Positron-emission tomography (PET) can be used to visualize active stage cancer. Fluorine-18 ([18F])-labeled 2-([18F])2-deoxy-2- fluoroglucose (([18F])-FDG), which accumulates in glucose-dependent tissues, is a good cancer-targeting tracer. However, ([18F])-FDG is obscured in glucose-dependent normal tissues. In this study, we assessed the cancer-selective accumulation of zinc-labeled glycoconjugated 5,10,15,20-tetrakis(pentafluorophenyl)porphyrin (ZnGlc1-4), both in vitro and in vivo. Experiments using both normal and cancer cells confirmed the relationship between cancer cell-selective accumulation and the substitution numbers and orientations of glycoconjugated porphyrins. ZnGlctrans-2 accumulated at greater levels in cancer cells compared with other glycoconjugated porphyrins. PET imaging showed that ZnGlctrans-2 accumulated in tumor.
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