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Article / Jun 20, 2022

Multivalent NHS-activated acrylates for orthogonal site-selective functionalisation of peptides at cysteine residues

  • Mariama Djalo
  • Maria J. S. A. Silva
  • Helio Faustino
  • Sandra N. Pinto
  • Ricardo Mendonca
  • Pedro Gois
Chemical Communications (Cambridge, United Kingdom), june 20, 2022

The site-selective chem. appendage of multiple functionalities on a native peptide backbone is a highly demanding and complex tool of modern chem. biol. Here, novel NHS-activated acrylates were designed to hold various payloads in a single bioconjugation handle that is able to site-selectively and orthogonally target the N-terminal cysteine of peptides.