ArticleChemical science2022
All-in-one disulfide bridging enables the generation of antibody conjugates with modular cargo loading.
Article in Chemical science, 2022. 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.
- Site-Specific Labeling of PD-L1 Fab through Disulfide Rebridging for ImmunoPET Imaging.Chemical & biomedical imaging · 2026Article
- Generation of DAR1 Glycosite-Specific Antibody-Drug Conjugates Using DisacLink Technology.Chembiochem : a European journal of chemical biology · 2026Article
- Boosting peptide half-life: enabling efficient generation of Fc-peptide conjugates.Chemical science · 2026Article
- On-resin assembly of cysteine-reactive linkers for controlled site-selective antibody bioconjugation.Nature protocols · 2026Review
- Stoichiometrically Defined Antibody-DNA Conjugates for Quantitative Super-Resolution Imaging.Nano letters · 2026Article
- Enabling the synthesis of multi-payload thio-antibody conjugates through the use of pyridazinediones,RSC chemical biology · 2026Article
- Antibody-drug conjugates for infectious and neglected tropical diseases: chemical design principles, target biology, and translational challenges.Frontiers in chemistry · 2026Review
- Cysteine Re-bridging Using Divinyl Pyrimidine Reagents for the Generation of Antibody-Drug Conjugates.Methods in molecular biology (Clifton, N.J.) · 2026Article
- Intact Mass Spectrometry Analysis of Immuno-Isolated Human Therapeutic Antibodies from Serum.Methods in molecular biology (Clifton, N.J.) · 2026Article
- Site-specific labelling of native peptides and proteins: chemical and enzymatic strategies.Beilstein journal of organic chemistry · 2026Review
- Homogeneous antibody-drug conjugates with dual payloads: potential, methods and considerations.mAbs · 2025Review
- Article
- Unsaturated Phosphine Oxides for Modular Antibody Rebridging and Single Reagent Peptide-Cyclization-Bioconjugation.Angewandte Chemie (International ed. in English) · 2025Article
- Methods for the Generation of Single-Payload Antibody-Drug Conjugates.ChemMedChem · 2025Article
- Therapeutic potential of antibody-drug conjugates possessing bifunctional anti-inflammatory action in the pathogenies of rheumatoid arthritis.Arthritis research & therapy · 2024Review
- NSPs: chromogenic linkers for fast, selective, and irreversible cysteine modification.Chemical science · 2024Article
- Homogeneous multi-payload antibody-drug conjugates.Nature chemistry · 2024Review
- The Nitrile Bis-Thiol Bioconjugation Reaction.Journal of the American Chemical Society · 2024Article
- Antibody-drug conjugates in cancer therapy: innovations, challenges, and future directions.Archives of pharmacal research · 2024Review
- Disulfide re-bridging reagents for single-payload antibody-drug conjugates.Chemical communications (Cambridge, England) · 2023Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Antibody-drug conjugates (ADCs) are valuable therapeutic entities which leverage the specificity of antibodies to selectively deliver cytotoxins to antigen-expressing targets such as cancer cells. However, current methods for their construction still suffer from a number of shortcomings. For instance, using a single modification technology to modulate the drug-to-antibody ratio (DAR) in integer increments while maintaining homogeneity and stability remains exceptionally challenging. Herein, we report a novel method for the generation of antibody conjugates with modular cargo loading from native antibodies. Our approach relies on a new class of disulfide rebridging linkers, which can react with eight cysteine residues, thereby effecting all-in-one bridging of all four interchain disulfides in an IgG1 antibody with a single linker molecule. Modification of the antibody with the linker in a 1 : 1 ratio enabled the modulation of cargo loading in a quick and selective manner through derivatization of the linker with varying numbers of payload attachment handles to allow for attachment of either 1, 2, 3 or 4 payloads (fluorescent dyes or cytotoxins). Assessment of the biological activity of these conjugates demonstrated their exceptional stability in human plasma and utility for cell-selective cytotoxin delivery or imaging/diagnostic applications.
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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.