ArticlePloS one2013
Influence of macrocyclic chelators on the targeting properties of (68)Ga-labeled synthetic affibody molecules: comparison with (111)In-labeled counterparts.
Article in PloS one, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
24 citing papers in PubMed, 60 citations in OpenAlex.
- Selection of the optimal chelator for labeling of DARPin Ec1 with gallium-68 for PET imaging of EpCAM expression.EJNMMI radiopharmacy and chemistry · 2025Article
- Preclinical research progress in HER2-targeted small-molecule probes for breast cancer.Radiologie (Heidelberg, Germany) · 2024Review
- Surface-engineered bacteria in drug development.Microbial biotechnology · 2024Review
- Implications of physics, chemistry and biology for dosimetry calculations using theranostic pairs.Theranostics · 2022Review
- Advances in the Application of Radionuclide-Labeled HER2 Affibody for the Diagnosis and Treatment of Ovarian Cancer.Frontiers in oncology · 2022Review
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- Development of Radiogallium-Labeled Peptides for Platelet-Derived Growth Factor ReceptorMolecules (Basel, Switzerland) · 2020Article
- Preclinical Evaluation of the Copper-64 Labeled GRPR-Antagonist RM26 in Comparison with the Cobalt-55 Labeled Counterpart for PET-Imaging of Prostate Cancer.Molecules (Basel, Switzerland) · 2020Article
- Assessment of Chemotherapy-Induced Organ Damage with Ga-68 Labeled Duramycin.Molecular imaging and biology · 2020Article
- Affibody Molecules as Targeting Vectors for PET Imaging.Cancers · 2020Review
- Article
- Increase in negative charge ofScientific reports · 2019Article
- PET Imaging of HER2-Positive Tumors with Cu-64-Labeled Affibody Molecules.Molecular imaging and biology · 2019Article
- Preclinical Evaluation of [Cells · 2018Article
- Radionuclide imaging of VEGFR2 in glioma vasculature using biparatopic affibody conjugate: proof-of-principle in a murine model.Theranostics · 2018Article
- Radiolabeling and Preliminary Evaluation of Ga-68 Labeled NODAGA-Ubiquicidin Fragments for Prospective Infection Imaging.Molecular imaging and biology · 2017Article
- Comparative Evaluation of Anti-HER2 Affibody Molecules Labeled withContrast media & molecular imaging · 2017Article
- Preclinical evaluation of [(68)Ga]NOTA-pentixafor for PET imaging of CXCR4 expression in vivo - a comparison to [(68)Ga]pentixafor.EJNMMI research · 2016Article
- Evaluation of a PACAP Peptide Analogue Labeled with (68)Ga Using Two Different Chelating Agents.Cancer biotherapy & radiopharmaceuticals · 2016Article
- Advances in PET Detection of the Antitumor T Cell Response.Advances in immunology · 2016Review
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Affibody molecules are a class of small (7 kDa) non-immunoglobulin scaffold-based affinity proteins, which have demonstrated substantial potential as probes for radionuclide molecular imaging. The use of positron emission tomography (PET) would further increase the resolution and quantification accuracy of Affibody-based imaging. The rapid in vivo kinetics of Affibody molecules permit the use of the generator-produced radionuclide (68)Ga (T1/2=67.6 min). Earlier studies have demonstrated that the chemical nature of chelators has a substantial influence on the biodistribution properties of Affibody molecules. To determine an optimal labeling approach, the macrocyclic chelators 1,4,7,10-tetraazacylododecane-1,4,7,10-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-N,N,N-triacetic acid (NOTA) and 1-(1,3-carboxypropyl)-1,4,7- triazacyclononane-4,7-diacetic acid (NODAGA) were conjugated to the N-terminus of the synthetic Affibody molecule ZHER2:S1 targeting HER2. Affibody molecules were labeled with (68)Ga, and their binding specificity and cellular processing were evaluated. The biodistribution of (68)Ga-DOTA-ZHER2:S1, (68)Ga-NOTA-ZHER2:S1 and (68)Ga-NODAGA-ZHER2:S1, as well as that of their (111)In-labeled counterparts, was evaluated in BALB/C nu/nu mice bearing HER2-expressing SKOV3 xenografts. The tumor uptake for (68)Ga-DOTA-ZHER2:S1 (17.9 ± 0.7%IA/g) was significantly higher than for both (68)Ga-NODAGA-ZHER2:S1 (16.13 ± 0.67%IA/g) and (68)Ga-NOTA-ZHER2:S1 (13 ± 3%IA/g) at 2 h after injection. (68)Ga-NODAGA-ZHER2:S1 had the highest tumor-to-blood ratio (60 ± 10) in comparison with both (68)Ga-DOTA-ZHER2:S1 (28 ± 4) and (68)Ga-NOTA-ZHER2:S1 (42 ± 11). The tumor-to-liver ratio was also higher for (68)Ga-NODAGA-ZHER2:S1 (7 ± 2) than the DOTA and NOTA conjugates (5.5 ± 0.6 vs.3.3 ± 0.6). The influence of chelator on the biodistribution and targeting properties was less pronounced for (68)Ga than for (111)In. The results of this study demonstrate that macrocyclic chelators conjugated to the N-terminus have a substantial influence on the biodistribution of HER2-targeting Affibody molecules labeled with (68)Ga.This can be utilized to enhance the imaging contrast of PET imaging using Affibody molecules and improve the sensitivity of molecular imaging. The study demonstrated an appreciable difference of chelator influence for (68)Ga and (111)In.
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