MAPN: First-in-Class Reagent for Kinetically Resolved Thiol-to-Thiol Conjugation
| Autor: | Alain Van Dorsselaer, Sergii Kolodych, J.-Y. Bonnefoy, Sarah Cianférani, Alain Wagner, Jitka Eberova, Zoljargal Baatarkhuu, Johann Stojko, Oleksandr Koniev |
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| Rok vydání: | 2015 |
| Předmět: |
Immunoconjugates
Biomedical Engineering Pharmaceutical Science Bioengineering Conjugated system Mertansine Maleimides chemistry.chemical_compound Cell Line Tumor Humans Organic chemistry Sulfhydryl Compounds Maleimide Pharmacology chemistry.chemical_classification Bioconjugation Organic Chemistry Kinetics chemistry Alkynes Reagent Thiol Indicators and Reagents Biotechnology Cysteine Conjugate |
| Zdroj: | Bioconjugate Chemistry. 26:1863-1867 |
| ISSN: | 1520-4812 1043-1802 |
| Popis: | Thiols are among the most frequently used functional groups in the field of bioconjugation. While there exists a variety of heterobifunctional reagents that allow for coupling thiols to other functions (e.g., amines, carboxylic acids), there is no specific reagent for creating heteroconjugates using two different thiols. In response to the ever-increasing demand for bioconjugation tools, we have developed p-(maleimide)-phenylpropionitrile (MAPN)-an efficient reagent for kinetically resolved thiol-to-thiol coupling. In a comparative study with its closest commercially available analogue, p-phenylenedimaleimide, MAPN has shown substantial advantages for the preparation of thiol-thiol heteroconjugates. Namely, an antibody-drug conjugate (ADC) with mertansine (DM1), conjugated to the cysteine residues of Trastuzumab, was prepared for the first time. |
| Databáze: | OpenAIRE |
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