ArticleCell chemical biology2019
Site-Selective Antibody Functionalization via Orthogonally Reactive Arginine and Lysine Residues.
Article in Cell chemical biology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
19 citing papers in PubMed, 14 citations in OpenAlex.
- DVD-IgG1 antibody-drug conjugates: Expanding the landscape of targeted cancer therapy.Current opinion in chemical biology · 2026Review
- 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
- Predictable Modulation of a Spontaneous Post-translational Modification in Living Cells.Angewandte Chemie (International ed. in English) · 2025Article
- The Evolving Landscape of Antibody-Drug Conjugates: In Depth Analysis of Recent Research Progress.Bioconjugate chemistry · 2023Review
- 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
- Chemical Conjugation to Less Targeted Proteinogenic Amino Acids.Chembiochem : a European journal of chemical biology · 2022Review
- Reactive Oxygen Species (ROS) Activated Liposomal Cell Delivery using a Boronate-Caged Guanidine Lipid.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
- Recent developments in chemical conjugation strategies targeting native amino acids in proteins and their applications in antibody-drug conjugates.Chemical science · 2021Review
- A new immunochemical strategy for triple-negative breast cancer therapy.Scientific reports · 2021Article
- Diethynyl Phosphinates for Cysteine-Selective Protein Labeling and Disulfide Rebridging.Angewandte Chemie (International ed. in English) · 2021Article
- An Engineered Arginine Residue of Unusual pH-Sensitive Reactivity Facilitates Site-Selective Antibody Conjugation.Biochemistry · 2021Article
- Characterization of TnmH as anJournal of medicinal chemistry · 2020Article
- Generation and validation of structurally defined antibody-siRNA conjugates.Nucleic acids research · 2020Article
- Site-Specific Antibody-Drug Conjugates in Triple Variable Domain Fab Format.Biomolecules · 2020Article
- Site-Specific Lysine Arylation as an Alternative Bioconjugation Strategy for Chemically Programmed Antibodies and Antibody-Drug Conjugates.Bioconjugate chemistry · 2019Article
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8 authors at 1 institution in 1 country.
Funding
Abstract
Homogeneous antibody-drug conjugates (ADCs) that use a highly reactive buried lysine (Lys) residue embedded in a dual variable domain (DVD)-IgG1 format can be assembled with high precision and efficiency under mild conditions. Here we show that replacing the Lys with an arginine (Arg) residue affords an orthogonal ADC assembly that is site-selective and stable. X-ray crystallography confirmed the location of the reactive Arg residue at the bottom of a deep pocket. As the Lys-to-Arg mutation is confined to a single residue in the heavy chain of the DVD-IgG1, heterodimeric assemblies that combine a buried Lys in one arm, a buried Arg in the other arm, and identical light chains, are readily assembled. Furthermore, the orthogonal conjugation chemistry enables the loading of heterodimeric DVD-IgG1s with two different cargos in a one-pot reaction and thus affords a convenient platform for dual-warhead ADCs and other multifaceted antibody conjugates.
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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.