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Tuneable thiol exchange linkers for traceless drug release applications in prodrugs and ADCs.
Walther, Raoul; Park, Mahri; Ashman, Nicola; Welch, Martin; Carroll, Jason S; Spring, David R.
Afiliação
  • Walther R; Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge, UK.
  • Park M; Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge, UK.
  • Ashman N; Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge, UK.
  • Welch M; Department of Biochemistry, University of Cambridge, CB2 1QW Cambridge, UK.
  • Carroll JS; Cancer Research UK Cambridge Institute, Robinson Way, CB2 0RE Cambridge, UK.
  • Spring DR; Yusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, CB2 1EW Cambridge, UK.
Chem Commun (Camb) ; 60(55): 7025-7028, 2024 Jul 04.
Article em En | MEDLINE | ID: mdl-38888299
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Sulfidrila / Pró-Fármacos / Imunoconjugados / Liberação Controlada de Fármacos Limite: Humans Idioma: En Ano de publicação: 2024 Tipo de documento: Article
Texto completo
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XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Compostos de Sulfidrila / Pró-Fármacos / Imunoconjugados / Liberação Controlada de Fármacos Limite: Humans Idioma: En Ano de publicação: 2024 Tipo de documento: Article