PET Imaging of VEGFR with a Novel 64Cu-Labeled Peptide
PET Imaging of VEGFR with a Novel 64Cu-Labeled Peptide
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使用新型 64Cu 标记肽对 VEGFR 进行 PET 成像
DOI：
10.1021/acsomega.9b03953
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发表时间：
2020-04-21
期刊：
影响因子：
4.1
通讯作者：
Zhang, Ming-Rong
中科院分区：
文献类型：
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作者：
Hu, Kuan;Shang, Jingjie;Zhang, Ming-Rong
血管内皮生长因子受体（VEGFRs）被认为是肿瘤血管生成的重要生物标志物。在此，我们开发了一种基于肽的VEGFR正电子发射断层扫描（PET）示踪剂。新型[Cu-64]VEGF（125-136）肽具有令人满意的放射特性，在各种小鼠模型中显示出良好的VEGFR可视化特异性，其中肿瘤特异性放射性摄取与VEGFR表达水平高度相关。此外，该示踪剂在B16F10小鼠中显示出高的肿瘤摄取（注射后20分钟约为5.89% ID/g）和良好的药代动力学，在注射后1小时内达到最大的成像质量。这些特征表明[Cu-64]VEGF（125-136）是一种有前景的、临床可翻译的肿瘤血管生成成像PET示踪剂。
Vascular endothelial growth factor receptors (VEGFRs) are well recognized as significant biomarkers of tumor angiogenesis. Herein, we have developed a first-of-its-kind peptide-based VEGFR positron emission tomography (PET) tracer. The novel [Cu-64]VEGF(125-136) peptide possessed satisfactory radio-characteristics and showed good specificity for the visualization of VEGFR in various mouse models, in which the tumor-specific radioactivity uptake was highly correlated to the VEGFR expression level. Moreover, the tracer showed high tumor uptake (ca. 5.89 %ID/g at 20 min postinjection in B16F10 mice) and excellent pharmacokinetics, achieving the maximum imaging quality within 1 h after injection. These features convey [Cu-64]VEGF(125-136) as a promising, clinically translatable PET tracer for the imaging of tumor angiogenesis.