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.

SUBMITTER: Walther R 

PROVIDER: S-EPMC11223184 | biostudies-literature | 2024 Jul

REPOSITORIES: biostudies-literature