Site-selective three-component reaction for dual-functionalization of peptides

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A site-selective dual-functionalization of peptides is presented, involving readily available maleimides as well as N-hydroxylamines. The modification proceeds through a three component 1,3-dipolar cycloaddition, forming a stable product. This was exemplified by the one-pot attachment of two molecular imaging moieties to a tumor binding cyclic peptide, and was extended to the conjugation of a DOTA chelator to a 12 kDa protein.
Original languageEnglish
JournalChemical Communications
Issue number19
Pages (from-to)1936-1938
Number of pages3
Publication statusPublished - 2013

ID: 88717747