ArticleMolecular pharmaceutics2012
Positron emission tomography imaging of vascular endothelial growth factor receptor expression with (61)Cu-labeled lysine-tagged VEGF121.
Article in Molecular pharmaceutics, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Novel Molecular Classification of Breast Cancer with PET Imaging.Medicina (Kaunas, Lithuania) · 2024Review
- Article
- Production of the PET radionuclideEJNMMI radiopharmacy and chemistry · 2024Article
- The Role of VEGF Receptors as Molecular Target in Nuclear Medicine for Cancer Diagnosis and Combination Therapy.Cancers · 2021Review
- PET Imaging of VEGFR with a NovelACS omega · 2020Article
- Molecular imaging of Toll-like receptor 4 detects ischemia-reperfusion injury during intussusception.Oncotarget · 2018Article
- Radionuclide imaging of VEGFR2 in glioma vasculature using biparatopic affibody conjugate: proof-of-principle in a murine model.Theranostics · 2018Article
- PET Imaging of VEGFR-2 Expression in Lung Cancer with 64Cu-Labeled Ramucirumab.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2016Article
- Deglycosylation of mAb by EndoS for improved molecular imaging.Molecular imaging and biology · 2015Article
- Radiolabeling and evaluation of (64)Cu-DOTA-F56 peptide targeting vascular endothelial growth factor receptor 1 in the molecular imaging of gastric cancer.American journal of cancer research · 2015Article
- VEGF₁₂₁-conjugated mesoporous silica nanoparticle: a tumor targeted drug delivery system.ACS applied materials & interfaces · 2014Article
- New radiotracers for imaging of vascular targets in angiogenesis-related diseases.Advanced drug delivery reviews · 2014Review
- New strategy for monitoring targeted therapy: molecular imaging.International journal of nanomedicine · 2013Review
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Authors and funding
9 authors.
Funding
Abstract
Overexpression of vascular endothelial growth factor (VEGF) and VEGF receptors (VEGFRs) indicates poor prognosis for cancer patients in a variety of clinical studies. Our goal is to develop a tracer for positron emission tomography (PET) imaging of VEGFR expression using recombinant human VEGF121 with three lysine residues fused to the N-terminus (denoted as K3-VEGF121), which can facilitate radiolabeling without affecting its VEGFR binding affinity. K3-VEGF121 was conjugated with 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) and labeled with (61)Cu (t1/2: 3.3 h; 62% β(+)). The IC50 value of NOTA-K3-VEGF121 for VEGFR-2 was comparable to that of K3-VEGF121 (1.50 and 0.65 nM, respectively) based on a cell binding assay. (61)Cu labeling was achieved with good yield (55 ± 10%) and specific activity (4.2 GBq/mg). Serial PET imaging showed that the 4T1 tumor uptake of (61)Cu-NOTA-K3-VEGF121 was 3.4 ± 0.5, 4.9 ± 1.0, 5.2 ± 1.0, and 4.8 ± 0.8%ID/g (n = 4) at 0.5, 2, 4, and 8 h postinjection, respectively, which was consistent with biodistribution data measured by γ counting. Blocking experiments and ex vivo histology confirmed the VEGFR specificity of (61)Cu-NOTA-K3-VEGF121. Extrapolated human dosimetry calculation showed that liver was the organ with the highest radiation dose. The use of (61)Cu as the radiolabel is desirable for small proteins such as K3-VEGF121, which has a much higher β(+) branching ratio than the commonly used (64)Cu (62% vs 17%), thereby offering stronger signal intensity and lower tracer dose for PET imaging.
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