Issue 38, 2011

A novel pathway for maytansinoid release from thioether linked antibody–drug conjugates (ADCs) under oxidative conditions

Abstract

A novel pathway for ex vivo maytansinoid release from thioether linked antibody maytansinoid conjugates (AMCs) upon incubation in human plasma has been identified. A thioether succinimide-linked AMC can undergo chemical oxidation followed by sulfoxide elimination under mild aqueous conditions (pH 5.5–7.5, 37 °C). Oxidized thioether-linked AMCs exhibit high, target-specific cytotoxicity toward cancer cells.

Graphical abstract: A novel pathway for maytansinoid release from thioether linked antibody–drug conjugates (ADCs) under oxidative conditions

Supplementary files

Article information

Article type
Communication
Submitted
11 Jul 2011
Accepted
10 Aug 2011
First published
26 Aug 2011

Chem. Commun., 2011,47, 10752-10754

A novel pathway for maytansinoid release from thioether linked antibody–drug conjugates (ADCs) under oxidative conditions

N. Fishkin, E. K. Maloney, R. V. J. Chari and R. Singh, Chem. Commun., 2011, 47, 10752 DOI: 10.1039/C1CC14164C

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