PT - JOURNAL ARTICLE AU - Hu, Kuan AU - Shang, Jingjie AU - Xie, Lin AU - Hanyu, Masayuki AU - Zhang, Yiding AU - Yang, Zhimin AU - Yang, Zhimin AU - Xu, Hao AU - Wang, Lu AU - Zhang, Ming-Rong TI - <strong>Positron Emission Tomography Imaging of Vascular Endothelial</strong><strong> </strong><strong>Growth Factor</strong><strong> </strong><strong>Receptor Expression with</strong><strong> a new</strong><strong> </strong><strong><sup>64</sup></strong><strong>Cu labeled peptide</strong><strong/> DP - 2020 May 01 TA - Journal of Nuclear Medicine PG - 1052--1052 VI - 61 IP - supplement 1 4099 - http://jnm.snmjournals.org/content/61/supplement_1/1052.short 4100 - http://jnm.snmjournals.org/content/61/supplement_1/1052.full SO - J Nucl Med2020 May 01; 61 AB - 1052Objectives: Noninvasive positron emission tomography (PET) imaging of vascular endothelial growth factor receptor 2 (VEGFR-2) expression could be a valuable tool for evaluation of patients with a variety of malignancies, and particularly for monitoring those undergoing antiangiogenic therapies that block VEGF/VEGFR-2 function. VEGF125-136 (QKRKRKKSRYKS) is a 12 amino acid peptide encoded by exon 6 of VEGF-A which was first identified as an effective inhibitor to VEGFR-2. The aim of this work was to develop and evaluate in mice the 64Cu labelled analogue as an in vivo tracer for VEGFR-2 expression in solid tumours. Methods: VEGF125-136 was conjugated with PEG3 and DOTA and then labeled with 64Cu (denoted as [64Cu]VEGF125-136) for small-animal PET of mice bearing B16F10 human melanoma cells, U87MG human glioblastoma cells, and MDA-231 human breast cancer xenografts. Biodistribution studies, autoradiography and immunofluorescence staining were carried out to confirm the noninvasive imaging results. Results: The radiolabeling yield and specific activity of [64Cu]VEGF125-136 were more than 95% and 74.3 ± 3.8 GBq/µmol, respectively. Noninvasive microPET showed that [64Cu]VEGF125-136 had variable uptake in different tumors, with the order: B16F10 &gt; U87MG &gt; MDA-231. The pattern of radiotracer uptake was correlated well with variations in VEGFR-2 expression determined ex vivo by immunohistochemical analysis. Moreover, the tracer showed high tumor uptake (5.89 ± 2.58 %ID/g at 20 min postinjection in B16F10 mice) and excellent pharmacokinetics, achieving the maximum imaging quality within 1 h after injection. Biodistribution studies and autoradiography confirmed the VEGFR-2 specificity of [64Cu]VEGF125-136. Conclusions: We have developed a VEGFR-2-specific PET tracer, [64Cu]VEGF125-136. This tracer may be translated into the clinic for imaging tumor angiogenesis and monitoring antiangiogenic treatment efficacy.