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

Journal article

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.

Authors: Cornelissen, B; Thonissen, T; Kersemans, V; Van De Wiele, C; Lahorte, C

• Publication status: Published
• Journal: Nuclear medicine and biology
• Volume: 31
• Issue: 6
• Pages: 679-689
• Publication date: 2004-08-01
• DOI: 10.1016/j.nucmedbio.2004.03.004
• EISSN: 1872-9614
• ISSN: 0969-8051
• Language: English
• Keywords: Tissue Distribution; Cell Line; Alkyl and Aryl Transferases; Radiopharmaceuticals; Mice; Epidermal Growth Factor; Enzyme Inhibitors; Male; Neoplasm Transplantation; Mice, Nude; Iodine Radioisotopes; Magnetic Resonance Imaging; Regression Analysis; Quinolones; Humans; Receptor, Epidermal Growth Factor; Animals; Farnesyltranstransferase