ArticleInternational journal of molecular sciences2017
A Versatile Chemo-Enzymatic Conjugation Approach Yields Homogeneous and Highly Potent Antibody-Drug Conjugates.
Article in International journal of molecular sciences, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- The evolving landscape of enzymatic technologies for precision synthesis of antibody-drug conjugates.Antibody therapeutics · 2026Review
- CD20-directed antibody-drug conjugates in non-hodgkin lymphoma: translating preclinical promise into clinical reality.Journal of hematology & oncology · 2026Review
- A review of conjugation technologies for antibody drug conjugates.Antibody therapeutics · 2025Review
- Optimized Production of Fc Fusion Proteins by Sortase Enzymatic Ligation.Industrial & engineering chemistry research · 2021Article
- Facile Generation of Potent Bispecific Fab via Sortase A and Click Chemistry for Cancer Immunotherapy.Cancers · 2021Article
- Antibody-drug conjugates for the treatment of lymphoma: clinical advances and latest progress.Journal of hematology & oncology · 2021Review
- Toward Homogenous Antibody Drug Conjugates Using Enzyme-Based Conjugation Approaches.Pharmaceuticals (Basel, Switzerland) · 2021Review
- TCR-mimic antibody-drug conjugates targeting intracellular tumor-specific mutant antigen KRAS G12V mutation.Asian journal of pharmaceutical sciences · 2020Article
- Click Chemistry Conjugations.Methods in molecular biology (Clifton, N.J.) · 2020Article
- The Antitumor Activity of TCR-Mimic Antibody-Drug Conjugates (TCRm-ADCs) Targeting the Intracellular Wilms Tumor 1 (WT1) Oncoprotein.International journal of molecular sciences · 2019Article
- Broadening the scope of sortagging.RSC advances · 2019Review
Corrections and comments
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The therapeutic efficacy of antibodies can be successfully improved through targeted delivery of potent cytotoxic drugs in the form of antibody-drug conjugates. However, conventional conjugation strategies lead to heterogeneous conjugates with undefined stoichiometry and sites, even with considerable batch-to-batch variability. In this study, we have developed a chemo-enzymatic strategy by equipping the C-terminus of anti-CD20 ofatumumab with a click handle using Sortase A, followed by ligation of the payload based on a strain-promoted azide-alkyne cycloaddition to produce homogeneous conjugates. The resulting antibody-drug conjugates fully retained their antigen binding capability and proved to be internalized and trafficked to the lysosome, which released the payload with a favorable efficacy in vitro and in vivo. Thus, this reported method is a versatile tool with maximum flexibility for development of antibody-drug conjugates and protein modification.
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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.