ArticleOrganic & biomolecular chemistry2018
Highly homogeneous antibody modification through optimisation of the synthesis and conjugation of functionalised dibromopyridazinediones.
Article in Organic & biomolecular chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 78 citations in OpenAlex.
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- Site-Specific Labeling of PD-L1 Fab through Disulfide Rebridging for ImmunoPET Imaging.Chemical & biomedical imaging · 2026Article
- Efficiency landscape of bioorthogonal click reactions producing bispecific antibody conjugates.Cell reports methods · 2026Article
- On-resin assembly of cysteine-reactive linkers for controlled site-selective antibody bioconjugation.Nature protocols · 2026Review
- Enabling the synthesis of multi-payload thio-antibody conjugates through the use of pyridazinediones,RSC chemical biology · 2026Article
- Tunable Linkers for Dynamic Thiol-Based Bioconjugation Strategies.Biomacromolecules · 2026Review
- A Modular and Convergent "Stick and Click" Conjugation Platform Enables Fast Antibody Conjugate Library Synthesis.Bioconjugate chemistry · 2026Article
- Mass spectrometric imaging and quantitative analysis of theInorganic chemistry frontiers · 2025Article
- Unsaturated Phosphine Oxides for Modular Antibody Rebridging and Single Reagent Peptide-Cyclization-Bioconjugation.Angewandte Chemie (International ed. in English) · 2025Article
- Comparative Study of Click Handle Stability in Common Ligation Conditions.Bioconjugate chemistry · 2025Article
- A review of conjugation technologies for antibody drug conjugates.Antibody therapeutics · 2025Review
- Site-Selective Antibody Conjugation with Dibromopyrazines.Bioconjugate chemistry · 2024Article
- Exploring the next generation of antibody-drug conjugates.Nature reviews. Clinical oncology · 2024Review
- The Nitrile Bis-Thiol Bioconjugation Reaction.Journal of the American Chemical Society · 2024Article
- Orthogonal Hydroxyl Functionalization of cGAMP Confers Metabolic Stability and Enables Antibody Conjugation.ACS central science · 2023Article
- Antibody-Proteolysis Targeting Chimera Conjugate Enables Selective Degradation of Receptor-Interacting Serine/Threonine-Protein Kinase 2 in HER2+ Cell Lines.Bioconjugate chemistry · 2023Article
- Chemical generation of checkpoint inhibitory T cell engagers for the treatment of cancer.Nature chemistry · 2023Article
- Synthesis and Application of Two-Photon Active Fluorescent Rhodol Dyes for Antibody Conjugation andACS omega · 2023Article
- Enabling the formation of native mAb, Fab' and Fc-conjugates using a bis-disulfide bridging reagent to achieve tunable payload-to-antibody ratios (PARs).Chemical science · 2023Article
- Optimizing Conjugation Chemistry, Antibody Conjugation Site, and Surface Density in Antibody-Nanogel Conjugates (ANCs) for Cell-Specific Drug Delivery.Bioconjugate chemistry · 2023Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 3 countries.
Funding
Abstract
Due to their exquisite cysteine-selectivity, excellent stability, and ability to functionally rebridge disulfide bonds, dibromopyridazinediones are emerging as an exciting new class of bioconjugation reagents, particularly in the field of antibody conjugation. Despite this, relatively little work has been performed on the optimisation of their synthesis and subsequent reaction with immunoglobulins. Herein we present a novel synthetic route towards functionalised dibromopyridazinediones, proceeding via an isolatable dibromopyridazinedione-NHS ester. Reaction of this activated intermediate with a variety of amines produces functional dibromopyridazinediones in good to excellent yields. The disulfide rebridging capacity of these reagents was optimised on the clinically relevant IgG1 trastuzumab, resulting in a general method which allows for the generation of site-selectively modified native trastuzumab with over 90% homogeneity (no disulfide scrambling) without the need for protein engineering or enzymatic conjugation.
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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.