Issue 65, 2023

Disulfide re-bridging reagents for single-payload antibody-drug conjugates

Abstract

Numerous antibody-drug conjugate (ADC) linker technologies exist for the synthesis of ADCs with drug-to-antibody ratios (DARs) being an even integer (typically 2, 4 or 8). However, ADCs with odd-integer DARs are significantly harder to synthesise. Here, we report the synthesis of ADCs loaded with a single warhead, using TetraDVP linkers which simultaneously re-bridge all four interchain disulfides of an IgG1 antibody.

Graphical abstract: Disulfide re-bridging reagents for single-payload antibody-drug conjugates

Supplementary files

Article information

Article type
Communication
Submitted
21 Jun 2023
Accepted
17 Jul 2023
First published
18 Jul 2023
This article is Open Access
Creative Commons BY license

Chem. Commun., 2023,59, 9868-9871

Disulfide re-bridging reagents for single-payload antibody-drug conjugates

T. A. King, S. J. Walsh, M. Kapun, T. Wharton, S. Krajcovicova, M. S. Glossop and D. R. Spring, Chem. Commun., 2023, 59, 9868 DOI: 10.1039/D3CC02980H

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