I-F56肽作为针对人胃癌异种移植小鼠中血管内皮生长因子受体1（VEGFR1）的放射性分析剂。
I-F56 Peptide as Radioanalysis Agent Targeting VEGFR1 in Mice Xenografted with Human Gastric Tumor.
作者信息
Zhu Hua, Zhao Chuanke, Liu Fei, Wang Lixin, Feng Junnan, Shou Chengchao, Yang Zhi
机构信息
Department of Nuclear Medicine and Department of Biochemistry and Molecular Biology, Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Peking University Cancer Hospital & Institute , Beijing 100142, China.
出版信息
ACS Med Chem Lett. 2017 Jan 20;8(2):266-269. doi: 10.1021/acsmedchemlett.6b00498. eCollection 2017 Feb 9.
I-Radiolabeled F56 peptide was designed as a radioactive analogue of F56 (peptide WHSDMEWWYLLG) to bind with VEGFR1 receptor. It was synthesized in high radiochemical yield and specific activity. The stability of I-F56 was tested, and the bioactivity of I-F56 was confirmed by both cell uptake and binding affinity measurement in VEGFR1 positive BGC-823 cells. The time-radioactivity relationship and biodistribution of I-F56 tracer were conducted using nude mice bearing human gastric carcinoma BGC-823, by noninvasive micro-SPECT/CT imaging. The tracer's tumor uptake was further confirmed by autoradiography and HE stain of I-F56 in tumor tissues ex vivo. Those results demonstrated that I-F56 holds great potential as a diagnostic agent in both molecular imaging and radioanalysis probe for gastric cancer.
碘标记的F56肽被设计为F56（肽WHSDMEWWYLLG）的放射性类似物，用于与血管内皮生长因子受体1（VEGFR1）结合。它以高放射化学产率和比活度合成。测试了碘-F56的稳定性，并通过VEGFR1阳性的BGC-823细胞中的细胞摄取和结合亲和力测量证实了碘-F56的生物活性。使用荷人胃癌BGC-823的裸鼠，通过无创微型单光子发射计算机断层扫描/计算机断层扫描（micro-SPECT/CT）成像研究了碘-F56示踪剂的时间-放射性关系和生物分布。通过离体肿瘤组织中碘-F56的放射自显影和苏木精-伊红（HE）染色进一步证实了示踪剂的肿瘤摄取。这些结果表明，碘-F56作为胃癌分子成像和放射分析探针的诊断剂具有巨大潜力。
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