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- W2128656449 abstract "1401 Objectives NGR peptides could specifically target to aminopeptidase N (APN) which was highly expressed in tumor and angiogenic endothelial cells. Fcy, a yeast cytosine deaminase, can convert 5-fluorocytosine (5-FC) prodrug into cytotoxic 5-fluorouracil (5-FU). This study developed a targeted enzyme-mediated prodrug activation therapy, NGR-Fcy/5-FC, and characterized in sarcoma animal models. Methods NGR-Fcy and Fcy recombinant protein were both constructed and purified from E.coli with high yield (15 mg/L). The enzyme activity, in vitro binding affinity and cytotoxicity were assayed. Both NGR-Fcy and Fcy were labeled with I-131 to give their radioactive surrogates with high radiochemical purities. The biodistribution study of HT1080 tumor bearing mice after intravenous injection of 131I-NGR-Fcy and 131I-Fcy was conducted. Results The 5-FC/5-FU-converting activity of NGR-Fcy (Km=0.56±0.09 mM and Vmax=101.1±5.2 μM/m/μg) was similar to that of Fcy (Km=0.64±0.12 mM and Vmax= 107.8±7.2 μM/m/μg). NGR-Fcy could specifically bind to high APN-expressing tumor cells (HT1080) and endothelial cells (BAEC), but not to APN-negative cells (HT29). After NGR-Fcy/5-FC treatment, the viability of HT1080 and BAEC was significantly reduced (IC50= 14.8±0.4 and 33.4±0.4 μM, respectively), while that of HT29 was not (IC50= 39430.4±347.2 μM). The tumor uptake of 131I-NGR-Fcy was higher than that of 131I-Fcy in HT1080 tumor bearing mice. Conclusions This study developed a prodrug activation therapy system, NGR-Fcy/5-FC, which can specifically bound to high APN-expressing tumor and endothelial cells and exhibit remarkable cytotoxicity by converting 5-FC to 5-FU. Research Support This work was supported by Grants from the National Science Council of Taiwan (NSC 102-2627-M-010-002 and NSC 102-2627-M-010-001)." @default.
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- W2128656449 date "2014-07-24" @default.
- W2128656449 modified "2023-09-26" @default.
- W2128656449 title "Is Radiocholine PET/CT Already Clinically Useful in Patients with Prostate Cancer?" @default.
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- W2128656449 doi "https://doi.org/10.2967/jnumed.114.142679" @default.
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