Synthesis of N-methylated peptides: on-resin methylation and microwave-assisted couplings

Renée Roodbeen, Knud Jørgen Jensen

4 Citations (Scopus)

Abstract

N-Methylation may positively influence the pharmacokinetic properties of peptides by improving oral availability and in vivo half-life. Additionally, target affinity and specificity may be improved. Here, we describe the solid-phase N-methylation of peptides using direct alkylation. This method allows a rapid N-methyl scan of synthetic, bioactive peptides. Additionally, a microwave-enhanced method for the difficult coupling onto the methylated N terminus is provided.

Original languageEnglish
Title of host publicationPeptide synthesis and applications
EditorsKnud J. Jensen, Pernille T. Shelton, Søren L. Pedersen
Number of pages9
PublisherHumana Press
Publication date2013
Pages141-149
ISBN (Print)978-1-62703-543-9
ISBN (Electronic)978-1-62703-544-6
DOIs
Publication statusPublished - 2013
SeriesMethods in Molecular Biology
Volume1047
ISSN1064-3745

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