ArticleBioconjugate chemistry2015
Click-chemistry strategy for labeling antibodies with copper-64 via a cross-bridged tetraazamacrocyclic chelator scaffold.
Article in Bioconjugate chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 20 citations in OpenAlex.
- Molecular targets and the emerging role of copper radionuclides in prostate cancer theranostics.EJNMMI research · 2025Review
- Monovalent and Divalent Designs of Copper Radiotheranostics Targeting Fibroblast Activation Protein in Cancer.Cancers · 2024Article
- Improved extraction efficiency of radioactive copper produced via accelerator neutrons method through phosphate buffer-enhanced column pre-treatment.Scientific reports · 2024Article
- Apoptosis Imaging in Oncology by Means of Positron Emission Tomography: A Review.International journal of molecular sciences · 2021Review
- ImmunoPET: Concept, Design, and Applications.Chemical reviews · 2020Review
- Avenues to molecular imaging of dying cells: Focus on cancer.Medicinal research reviews · 2018Review
- PET radiometals for antibody labeling.Journal of labelled compounds & radiopharmaceuticals · 2018Review
- Click Chemistry and Radiochemistry: The First 10 Years.Bioconjugate chemistry · 2016Review
- Aminopeptidase P Mediated Targeting for Breast Tissue Specific Conjugate Delivery.Bioconjugate chemistry · 2016Article
- High Yield Production and Radiochemical Isolation of Isotopically Pure Arsenic-72 and Novel Radioarsenic Labeling Strategies for the Development of Theranostic Radiopharmaceuticals.Bioconjugate chemistry · 2016Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
We report a click-chemistry based modular strategy for antibody labeling with (64)Cu (t1/2 = 12.7 h; β(+) 0.656 MeV, 17.4%; β(-) 0.573 MeV, 39%; EC 43%) under ambient condition utilizing a cross-bridged tetraazamacrocyclic (CB-TE2A) analogue, which otherwise requires harsh conditions that make the CB-TE2A analogues under-utilized for protein labeling despite the fact that they form kinetically inert copper complexes with high in vivo stability. Our strategy involves prelabeling a CB-TE2A based scaffold (CB-TE2A-1C) with (64)Cu and its subsequent reaction with an antibody via the tetrazine-norbornene mediated click chemistry. The effectiveness of this strategy was demonstrated by labeling two monoclonal antibodies, an anti-PSMA antibody (YPSMA-1) and a chimeric anti-phosphatidylserine antibody (Bavituximab). The immunoreactivity of the antibodies remained unchanged after the tetrazine modification and click-chemistry (64)Cu labeling. To further demonstrate the practicality of the modular (64)Cu labeling strategy, we tested positron emission tomography (PET) imaging of tumor with the (64)Cu-labeled bavituximab in a mouse xenograft model. The tumor visualization and uptake of the labeled antibody exhibited the versatility of the click-chemistry strategy.
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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.