Influence of farnesyl transferase inhibitor treatment on epidermal growth factor receptor status

Nucl Med Biol. 2004 Aug;31(6):679-89. doi: 10.1016/j.nucmedbio.2004.03.004.

Abstract

The radiolabelled growth factor [(123/125)I] I-hEGF is evaluated in vitro and in vivo to monitor the acute effects on the EGFR of R115777, a farnesyl transferase inhibitor (FTI). Upregulation of the EGFR after incubation with R115777 correlated linearly with FTI induced acute growth inhibition. Receptor mediated [125I] I-hEGF internalization decreased following R115777 treatment. Preliminary data suggest that the net in vivo effect is a decrease of [123I] I-hEGF uptake in the tumour. These findings suggest the possible use of radioiodinated hEGF as a radiodiagnosticum to investigate EGFR status changes as a predictor for eventual FTI chemotherapy outcome in vivo.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Animals
  • Cell Line
  • Enzyme Inhibitors / pharmacology*
  • Epidermal Growth Factor / chemistry
  • Epidermal Growth Factor / metabolism
  • ErbB Receptors / drug effects*
  • Farnesyltranstransferase
  • Humans
  • Iodine Radioisotopes / chemistry
  • Magnetic Resonance Imaging
  • Male
  • Mice
  • Mice, Nude
  • Neoplasm Transplantation
  • Quinolones / pharmacology
  • Radiopharmaceuticals / chemical synthesis
  • Regression Analysis
  • Tissue Distribution

Substances

  • Enzyme Inhibitors
  • Iodine Radioisotopes
  • Quinolones
  • Radiopharmaceuticals
  • Epidermal Growth Factor
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase
  • ErbB Receptors
  • tipifarnib