ReviewJournal of labelled compounds & radiopharmaceuticals2014
The inverse electron demand Diels-Alder click reaction in radiochemistry.
Review in Journal of labelled compounds & radiopharmaceuticals, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 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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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
40 citing papers in PubMed, 61 citations in OpenAlex.
- Affinity-Tuned Albumin Hitchhiking Extends the Bioorthogonal Capture Window in Pretargeting Radiotheranostics.Advanced healthcare materials · 2026Article
- A novelEJNMMI radiopharmacy and chemistry · 2026Article
- Exploring the Power of Metal-Free Click Transformations toward the Synthesis of Highly Functionalized Dendrimers for Applications in Drug Delivery.ACS applied materials & interfaces · 2025Article
- Radiochemistry for positron emission tomography.Nature communications · 2023Review
- Toward OptimizedPharmaceutics · 2022Article
- Recent Advances in the Development of Tetrazine Ligation Tools for Pretargeted Nuclear Imaging.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Technological Innovations in Photochemistry for Organic Synthesis: Flow Chemistry, High-Throughput Experimentation, Scale-up, and Photoelectrochemistry.Chemical reviews · 2022Review
- Side-by-Side Comparison of Five Chelators forCancers · 2021Article
- Click-functionalized hydrogel design for mechanobiology investigations.Molecular systems design & engineering · 2021Article
- Perspectives on metals-based radioimmunotherapy (RIT): moving forward.Theranostics · 2021Review
- A Cleavable CJournal of the American Chemical Society · 2020Article
- A Pretargeted Imaging Strategy for Immune Checkpoint Ligand PD-L1 Expression in Tumor Based on Bioorthogonal Diels-Alder Click Chemistry.Molecular imaging and biology · 2020Article
- Improving Tumor-to-Background Contrast through Hydrophilic Tetrazines: The Construction ofChemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Site-SpecificPharmaceutics · 2019Article
- A Dual-Modality Linker Enables Site-Specific Conjugation of Antibody Fragments forJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
- Article
- HydrophilicChemical communications (Cambridge, England) · 2019Article
- Leveraging Bioorthogonal Click Chemistry to ImproveClinical cancer research : an official journal of the American Association for Cancer Research · 2019Article
- Pretargeted Nuclear Imaging and Radioimmunotherapy Based on the Inverse Electron-Demand Diels-Alder Reaction and Key Factors in the Pretargeted Synthetic Design.Contrast media & molecular imaging · 2019Review
- An Efficient Method for Labeling Single Domain Antibody Fragments withBioconjugate chemistry · 2018Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
The inverse electron-demand Diels-Alder (IEDDA) cycloaddition between 1,2,4,5-tetrazines and strained alkene dienophiles is an emergent variety of catalyst-free 'click' chemistry that has the potential to have a transformational impact on the synthesis and development of radiopharmaceuticals. The ligation is selective, rapid, high-yielding, clean, and bioorthogonal and, since its advent in 2008, has been employed in a wide variety of chemical settings. In radiochemistry, the reaction has proven particularly useful with (18) F and has already been utilized to create a number of (18) F-labeled agents, including the PARP1-targeting small molecule (18) F-AZD2281, the αv β3 integrin-targeting peptide (18) F-RGD, and the GLP-1-targeting peptide (18) F-exendin. The inherent flexibility of the ligation has also been applied to the construction of radiometal-based probes, specifically the development of a modular strategy for the synthesis of radioimmunoconjugates that effectively eliminates variability in the construction of these agents. Further, the exceptional speed and biorthogonality of the reaction have made it especially promising in the realm of in vivo pretargeted imaging and therapy, and pretargeted imaging strategies based on the isotopes (111) In, (18) F, and (64) Cu have already proven capable of producing images with high tumor contrast and low levels of uptake in background, nontarget organs. Ultimately, the characteristics of inverse electron-demand Diels-Alder click chemistry make it almost uniquely well-suited for radiochemistry, and although the field is young, this ligation has the potential to make a tremendous impact on the synthesis, development, and study of novel radiopharmaceuticals.
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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.