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]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 [⁶⁴Cu]VEGF_125-136 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