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

Renée Roodbeen, Knud Jørgen Jensen

4 Citationer (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.

OriginalsprogEngelsk
TitelPeptide synthesis and applications
RedaktørerKnud J. Jensen, Pernille T. Shelton, Søren L. Pedersen
Antal sider9
ForlagHumana Press
Publikationsdato2013
Sider141-149
ISBN (Trykt)978-1-62703-543-9
ISBN (Elektronisk)978-1-62703-544-6
DOI
StatusUdgivet - 2013
NavnMethods in Molecular Biology
Vol/bind1047
ISSN1064-3745

Emneord

  • Backbone amide linker
  • Handle
  • Peptide
  • Aldehyde
  • Thioester
  • N-Alkyl amide
  • Cyclic peptide
  • Reductive amination

Fingeraftryk

Dyk ned i forskningsemnerne om 'Synthesis of N-methylated peptides: on-resin methylation and microwave-assisted couplings'. Sammen danner de et unikt fingeraftryk.

Citationsformater