125I–F56 Peptide as Radioanalysis Agent Targeting VEGFR1 in Mice Xenografted with Human Gastric Tumor

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• 作者：Hua Zhu ; Chuanke Zhao ; Fei Liu ; Lixin Wang ; Junnan Feng ; Chengchao Shou ; Zhi Yang
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：February 9, 2017
• 年：2017
• 卷：8
• 期：2
• 页码：266-269
• 全文大小：320K
• ISSN：1948-5875

文摘

¹²⁵I-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 in vitro stability of ¹²⁵I–F56 was tested, and the bioactivity of ¹²⁵I–F56 was confirmed by both cell uptake and binding affinity measurement in VEGFR1 positive BGC-823 cells. The time–radioactivity relationship and biodistribution of ¹²⁵I–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 ¹²⁵I–F56 in tumor tissues ex vivo. Those results demonstrated that ¹²⁵I–F56 holds great potential as a diagnostic agent in both molecular imaging and radioanalysis probe for gastric cancer.