Título: Angewandte Chemie - International EditionImportada do Authenticus Pesquisar Publicações da Revista

Vol. 58

Páginas: 6640-6644

ISSN: 1433-7851

Editora: Wiley-Blackwell

ISI Web of Knowledge - 8 Citações

Scopus - 10 Citações

ID Authenticus: P-00V-3S1

DOI: 10.1002/anie.201901405

Abstract (EN): Quaternized vinyl- and alkynyl-pyridine reagents were shown to react in an ultrafast and selective manner with several cysteine-tagged proteins at near-stoichiometric quantities. We have demonstrated that this method can effectively create a homogenous antibody-drug conjugate that features a precise drug-to-antibody ratio of 2, which was stable in human plasma and retained its specificity towards Her2+ cells. Finally, the developed warhead introduces a +1 charge to the overall net charge of the protein, which enabled us to show that the electrophoretic mobility of the protein may be tuned through the simple attachment of a quaternized vinyl pyridinium reagent at the cysteine residues. We anticipate the generalized use of quaternized vinyl- and alkynyl-pyridine reagents not only for bioconjugation, but also as warheads for covalent inhibition and as tools to profile cysteine reactivity.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 5