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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.

Original publication

DOI

10.1016/j.nucmedbio.2004.03.004

Type

Journal article

Journal

Nucl Med Biol

Publication Date

08/2004

Volume

31

Pages

679 - 689

Keywords

Alkyl and Aryl Transferases, Animals, Cell Line, Enzyme Inhibitors, Epidermal Growth Factor, ErbB Receptors, Farnesyltranstransferase, Humans, Iodine Radioisotopes, Magnetic Resonance Imaging, Male, Mice, Mice, Nude, Neoplasm Transplantation, Quinolones, Radiopharmaceuticals, Regression Analysis, Tissue Distribution