[Basic studies on the 111In labeled antisense oligonucleotide for tumor imaging].
Antisense oligonucleotide labeled with short lived radionuclide has been proposed as a radiopharmaceutical for the detection of abnormal gene expression. In this study, plausibility of 32P or 111In labeled oligonucleotide was basically evaluated using c-erbB-2 protooncogene mRNA as a model target. In cell uptake studies, sequence specific accumulation of 32P-oligonucleotide was found in the cells with c-erbB-2 mRNA expression, but not control cells, indicating the basic possibility of antisense strategy. Synthesis of 111In labeled isothiocyanobenzyl-EDTA (IBE)-oligonucleotide could be performed, but some problems were found in purification step. Stability of 111In-IBE-oligonucleotide was high when compared with that of 32P-oligonucleotide, and in vivo biodistribution data might indicate that 111In-IBE-oligonucleotide was plausible for tumor imaging.
Fujibayashi
Y
Y
Department of Radiopharmaceutical Chemistry, Biomedicaimaging Research Center, Fukui Medical School, Japan.
Nakagawa
K
K
Waki
A
A
Sakahara
H
H
Konishi
J
J
Yokoyama
A
A
D000818:Animals; D004355:Drug Stability; D015972:Gene Expression Regulation, Neoplastic; D018734:Genes, erbB-2; D007205:Indium Radioisotopes / Q000493:pharmacokinetics; D007553:Isotope Labeling; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000175:diagnosis* / Q000235:genetics / Q000378:metabolism; D016376:Oligonucleotides, Antisense / Q000493:pharmacokinetics; D014018:Tissue Distribution
D007205:Indium Radioisotopes; D016376:Oligonucleotides, Antisense