PET Imaging of a Novel Anxal-targeted Peptide 18 F-Al-NODA-Bn-p-SCN-GGGRDN-IF7 in A431 Cancer Mouse Models,Journal of Labelled Compounds and Radiopharmaceuticals

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PET Imaging of a Novel Anxal-targeted Peptide 18 F-Al-NODA-Bn-p-SCN-GGGRDN-IF7 in A431 Cancer Mouse Models
Journal of Labelled Compounds and Radiopharmaceuticals ( IF 0.9 ) Pub Date : 2020-07-20 , DOI: 10.1002/jlcr.3865
Fei Chen ₁ , Yichun Xiao ₁ , Kejing Shao ₁ , Bao Zhu ₁ , Mengjun Jiang ₂

Affiliation

Annexin 1 (Anxa1) is a highly specific surface marker of tumor vasculature in the lung and prostate solid tumors. The IF7 peptide was modified with a hydrophilic linker, GGGRDN, and coupled with a new bifunctional chelating agent NODA-Bn-p-SCN. The resulting peptides (NODA-Bn-p-SCN-GGGRDN-IF7) were successfully labeled with Al18 F. The targeting characteristics of the radiolabeled peptides were evaluated in the Anxa1 positive A431 tumor model. Micro-PET imaging revealed that the A431 tumors were clearly visualized (5.74 ± 1.13 % ID/g, 3.92 ± 0.78 % ID/g and 1.30 ± 0.43 % ID/g at 0.5h, 1h and 2h post-injection, respectively). Anxa1 binding specificity was also demonstrated by reduced tumor uptake after co-injection with excessive unlabeled GGGRDN-IF7 peptide at 30 min, 60 min, and 120 min post-injection. 18 F-Al-NODA-Bn-p-SCN-GGGRDN-IF7 might be a potential PET imaging agent for detecting Anxa1 levels in cancers due to the favorable characteristics such as convenient synthesis, specific Anxa1 targeting, and good tumor uptakes.

中文翻译：

A431 癌症小鼠模型中新型 Anxal 靶向肽 18 F-Al-NODA-Bn-p-SCN-GGGRDN-IF7 的 PET 成像

膜联蛋白 1 (Anxa1) 是肺和前列腺实体瘤中肿瘤血管系统的高度特异性表面标志物。 IF7 肽用亲水接头 GGGRDN 进行修饰，并与新型双功能螯合剂 NODA-Bn-p-SCN 偶联。所得肽 (NODA-Bn-p-SCN-GGGRDN-IF7) 成功用 Al18 F 标记。在 Anxa1 阳性 A431 肿瘤模型中评估了放射性标记肽的靶向特性。微型 PET 成像显示 A431 肿瘤清晰可见（注射后 0.5 小时、1 小时和 2 小时分别为 5.74 ± 1.13 % ID/g、3.92 ± 0.78 % ID/g 和 1.30 ± 0.43 % ID/g）。 Anxa1 结合特异性还通过在注射后 30 分钟、60 分钟和 120 分钟共注射过量未标记的 GGGRDN-IF7 肽后肿瘤摄取减少来证明。 18 F-Al-NODA-Bn-p-SCN-GGGRDN-IF7 因其合成方便、Anxa1 特异性靶向和良好的肿瘤摄取等有利特性，可能成为检测癌症中 Anxa1 水平的潜在 PET 成像剂。

更新日期：2020-07-20

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