase inhibitors in cancer.
  • To explore the role of RhoB isoprenylation in the antineoplastic effects of FTIs.
  • To propose new therapeutic strategies based on targeting RhoB.

Main Methods:

  • Analysis of recent scientific literature and evidence.
  • Conceptual shift from Ras-centric to Rho-centric mechanisms.
  • Review of farnesyltransferase inhibitor (FTI) action.

Main Results:

  • Farnesyltransferase inhibitors suppress cancer cell proliferation via mechanisms independent of Ras inhibition.
  • Alterations in the isoprenylation of RhoB, an endosomal Rho protein, are responsible for the antineoplastic properties of FTIs.
  • RhoB plays a role in receptor trafficking, and its altered isoprenylation impacts cancer cell behavior.

Conclusions:

  • The primary mechanism of farnesyltransferase inhibitors in cancer involves RhoB, not Ras.
  • Understanding the role of RhoB offers new perspectives on FTI action.
  • This knowledge can guide the development of improved and broader clinical applications for FTIs in cancer therapy.

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