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PET Imaging of VEGFR with a Novel 64Cu-Labeled Peptide.


ABSTRACT: 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 [64Cu]VEGF125-136 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 [64Cu]VEGF125-136 as a promising, clinically translatable PET tracer for the imaging of tumor angiogenesis.

SUBMITTER: Hu K 

PROVIDER: S-EPMC7178340 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature

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PET Imaging of VEGFR with a Novel <sup>64</sup>Cu-Labeled Peptide.

Hu Kuan K   Shang Jingjie J   Xie Lin L   Hanyu Masayuki M   Zhang Yiding Y   Yang Zhimin Z   Xu Hao H   Wang Lu L   Zhang Ming-Rong MR  

ACS omega 20200408 15


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 [<sup>64</sup>Cu]VEGF<sub>125-136</sub> 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 VEG  ...[more]

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