Farnesyltransferase inhibitor effects on prostate tumor micro-environment and radiation survival

Prostate. 2005 Jan 1;62(1):69-82. doi: 10.1002/pros.20122.

Abstract

Background: Ras activation by mutation, overexpression, or receptor signaling can increase tumor cell survival after irradiation.

Methods: We examined whether inhibiting Ras activity with farnesyltransferase inhibitors (FTI) altered the radiosensitivity and tumor micro-environment in prostate tumors.

Results: Treatment with FTIs L-744,832 or FTI-277 reduced clonogenic survival of prostate tumor cells expressing oncogenic H-ras after irradiation. PI3-kinase/Akt and MAPK signaling pathways were downregulated by FTIs in these cells. FTI treatment reduced tumor hypoxia and also reduced MMP-9 expression in tumors with activated mutant H-ras. FTI treatment did not, however, increase apoptosis in irradiated intestine, demonstrating that acute radiation injury of this normal tissue was not enhanced by FTIs.

Conclusions: FTIs can enhance the killing of prostate tumors with activated H-Ras. Together with the absence of increased acute toxicity to normal bowel, these results imply that FTI treatment should be further studied as a possible adjuvant to radiotherapy in the treatment of abdominal cancers with activated Ras signaling.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Animals
  • Apoptosis / drug effects
  • Apoptosis / radiation effects
  • Cell Line, Tumor
  • Enzyme Inhibitors / pharmacology*
  • Farnesyltranstransferase
  • Genes, ras / drug effects*
  • Humans
  • Male
  • Matrix Metalloproteinase 9 / metabolism
  • Methionine / analogs & derivatives*
  • Methionine / pharmacology*
  • Mice
  • Mice, Nude
  • Mitogen-Activated Protein Kinases / metabolism
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / metabolism
  • Prostatic Neoplasms / radiotherapy*
  • Protein Serine-Threonine Kinases / metabolism
  • Proto-Oncogene Proteins / metabolism
  • Proto-Oncogene Proteins c-akt
  • Radiation Tolerance / drug effects
  • Radiation-Sensitizing Agents / pharmacology*
  • Signal Transduction
  • Xenograft Model Antitumor Assays

Substances

  • Enzyme Inhibitors
  • FTI 277
  • L 744832
  • Proto-Oncogene Proteins
  • Radiation-Sensitizing Agents
  • Methionine
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase
  • AKT1 protein, human
  • Protein Serine-Threonine Kinases
  • Proto-Oncogene Proteins c-akt
  • Mitogen-Activated Protein Kinases
  • Matrix Metalloproteinase 9