ArticleChembiochem : a European journal of chemical biology2025
Site-Specific Modification of Native IgGs with Flexible Drug-Load.
Article in Chembiochem : a European journal of chemical biology, 2025. 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.
- Toward Personalized Theranostics: A Modular PET Platform for Antibody-Based Imaging and Therapy.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Phage-Selected Clickable Gln-Donor Peptide for Lys-Selective Fab Labeling Using Engineered Microbial Transglutaminase.Antibodies (Basel, Switzerland) · 2026Article
- Scope of Microbial Transglutaminase for Site-Specific and Oriented Immobilization of Native Antibodies from Various Host Species.Langmuir : the ACS journal of surfaces and colloids · 2026Article
- Site-specific labelling of native peptides and proteins: chemical and enzymatic strategies.Beilstein journal of organic chemistry · 2026Review
- Antibody-drug conjugates for infectious and neglected tropical diseases: chemical design principles, target biology, and translational challenges.Frontiers in chemistry · 2026Review
- Homogeneous antibody-drug conjugates with dual payloads: potential, methods and considerations.mAbs · 2025Review
- SPARC: A Multipayload ADC Architecture for Programmable Drug Combinations.Bioconjugate chemistry · 2025Article
- Resin-Supported Site-Specific Antibody Conjugation Method Leads to Antibody-Drug Conjugates with Retained Efficacy and Improved Stability.Bioconjugate chemistry · 2025Article
- Broadening the Therapeutic Window of ADCs Using Site-Specific Bioconjugation Showcased by an MMAE-Containing Peptide Linker in a CD79b-Targeting ADC.Molecular cancer therapeutics · 2025Article
- Site-Specific Modification of Native IgGs with Flexible Drug-Load.Chembiochem : a European journal of chemical biology · 2025Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
Homogeneous, site-specifically conjugated antibodies have shown to result in antibody-drug conjugates (ADCs) with improved efficacy and tolerability compared to stochastically conjugated ADCs. However, precisely controlling the drug load as well as attaching multiple payload moieties to the antibody remains challenging. Here, we demonstrate the simple and direct modification of native IgG-antibodies at the residue glutamine 295 (Q295) without the need for any protein engineering with flexible drug-to-antibody ratios of one or multiple payloads. The conjugation is enabled through short, positively charged lysine containing peptides and native, commercially available microbial transglutaminase. In proof-of-concept studies, HER2-targeting ADCs based on trastuzumab were generated with drug-to-antibody ratios (DARs) of 2 and 4 of the same or different payloads using orthogonal conjugation chemistries. Quantitative biodistribution studies performed with
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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.