Preliminary evaluation of novel 18F-AlF-NOTA-IF7 as a tumor imaging agent
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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.
KeywordsAnnexin 1 NOTA 18F-AlF-NOTA-IF7 MicroPET imaging
This project was supported by the Science Foundation of Health Department of Jiangsu Province (H201226), the Fund of Wuxi Science and Technology Development (CSE31N1409), the Foundation of Wuxi Hospital Management Center (YGZXM14014), National Natural Science Foundation of China (81471736), the Vocational Education Science Foundation of Health Department of Jiangsu Province (JZ201413) and the Health Technology Planning Project of Jiangsu Province (Grant No. Q201204).
- 2.Hatakeyama S, Sugihara K, Nakayama J, Akama TO, Wong SM, Kawashima H, Zhang J, Smith DF, Ohyama C, Fukuda M, Fukuda MN (2009) Identification of MRNA splicing factors as the endothelial receptor for carbohydrate-dependent lung colonization of cancer cells. Proc Natl Acad Sci USA 106:3095–3100CrossRefGoogle Scholar
- 12.Guhlke S, Wester HJ, Bruns C, Stocklin G (1994) (2-[18F]fluoropropionyl-(D)phel)-octreotide, a potential radiopharmaceutical for quantitative somatostatin receptor imaging with PET: synthesis, radiolabeling, in vitro validation and biodistribution in mice. Nucl Med Biol 21:819–825CrossRefGoogle Scholar