ArticleMolecular imaging and biology2014
Characterization and evaluation of (64)Cu-labeled A20FMDV2 conjugates for imaging the integrin αvβ 6.
Article in Molecular imaging and biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- PET imaging of hepatocellular carcinoma by targeting tumor-associated endothelium using [European journal of nuclear medicine and molecular imaging · 2022Article
- Synthesis and Systematic Study on the Effect of Different PEG Units on Stability of PEGylated, Integrin-αvβ6-Specific A20FMDV2 Analogues in Rat Serum and Human Plasma.Molecules (Basel, Switzerland) · 2022Article
- Therapeutic Efficacy ofPharmaceuticals (Basel, Switzerland) · 2022Article
- A comparison ofOncotarget · 2022Article
- Evaluation of Two Optical Probes for Imaging the Integrin αMolecular imaging and biology · 2020Article
- Preclinical evaluation of [European journal of nuclear medicine and molecular imaging · 2020Article
- PET/CT Imaging of NSCLC with a αMolecular imaging and biology · 2019Article
- Emerging imaging targets for infiltrative cardiomyopathy: Inflammation and fibrosis.Journal of nuclear cardiology : official publication of the American Society of Nuclear Cardiology · 2019Review
- Molecular design of radiocopper-labelled Affibody molecules.Scientific reports · 2018Article
- Small-animal SPECT/CT imaging of cancer xenografts and pulmonary fibrosis using aBiophysics reports · 2018Article
- The somatostatin receptor 2 antagonist 64Cu-NODAGA-JR11 outperforms 64Cu-DOTA-TATE in a mouse xenograft model.PloS one · 2018Article
- Imaging the Tumor Microenvironment.Advances in experimental medicine and biology · 2017Review
- Comparative Evaluation of Anti-HER2 Affibody Molecules Labeled withContrast media & molecular imaging · 2017Article
- Molecular imaging of integrin αvβ6 expression in living subjects.American journal of nuclear medicine and molecular imaging · 2014Review
- PET radiopharmaceuticals for imaging integrin expression: tracers in clinical studies and recent developments.BioMed research international · 2014Review
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8 authors.
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Abstract
purposeThe integrin αvβ6 is overexpressed in a variety of aggressive cancers and serves as a prognosis marker. This study describes the conjugation, radiolabeling, and in vitro and in vivo evaluation of four chelators to determine the best candidate for (64)Cu radiolabeling of A20FMDV2, an αvβ6 targeting peptide. PROCEDURES: Four chelators were conjugated onto PEG28-A20FMDV2 (1): 11-carboxymethyl-1,4,8,11-tetraazabicyclo[6.6.2]hexadecane-4-methanephosphonic acid (CB-TE1A1P), 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA), and 4,4'-((3,6,10,13,16,19-hexazazbicyclo[6.6.6]ico-sane-1,8-diylbis(aza-nediyl))bis(methylene)dibenzoic acid (BaBaSar). All peptides were radiolabeled with (64)Cu in ammonium acetate buffer at pH 6 and formulated to pH 7.2 in PBS for use. The radiotracers were evaluated using in vitro cell binding and internalization assays and serum stability assays. In vivo studies conducted include blocking, biodistribution, and small animal PET imaging. Autoradiography and histology were also conducted.
resultsAll radiotracers were radiolabeled in good radiochemical purity (>95 %) under mild conditions (37-50 °C for 15 min) with high specific activity (0.58-0.60 Ci/μmol). All radiotracers demonstrated αvβ6-directed cell binding (>46 %) with similar internalization levels (>23 %). The radiotracers (64)Cu-CB-TE1A1P-1 and (64)Cu-BaBaSar-1 showed improved specificity for the αvβ6 positive tumor in vivo over (64)Cu-DOTA-1 and (64)Cu-NOTA-1 (+/- tumor uptake ratios-3.82 +/- 0.44, 3.82 ± 0.41, 2.58 ± 0.58, and 1.29 ± 0.14, respectively). Of the four radiotracers, (64)Cu-NOTA-1 exhibited the highest liver uptake (10.83 ± 0.1 % ID/g at 4 h).
conclusionsWe have successfully conjugated, radiolabeled, and assessed the four chelates CB-TE1A1P, DOTA, NOTA, and BaBaSar both in vitro and in vivo. However, the data suggests no clear "best candidate" for the (64)Cu-radiolabeling of A20FMDV2, but instead a trade-off between the different properties (e.g., stability, selectivity, pharmacokinetics, etc.) with no obvious effects of the individual chelators.
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