ArticleMolecular pharmaceutics2014
Comparison of conjugation strategies of cross-bridged macrocyclic chelators with cetuximab for copper-64 radiolabeling and PET imaging of EGFR in colorectal tumor-bearing mice.
Article in Molecular pharmaceutics, 2014. 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, 51 citations in OpenAlex.
- Bioorthogonal Chemistry in Biomolecule Quantification: A Review of Reactions and Strategies.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Review
- Phosphonate-Based Aza-Macrocycle Ligands for Low-Temperature, Stable Chelation of Medicinally Relevant Rare Earth Radiometals and Radiofluorination.Journal of the American Chemical Society · 2024Article
- Sortase-Mediated Site-Specific Conjugation to Prepare Fluorine-18-Labeled Nanobodies.Bioconjugate chemistry · 2024Article
- Copper in colorectal cancer: From copper-related mechanisms to clinical cancer therapies.Clinical and translational medicine · 2024Review
- Methods for the Production of Radiolabeled Bioagents for ImmunoPET.Methods in molecular biology (Clifton, N.J.) · 2024Review
- Synthesis and In Vitro Comparison of DOTA, NODAGA and 15-5 Macrocycles as Chelators for theMolecules (Basel, Switzerland) · 2022Article
- Development and Functional Characterization of a Versatile Radio-/Immunotheranostic Tool for Prostate Cancer Management.Cancers · 2022Article
- Precise engineering of cetuximab encapsulated gadollium nanoassemblies:Drug delivery · 2021Article
- Enzyme mediated incorporation of zirconium-89 or copper-64 into a fragment antibody for same day imaging of epidermal growth factor receptor.Chemical science · 2021Article
- A Pretargeted Imaging Strategy for EGFR-Positive Colorectal Carcinoma via Modulation of Tz-Radioligand Pharmacokinetics.Molecular imaging and biology · 2021Article
- ImmunoPET: Concept, Design, and Applications.Chemical reviews · 2020Review
- Article
- Antibody-nucleotide conjugate as a substrate for DNA polymerases.Chemical science · 2018Article
- A multi-functional polymeric carrier for simultaneous positron emission tomography imaging and combination therapy.Acta biomaterialia · 2018Article
- Chemical aspects of metal ion chelation in the synthesis and application antibody-based radiotracers.Journal of labelled compounds & radiopharmaceuticals · 2018Review
- Article
- Click Chemistry and Radiochemistry: The First 10 Years.Bioconjugate chemistry · 2016Review
- New Bifunctional Chelator p-SCN-PhPr-NE3TA for Copper-64: Synthesis, Peptidomimetic Conjugation, Radiolabeling, and Evaluation for PET Imaging.Inorganic chemistry · 2016Article
- Novel Strategy for Preparing Dual-Modality Optical/PET Imaging Probes via Photo-Click Chemistry.Bioconjugate chemistry · 2016Article
- Highly-efficient and versatile fluorous-tagged Cu(I)-catalyzed azide-alkyne cycloaddition ligand for preparing bioconjugates.Chemical communications (Cambridge, England) · 2015Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
Epidermal growth-factor receptor (EGFR) is overexpressed in a wide variety of solid tumors and has served as a well-characterized target for cancer imaging and therapy. Cetuximab was the first mAb targeting EGFR approved by the FDA for the treatment of metastatic colorectal and head and neck cancers. Previous studies showed that (64)Cu (T1/2 = 12.7 h; β(+) (17.4%)) labeled DOTA-cetuximab showed promise for PET imaging of EGFR-positive tumors; however the in vivo stability of this compound has been questioned. In this study, two recently developed cross-bridged macrocyclic chelators (CB-TE1A1P and CB-TE1K1P) were conjugated to cetuximab using standard NHS coupling procedures and/or strain-promoted azide-alkyne cycloaddition (SPAAC) methodologies. The radiolabeling and in vitro/vivo evaluation of the resulting cetuximab conjugates were compared. Improved Cu-64 labeling efficiency and high specific activity (684 kBq/μg, decay corrected to the end of bombardment) were obtained with the CB-TE1K1P-PEG4-click-cetuximab conjugate. Saturation binding assays indicated that the prepared cetuximab conjugates had comparable affinity (1.32-2.00 nM) in the HCT116 human colorectal tumor cell membranes. In the subsequent in vivo evaluation, (64)Cu-CB-TE1K1P-PEG4-click-cetuximab demonstrated more rapid renal clearance with a higher tumor/nontumor ratio than other (64)Cu-labeled cetuximab conjugates, and it shows the greatest promise for imaging and therapy of EGFR-positive tumors.
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