Preliminary evaluation of novel 18F-AlF-NOTA-IF7 as a tumor imaging agent
Preliminary evaluation of novel 18F-AlF-NOTA-IF7 as a tumor imaging agent
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DOI：
10.1007/s10967-015-4533-3
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发表时间：
2016-06-01
影响因子：
1.6
通讯作者：
Lin, Xiufeng
中科院分区：
文献类型：
--
作者：
Gu, Xiaobo;Jiang, Mengjun;Lin, Xiufeng
膜联蛋白1（Annexin 1，Anxa 1）是一种高度特异性的肿瘤血管表面标志物。IFLLWQR（Ile-Phe-Leu-Leu-Trp-Gln-Arg，IF 7）是一种糖配体模拟7肽，可靶向肿瘤血管系统中的Anxa 1。首先将IF 7与大环螯合剂1，4，7-三氮杂环壬烷-1，4，7-三乙酸（NOTA）缀合，然后将所得生物缀合物NOTA-IF 7经由（AlF）-F-18中间体放射性氟化以合成F-18-AlF-NOTA-IF 7。MicroPET研究表明，F-18-AlF-NOTA-IF 7在肿瘤中具有良好的摄取。F-18-AlF-NOTA-IF 7是一种很有前途的肿瘤显像剂。F-18-AlF-NOTA-IF 7具有合成方便、特异性靶向Anxa 1和肿瘤摄取适中等优点，使其成为肿瘤显像的可能。
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 (AlF)-F-18 intermediate to synthesize F-18-AlF-NOTA-IF7. MicroPET studies demonstrated that F-18-AlF-NOTA-IF7 had good uptake in tumor. F-18-AlF-NOTA-IF7 is a promising radiopharmaceutical in tumor imaging. The favorable characterizations of F-18-AlF-NOTA-IF7 such as convenient synthesis, specific Anxa1 targeting and moderate tumor uptake make it possible for imaging of cancers.