Journal
BIOCONJUGATE CHEMISTRY
Volume 26, Issue 9, Pages 1863-1867Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.5b00440
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Funding
- SATT Conectus BioReLiable project
- CNRS
- University of Strasbourg
- Region Alsace
- GIS IBiSA
- International Center for Frontier Research in Chemistry (icFRC)
- Institut de Recherche Servier
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Thiols are among the most frequently used functional groups in the field of bio conjugation. 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.
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