ArticleChemical science2023
Compact hydrophilic electrophiles enable highly efficacious high DAR ADCs with excellent
Article in Chemical science, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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Who cites it
18 citing papers in PubMed, 28 citations in OpenAlex.
- Peptide Nucleic Acid Probes for Pretargeted Affibody-Mediated Delivery of Cytotoxic Payloads to HER2-Positive Carcinoma.Bioconjugate chemistry · 2026Article
- Reflection on "Site-specific PEGylation of proteins by a Staudinger-phosphite reaction": from protein modification to ADCs in the clinic.Chemical science · 2026Article
- DNA-drug conjugates enable logic-gated drug delivery amplified by hybridization chain reactions.Nature biotechnology · 2026Article
- Unsaturated Phosphorus Electrophiles to Probe Protein Tyrosine Phosphatases.Angewandte Chemie (International ed. in English) · 2026Article
- Modular Vinyl Phosphonamidates for Cysteine-Directed Protein Targeting.Journal of the American Chemical Society · 2026Article
- Expanding the payload scope in antibody-drug conjugates by delivery of hydroxy-containing drugs through self-immolative phosphoramidates.Nature communications · 2026Article
- Innovative use of therapeutic antibodies in lung cancer: the current landscape of ADCs and other antibody-based therapies.Frontiers in oncology · 2026Review
- Article
- Near-Infrared Photoimmunotherapy Targeting Esophagogastric Junction Adenocarcinoma With Fully Human Anti-EpCAM Antibody.Cancer science · 2025Article
- TUB-040, a Homogeneous and Hydrophilic NaPi2b-Targeting ADC with Stably Linked Exatecan, Exhibits Long-lasting Antitumor Activity and a Well-Tolerated Safety Profile.Molecular cancer therapeutics · 2025Article
- Orthogonal Site-Specific Dual Bioconjugation of Aryl and Alkyl Thiols.Journal of the American Chemical Society · 2025Article
- Methods for the Generation of Single-Payload Antibody-Drug Conjugates.ChemMedChem · 2025Article
- Effective eradication of acute myeloid leukemia stem cells with FLT3-directed antibody-drug conjugates.Leukemia · 2025Article
- Benzyl Ammonium Carbamates Undergo Two-Step Linker Cleavage and Improve the Properties of Antibody Conjugates.Angewandte Chemie (International ed. in English) · 2025Article
- Anti-tissue factor antibody conjugated with monomethyl auristatin E or deruxtecan in pancreatic cancer models.Cancer science · 2024Article
- NSPs: chromogenic linkers for fast, selective, and irreversible cysteine modification.Chemical science · 2024Article
- Exploring the next generation of antibody-drug conjugates.Nature reviews. Clinical oncology · 2024Review
- Design and Evaluation of Phosphonamidate-Linked Exatecan Constructs for Highly Loaded, Stable, and Efficacious Antibody-Drug Conjugates.Molecular cancer therapeutics · 2024Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The recent success of antibody-drug conjugates (ADC), exemplified by seven new FDA-approvals within three years, has led to increased attention for antibody based targeted therapeutics and fueled efforts to develop new drug-linker technologies for improved next generation ADCs. We present a highly efficient phosphonamidate-based conjugation handle that combines a discrete hydrophilic PEG-substituent, an established linker-payload and a cysteine-selective electrophile in one compact building block. This reactive entity provides homogeneous ADCs with a high drug-to-antibody ratio (DAR) of 8 in a one-pot reduction and alkylation protocol from non-engineered antibodies. The compact branched PEG-architecture introduces hydrophilicity without increasing the distance between antibody and payload, allowing the generation of the first homogeneous DAR 8 ADC from VC-PAB-MMAE without increased
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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.