ArticleAngewandte Chemie (International ed. in English)2017
Orthogonal Cysteine Protection Enables Homogeneous Multi-Drug Antibody-Drug Conjugates.
Article in Angewandte Chemie (International ed. in English), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 70 papers.
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Who cites it
70 citing papers in PubMed, 135 citations in OpenAlex.
- Emerging organoids and organoids-on-chip platforms for translational development of antibody‒drug conjugates and next-generation bioconjugates.Acta pharmaceutica Sinica. B · 2026Review
- Antibody-Drug Conjugates and Peptide-Drug Conjugates: Current Understandings and Future Perspectives.MedComm · 2026Review
- From Unmet Medical Need to Drug Candidate: A Translational Therapeutic Development Roadmap Illustrated by Dual-Payload Antibody-Drug Conjugates.Biomolecules · 2026Review
- Orthogonal Conjugation via Endoglycosidase and Microbial Transglutaminase Enables Efficient Synthesis of Dual-Payload Antibody-Drug Conjugates.ACS chemical biology · 2026Article
- Advancements in Dual-Load Antibody-Drug Conjugates and Challenges with Quality Analysis.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Scalable Flow Synthesis of Genetically Encodable Tetrazine Amino Acids.Organic process research & development · 2026Article
- Drug resistance to antibody-drug conjugates: mechanisms, challenges, and perspectives.Cancer biology & medicine · 2026Review
- Antibody-Drug Conjugates in Gynecologic Oncology: Advances, Challenges, and Future Directions.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy · 2026Review
- Homogeneous antibody-drug conjugates with dual payloads: potential, methods and considerations.mAbs · 2025Review
- The evolving landscape of antibody-drug conjugates (ADCs) for treatment of prostate cancer.NPJ precision oncology · 2025Review
- Antibody drugs conjugates in small-cell lung cancer: present-day status and promises.The oncologist · 2025Review
- SPARC: A Multipayload ADC Architecture for Programmable Drug Combinations.Bioconjugate chemistry · 2025Article
- Exploring Experimental and In Silico Approaches for Antibody-Drug Conjugates in Oncology Therapies.Pharmaceuticals (Basel, Switzerland) · 2025Review
- A Dual-Payload Bispecific ADC Improved Potency and Efficacy over Single-Payload Bispecific ADCs.Pharmaceutics · 2025Article
- Homogeneous Dual-Payload Antibody-Drug Conjugates Produced by Combined Distinct Conjugation Strategies.ACS medicinal chemistry letters · 2025Article
- Orthogonal Site-Specific Dual Bioconjugation of Aryl and Alkyl Thiols.Journal of the American Chemical Society · 2025Article
- 177Lu-Labeled Antibody-Drug Conjugate: A Dual-Mechanistic Treatment Modality in Solid Tumors.Molecular cancer therapeutics · 2025Article
- Site-Specific Modification of Native IgGs with Flexible Drug-Load.Chembiochem : a European journal of chemical biology · 2025Article
- Use of Aldehyde-Alkyne-Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers.ACS medicinal chemistry letters · 2025Article
- Site-Specific Quadruple-Functionalised Antibodies.Angewandte Chemie (International ed. in English) · 2025Article
10 more citing papers are in PubMed but not listed here.
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A strategy for the preparation of homogeneous antibody-drug conjugates (ADCs) containing multiple payloads has been developed. This approach utilizes sequential unmasking of cysteine residues with orthogonal protection to enable site-specific conjugation of each drug. In addition, because the approach utilizes conjugation to native antibody cysteine residues, it is widely applicable and enables high drug loading for improved ADC potency. To highlight the benefits of ADC dual drug delivery, this strategy was applied to the preparation of ADCs containing two classes of auristatin drug-linkers that have differing physiochemical properties and exert complementary anti-cancer activities. Dual-auristatin ADCs imparted activity in cell line and xenograft models that are refractory to ADCs comprised of the individual auristatin components. This work presents a facile method for construction of potent dual-drug ADCs and demonstrates how delivery of multiple cytotoxic warheads can lead to improved ADC activities. Lastly, we anticipate that the conditions utilized herein for orthogonal cysteine unmasking are not restricted to ADCs and can be broadly utilized for site-specific 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.