Issue 55, 2024

Tuneable thiol exchange linkers for traceless drug release applications in prodrugs and ADCs

Abstract

We describe a versatile and tuneable thiol responsive linker system using thiovinylketones, which relies on the conjugate addition–elimination mechanism of Michael acceptors for the traceless release of therapeutics. In a proof-of-principle study, we translate our findings to exhibit potent thiol-cleavable antibiotic prodrugs and antibody–drug conjugates.

Graphical abstract: Tuneable thiol exchange linkers for traceless drug release applications in prodrugs and ADCs

Supplementary files

Article information

Article type
Communication
Submitted
06 Apr 2024
Accepted
11 Jun 2024
First published
12 Jun 2024
This article is Open Access
Creative Commons BY license

Chem. Commun., 2024,60, 7025-7028

Tuneable thiol exchange linkers for traceless drug release applications in prodrugs and ADCs

R. Walther, M. Park, N. Ashman, M. Welch, J. S. Carroll and D. R. Spring, Chem. Commun., 2024, 60, 7025 DOI: 10.1039/D4CC01558D

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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