ArticleNature communications2024
An all-in-one tetrazine reagent for cysteine-selective labeling and bioorthogonal activable prodrug construction.
Article in Nature communications, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 19 papers.
What it found
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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.
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Who cites it
19 citing papers in PubMed, 47 citations in OpenAlex.
- Engineering Functional Biomaterials for Targeted and Localized Cancer Drug Delivery: A Structure-Property-Performance Design Perspective.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Organelle-Resolved Tetrazine-trans-Cyclooctene Click Chemistry for Cargo Delivery and Release.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Modular Assembly of Bioconjugates Enabled by a Pyridine-Based Chemoselective Sequential Conjugation Platform.Angewandte Chemie (International ed. in English) · 2026Article
- Tetrazine-Enabled Peptide Macrocyclization and Bioorthogonal Cell Penetration Profiling.JACS Au · 2026Article
- Pharmacokinetic Optimization of Radiocopper-Based Theranostic Pretargeting.Molecular pharmaceutics · 2026Article
- Exploiting intracellular oncogenic proteins to release cytotoxins.RSC medicinal chemistry · 2026Article
- Spatiotemporally controlled drug release via a click-release system utilizing mono-alkyl-hydroxylamine and cyclooctyne chemistry.Nature communications · 2026Article
- Bioorthogonal Chemistry in Biomolecule Quantification: A Review of Reactions and Strategies.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Review
- Spatiotemporally Controlled Bioorthogonal Prodrug Activation for Precise Chemotherapy.Small science · 2026Article
- Achieving cysteine-selective peptide/protein bioconjugation via tunable triazine-pyridine chemistry.Science advances · 2025Article
- Article
- Surface keratin 1, a tumor-selective peptide target in human triple-negative breast cancer.Scientific reports · 2025Article
- Manipulating DNA and RNA structures via click-to-release caged nucleic acids for biological and biomedical applications.Nucleic acids research · 2025Article
- Click-Controlled Photo-Uncaging: Click-Assembly of Platinum-Based Photoactive Protecting Groups for Light-Triggered Bioactive Molecule Release.Journal of the American Chemical Society · 2025Article
- Challenging and new opportunities for prodrug technology.Investigational new drugs · 2025Review
- Fluorogenic Tetrazine Bioorthogonal Probes for Advanced Application in Bioimaging and Biomedicine.Chemical & biomedical imaging · 2025Article
- Dual-Performing Vinyltetrazine for Rapid, Selective Bioconjugation and Functionalization of Cysteine Proteins.ACS chemical biology · 2025Article
- Ortho-functionalized pyridinyl-tetrazines break the inverse correlation between click reactivity and cleavage yields in click-to-release chemistry.Communications chemistry · 2024Article
- Strategies for the development of stimuli-responsive small molecule prodrugs for cancer treatment.Frontiers in pharmacology · 2024Review
Corrections and comments
- Erratum issued
Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
The prodrug design strategy offers a potent solution for improving therapeutic index and expanding drug targets. However, current prodrug activation designs are mainly responsive to endogenous stimuli, resulting in unintended drug release and systemic toxicity. In this study, we introduce 3-vinyl-6-oxymethyl-tetrazine (voTz) as an all-in-one reagent for modular preparation of tetrazine-caged prodrugs and chemoselective labeling peptides to produce bioorthogonal activable peptide-prodrug conjugates. These stable prodrugs can selectively bind to target cells, facilitating cellular uptake. Subsequent bioorthogonal cleavage reactions trigger prodrug activation, significantly boosting potency against tumor cells while maintaining exceptional off-target safety for normal cells. In vivo studies demonstrate the therapeutic efficacy and safety of this prodrug design approach. Given the broad applicability of functional groups and labeling versatility with voTz, we foresee that this strategy will offer a versatile solution to enhance the therapeutic range of cytotoxic agents and facilitate the development of bioorthogonal activatable biopharmaceuticals and biomaterials.
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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.