Positron emission tomography imaging of a novel Anxa1-targeted peptide 18F-Al-NODA-Bn-p-SCN-GGGRDN-IF7 in A431 cancer mouse models
Positron emission tomography imaging of a novel Anxa1-targeted peptide 18F-Al-NODA-Bn-p-SCN-GGGRDN-IF7 in A431 cancer mouse models
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DOI：
10.1002/jlcr.3865
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发表时间：
2020-07-20
影响因子：
1.8
通讯作者：
Jiang, Mengjun
中科院分区：
文献类型：
--
作者：
Chen, Fei;Xiao, Yichun;Jiang, Mengjun
膜联蛋白1(Annexin 1，Anxa1)是肺和前列腺实体瘤中肿瘤血管形成的高度特异性表面标志物。用亲水性连接物GGGRDN修饰IF7多肽，并与新的双功能螯合剂Noda-Bn-p-SCN偶联。将得到的多肽(Noda-Bn-p-SCN-GGGRDN-IF7)成功地标记为(Alf)-F-18。在Anxa1阳性A431肿瘤模型中评价了放射性标记多肽的靶向性。微正电子发射断层扫描(Micro-PET)显示，注射后0.5、1、2 h分别为5.74±-1.13%ID/g、3.92+/-0.78%ID/g和1.30±0.43%ID/g。在30、60和120min联合注射过量的未标记GGRDNIF7多肽后，肿瘤摄取减少也证明了AnxA1结合的特异性。post-injection.F-18-Al-NODA-Bn-p-SCN-GGGRDN-IF7具有合成方便、靶向性好、肿瘤摄取好等优点，有望成为检测肿瘤中AnxA1水平的一种潜在的正电子发射计算机断层扫描显像剂。
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 (AlF)-F-18. The targeting characteristics of the radiolabeled peptides were evaluated in the Anxa1 positive A431 tumor model. Micro-positron emission tomography (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 0.5, 1, and 2 h post-injection, respectively). Anxa1 binding specificity was also demonstrated by reduced tumor uptake after co-injection with excessive unlabeled GGGRDN-IF7 peptide at 30, 60, and 120 min post-injection.F-18-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.