18F-FP-PEG2-β-Glu-RGD2: A Symmetric Integrin αvβ3-Targeting Radiotracer for Tumor PET Imaging.
18F-FP-PEG2-β-Glu-RGD2: A Symmetric Integrin αvβ3-Targeting Radiotracer for Tumor PET Imaging.
复制标题
18F-FP-PEG2-β-Glu-RGD2：用于肿瘤 PET 成像的对称整合素 αvβ3 靶向放射性示踪剂
DOI：
10.1371/journal.pone.0138675
复制
发表时间：
2015
期刊：
影响因子：
3.7
通讯作者：
He S
中科院分区：
文献类型：
--
作者：
Hu K;Tang X;Tang G;Yao S;Yao B;Wang H;Nie D;Liang X;Tang C;He S
放射性标记环精氨酸-甘氨酸-天冬氨酸（RGD）肽可用于无创检测肿瘤中整合素αvβ3的表达。在这项研究中，我们对一种新的18f标记的RGD同二聚体肽进行了放射合成和生物学评价，该肽在谷氨酸β-氨基（18F-FP-PEG2-β- glul - rgd2）上有一个8-氨基-3,6-二草辛酸（PEG2）连接体，作为肿瘤成像的对称PET示踪剂。生物分布研究表明，18F-FP-PEG2-β-Glu-RGD2的放射性主要通过肾脏排泄从血液中迅速清除。18F-FP-PEG2-β-Glu-RGD2的显微pet - ct成像显示A549人肺腺癌小鼠模型、PC-3前列腺癌小鼠模型和原位移植C6脑胶质瘤模型的肿瘤高对比度和低背景。18F-FP-PEG2-β-Glu-RGD2在体外和体内均具有良好的稳定性。结果表明，该示踪剂是一种潜在的PET肿瘤显像示踪剂。
Radiolabeled cyclic arginine-glycine-aspartic (RGD) peptides can be used for noninvasive determination of integrin αvβ3 expression in tumors. In this study, we performed radiosynthesis and biological evaluation of a new 18F-labeled RGD homodimeric peptide with one 8-amino-3,6-dioxaoctanoic acid (PEG2) linker on the glutamate β-amino group (18F-FP-PEG2-β-Glu-RGD2) as a symmetric PET tracer for tumor imaging. Biodistribution studies showed that radioactivity of 18F-FP-PEG2-β-Glu-RGD2 was rapidly cleared from blood by predominately renal excretion. MicroPET-CT imaging with 18F-FP-PEG2-β-Glu-RGD2 revealed high tumor contrast and low background in A549 human lung adenocarcinoma-bearing mouse models, PC-3 prostate cancer-bearing mouse models, and orthotopic transplanted C6 brain glioma models. 18F-FP-PEG2-β-Glu-RGD2 exhibited good stability in vitro and in vivo. The results suggest that this tracer is a potential PET tracer for tumor imaging.