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Site-selective peptide functionalisation mediated via vinyl-triazine linchpins

. 2024 Jan 16 ; 60 (6) : 706-709. [epub] 20240116

Language English Country England, Great Britain Media electronic

Document type Journal Article

Herein we introduce 3-vinyl-1,2,4-triazines derivatives as dual-reactive linkers that exhibit selectivity towards cysteine and specific strained alkynes, enabling conjugate addition and inverse electron-demand Diels-Alder (IEDDA) reactions. This approach facilitates site-selective bioconjugation of biologically relevant peptides, followed by rapid and highly selective reactions with bicyclononyne (BCN) reagents.

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