ArticleAmerican journal of nuclear medicine and molecular imaging2011
Peptoid-based PET imaging of vascular endothelial growth factor receptor (VEGFR) expression.
Article in American journal of nuclear medicine and molecular imaging, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 26 citations in OpenAlex.
- Gold- and Platinum-Peptide Bioconjugates in Cancer Therapy: Recent Advances and Future Directions.Pharmaceutics · 2026Review
- Molecular targets and the emerging role of copper radionuclides in prostate cancer theranostics.EJNMMI research · 2025Review
- Cationic Peptoids for Systemic In Vivo Cartilage-Targeting.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Advances in Molecular Imaging of VEGFRs: Innovations in Imaging and Therapeutics.International journal of molecular sciences · 2025Review
- Peptoids: Smart and Emerging Candidates for the Diagnosis of Cancer, Neurological and Autoimmune Disorders.International journal of molecular sciences · 2023Review
- Unbiased peptoid cell screen identifies a peptoid targeting newly appeared cell surface vimentin on tumor transformed early lung cancer cells.Bioorganic & medicinal chemistry · 2022Article
- 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
- Immuno-PET imaging of VEGFR-2 expression in prostate cancer withAmerican journal of cancer research · 2019Article
- In Vitro ADME Properties of Two Novel Antimicrobial Peptoid-Based Compounds as Potential Agents against Canine Pyoderma.Molecules (Basel, Switzerland) · 2018Article
- 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
- Multimodality imaging of CXCR4 in cancer: current status towards clinical translation.Current molecular medicine · 2013Review
- Functionalized upconversion nanoparticles: versatile nanoplatforms for translational research.Current molecular medicine · 2013Review
- Review
- Molecular MRI of VEGFR-2 reveals intra-tumor and inter-tumor heterogeneity.American journal of nuclear medicine and molecular imaging · 2013Article
- Immuno-PET of tissue factor in pancreatic cancer.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2012Article
- Radiolabeled γ-AApeptides: a new class of tracers for positron emission tomography.Chemical communications (Cambridge, England) · 2012Article
- Positron emission tomography imaging of tumor angiogenesis with a 66Ga-labeled monoclonal antibody.Molecular pharmaceutics · 2012Article
- Positron Emission Tomography and Near-Infrared Fluorescence Imaging of Vascular Endothelial Growth Factor with Dual-Labeled Bevacizumab.American journal of nuclear medicine and molecular imaging · 2012Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Non-invasive detection of vascular endothelial growth factor receptor 2 (VEGFR2) by positron emission tomography (PET) would allow the evaluation of tumor vascular activity in vivo. Recently, a dimeric peptoid, GU40C4, was reported as a highly potent antagonist of VEGFR2 activation inhibiting angiogenesis and tumor growth in vivo. The purpose of this work was to evaluate the potential of this peptoid for PET imaging of VEGFR2 expression. To label GU40C4 and a control peptoid with a positron emitter, (64)Cu (t(1/2) = 12.7 h; β(+): 0.653 MeV, 17.4%), a cysteine was introduced to the C-terminus of the peptoids and then conjugated to a bifunctional chelator (DOTA: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) through the maleimide-thiol coupling chemistry. The in vitro binding assay showed a negligible effect of the DOTA conjugation on the VEGFR2 binding affinity of GU40C4. Both peptoid conjugates were efficiently labeled with (64)Cu in high radiochemical yields (> 90%); the specific activity was in the range of 10 - 80 GBq/μmol. PET imaging evaluation using a prostate cancer xenograft (PC3) mouse model showed that (64)Cu-DOTA-GU40C4 had a prominent and steady accumulation in the VEGFR2 positive PC3 tumors (2.25 ± 0.24, 2.15 ± 0.34, and 1.90 ± 0.18 %ID/g at 1, 4, and 20 h p.i., respectively; n = 3), which is significantly higher than the control peptoid conjugate (0.3 - 0.5 %ID/g; p < 0.001 at 1, 4, and 20 h p.i.). Interestingly, the mouse salivary glands were also clearly visualized by (64)Cu-DOTA-GU40C4 (3.17 ± 0.25, 3.00 ± 0.36, and 1.83 ± 0.21 %ID/g at 1, 4, and 20 h p.i., respectively; n = 3) rather than its control peptoid conjugate. VEGFR2 expression in the salivary glands was shown by polymerase chain reaction (PCR) assay. Our results demonstrate that (64)Cu-DOTA-GU40C4 can be used to image the expression of VEGFR2 in vivo.
Indexed as
Identifiers
23133797PMC3477717W1858030301What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.