Preliminary evaluation of novel super(18)F-AlF-NOTA-IF7 as a tumor imaging agent

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- triac...

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Veröffentlicht in:Journal of radioanalytical and nuclear chemistry 2016-06, Vol.308 (3), p.851-856
Hauptverfasser: Gu, Xiaobo, Jiang, Mengjun, Pan, Donghui, Cai, Gangming, Zhang, Rongjun, Zhou, Yaoyuan, Ding, Yaming, Zhu, Bao, Lin, Xiufeng
Format: Artikel
Sprache:eng
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Zusammenfassung: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 Al super(18)F intermediate to synthesize super(18)F-AlF-NOTA-IF7. MicroPET studies demonstrated that super(18)F-AlF-NOTA-IF7 had good uptake in tumor. super(18)F-AlF-NOTA-IF7 is a promising radiopharmaceutical in tumor imaging. The favorable characterizations of super(18)F-AlF-NOTA-IF7 such as convenient synthesis, specific Anxa1 targeting and moderate tumor uptake make it possible for imaging of cancers.
ISSN:0236-5731
1588-2780
DOI:10.1007/s10967-015-4533-3