ArticleBioconjugate chemistry2016
Pretargeted PET Imaging Using a Site-Specifically Labeled Immunoconjugate.
Article in Bioconjugate chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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Who cites it
46 citing papers in PubMed.
- Immuno-positron emission tomography in cardiovascular disease: Advances, challenges, and opportunities.Journal of nuclear cardiology : official publication of the American Society of Nuclear Cardiology · 2026Review
- Colorectal Cancer: A Landscape of New Potential Radiopharmaceuticals.Molecular diagnosis & therapy · 2026Review
- Emerging ImmunoPET probes for precision cancer immunotherapy: molecular targets and translational applications.Frontiers in oncology · 2026Review
- Brain-penetrating peptide and antibody radioligands for proof-of-concept PET imaging of fibrin in Alzheimer's disease.EJNMMI radiopharmacy and chemistry · 2025Article
- Generation of Site-Specifically Labeled Affinity Reagents via Use of a Self-Labeling Single Domain Antibody.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Trans-cyclooctene-a Swiss army knife for bioorthogonal chemistry: exploring the synthesis, reactivity, and applications in biomedical breakthroughs.EJNMMI radiopharmacy and chemistry · 2024Review
- Site-Specific Photoaffinity Bioconjugation for the Creation ofMolecular imaging and biology · 2023Article
- Radiochemistry for positron emission tomography.Nature communications · 2023Review
- Click chemistry: a transformative technology in nuclear medicine.Nature protocols · 2023Review
- Leveraging a Dual Variable Domain Immunoglobulin to Create a Site-Specifically Modified Radioimmunoconjugate.Molecular pharmaceutics · 2023Article
- Antibody-Based In Vivo Imaging of Central Nervous System Targets-Evaluation of a Pretargeting Approach Utilizing a TCO-Conjugated Brain Shuttle Antibody and Radiolabeled Tetrazines.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Pretargeted Imaging beyond the Blood-Brain Barrier-Utopia or Feasible?Pharmaceuticals (Basel, Switzerland) · 2022Article
- Pretargeted PET of Osteodestructive Lesions in Dogs.Molecular pharmaceutics · 2022Article
- Pretargeted PET Imaging with a TCO-Conjugated Anti-CD44v6 Chimeric mAb U36 and [Bioconjugate chemistry · 2022Article
- Development and evaluation of anFrontiers in nuclear medicine · 2022Article
- Tetrazine bioorthogonal chemistry derivedFrontiers in molecular biosciences · 2022Review
- Cucurbituril-Ferrocene: Host-Guest Based Pretargeted Positron Emission Tomography in a Xenograft Model.Bioconjugate chemistry · 2021Article
- IEDDA: An Attractive Bioorthogonal Reaction for Biomedical Applications.Molecules (Basel, Switzerland) · 2021Review
- New Bifunctional Chelators Incorporating Dibromomaleimide Groups for Radiolabeling of Antibodies with Positron Emission Tomography Imaging Radioisotopes.Bioconjugate chemistry · 2021Article
- Enzymatic Methods for the Site-Specific Radiolabeling of Targeting Proteins.Molecules (Basel, Switzerland) · 2021Review
Corrections and comments
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Authors and funding
9 authors.
Funding
Abstract
In recent years, both site-specific bioconjugation techniques and bioorthogonal pretargeting strategies have emerged as exciting technologies with the potential to improve the safety and efficacy of antibody-based nuclear imaging. In the work at hand, we have combined these two approaches to create a pretargeted PET imaging strategy based on the rapid and bioorthogonal inverse electron demand Diels-Alder reaction between a (64)Cu-labeled tetrazine radioligand ((64)Cu-Tz-SarAr) and a site-specifically modified huA33-trans-cyclooctene immunoconjugate ((ss)huA33-PEG12-TCO). A bioconjugation strategy that harnesses enzymatic transformations and strain-promoted azide-alkyne click chemistry was used to site-specifically append PEGylated TCO moieties to the heavy chain glycans of the colorectal cancer-targeting huA33 antibody. Preclinical in vivo validation studies were performed in athymic nude mice bearing A33 antigen-expressing SW1222 human colorectal carcinoma xenografts. To this end, mice were administered (ss)huA33-PEG12-TCO via tail vein injection and-following accumulation intervals of 24 or 48 h-(64)Cu-Tz-SarAr. PET imaging and biodistribution studies reveal that this strategy clearly delineates tumor tissue as early as 1 h post-injection (6.7 ± 1.7%ID/g at 1 h p.i.), producing images with excellent contrast and high tumor-to-background activity concentration ratios (tumor:muscle = 21.5 ± 5.6 at 24 h p.i.). Furthermore, dosimetric calculations illustrate that this pretargeting approach produces only a fraction of the overall effective dose (0.0214 mSv/MBq; 0.079 rem/mCi) of directly labeled radioimmunoconjugates. Ultimately, this method effectively facilitates the high contrast pretargeted PET imaging of colorectal carcinoma using a site-specifically modified immunoconjugate.
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Registered trials
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