ArticleBioconjugate chemistry2019
Site-Specific Lysine Arylation as an Alternative Bioconjugation Strategy for Chemically Programmed Antibodies and Antibody-Drug Conjugates.
Article in Bioconjugate chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 38 citations in OpenAlex.
- DVD-IgG1 antibody-drug conjugates: Expanding the landscape of targeted cancer therapy.Current opinion in chemical biology · 2026Review
- Predictable Modulation of a Spontaneous Post-translational Modification in Living Cells.Angewandte Chemie (International ed. in English) · 2025Article
- A review of conjugation technologies for antibody drug conjugates.Antibody therapeutics · 2025Review
- Application of a Biocatalytic Strategy for the Preparation of Tiancimycin-Based Antibody-Drug Conjugates Revealing Key Insights into Structure-Activity Relationships.Journal of medicinal chemistry · 2023Article
- Leveraging a Dual Variable Domain Immunoglobulin to Create a Site-Specifically Modified Radioimmunoconjugate.Molecular pharmaceutics · 2023Article
- Lysine-Directed Site-Selective Bioconjugation for the Creation of Radioimmunoconjugates.Bioconjugate chemistry · 2022Article
- Calibrating Catalytic DNA Nanostructures for Site-Selective Protein Modification.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
- Sculpting a Uniquely Reactive Cysteine Residue for Site-Specific Antibody Conjugation.Bioconjugate chemistry · 2022Article
- Novel development strategies and challenges for anti-Her2 antibody-drug conjugates.Antibody therapeutics · 2022Review
- Site-selective lysine conjugation methods and applications towards antibody-drug conjugates.Chemical communications (Cambridge, England) · 2021Review
- Chemically Programmable and Switchable CAR-T Therapy.Angewandte Chemie (International ed. in English) · 2020Article
- Pyrocinchonimides Conjugate to Amine Groups on Proteins via Imide Transfer.Bioconjugate chemistry · 2020Article
- Site-Specific Antibody-Drug Conjugates in Triple Variable Domain Fab Format.Biomolecules · 2020Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
By exploiting a uniquely reactive lysine residue (Lys99) for site-specific attachment of small molecules, the humanized catalytic antibody h38C2 has been used as bioconjugation module in the assembly of chemically programmed antibodies and antibody-drug conjugates. Treatment of h38C2 with β-lactam-functionalized small molecules has been previously shown to result in covalent conjugation by selective formation of a stable amide bond with the ε-amino group of the Lys99 residue. Here we report that heteroaryl methylsulfonyl (MS-PODA)-functionalized small molecules represent an alternative bioconjugation strategy through highly efficient, site-specific, and stable arylation of the Lys99 residue. A set of chemically programmed antibodies and antibody-drug conjugates assembled by Lys99 arylation provided proof-of-concept for the therapeutic utility of this alternative bioconjugation strategy. While being equally effective as β-lactam-functionalized ligands for bioconjugation with catalytic antibody h38C2, the MS-PODA moiety offers distinct synthetic advantages, making it highly attractive.
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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.