Abstract

Annexin 1 (Anxa1) is a highly specific surface marker of tumor vasculature. A carbohydrate ligand-mimicking 7-mer peptide, IFLLWQR (Ile-Phe-Leu–Leu-Trp-Gln-Arg, IF7) can target Anxa1 in tumor vasculature. IF7 was first conjugated with a macrocyclic chelator, 1, 4, 7- triazacyclononane-1, 4, 7- triacetic acid (NOTA), and the resulting bioconjugate NOTA-IF7 was then radiofluorinated via Al18F intermediate to synthesize 18F-AlF-NOTA-IF7. MicroPET studies demonstrated that 18F-AlF-NOTA-IF7 had good uptake in tumor. 18F-AlF-NOTA-IF7 is a promising radiopharmaceutical in tumor imaging. The favorable characterizations of 18F-AlF-NOTA-IF7 such as convenient synthesis, specific Anxa1 targeting and moderate tumor uptake make it possible for imaging of cancers.

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