Expanding Native Chemical Ligation Methodology with Synthetic Amino Acid Derivatives

Emma E. Watson, Lara R. Malins, Richard J. Payne

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

3 Citations (Scopus)

Abstract

Native chemical ligation represents one of the most important technologies for accessing peptides and proteins by chemical synthesis, including those bearing modified amino acids. The development of desulfurization chemistry that enables the conversion of cysteine residues to alanine residues has greatly expanded the scope of ligation chemistry, whereby ligation at 15 of the 20 proteinogenic amino acids is now possible through the incorporation of synthetic thiol-derived amino acids into peptide fragments. More recently, this concept has been further expanded to the 21st amino acid selenocysteine, and selenated amino acid derivatives, under a reaction manifold called the diselenide-selenoester ligation. These ligation reactions proceed with enhanced kinetics compared to native chemical ligation and can be used with a chemoselective deselenization step to access a range of protein targets.

Original languageEnglish
Title of host publicationTotal Chemical Synthesis of Proteins
EditorsAshraf Brik, Philip Dawson, Lei Liu
Place of PublicationWeinheim, Germany
PublisherWiley-Academy
Chapter5
Pages119-159
Number of pages41
ISBN (Electronic)9783527823567, 978-3-527-82357-4, 978-3-527-82358-1
ISBN (Print)9783527346608
DOIs
Publication statusPublished - 1 Jan 2021
Externally publishedYes

Keywords

  • amino acid synthesis
  • Deselenization
  • Desulfurization
  • Diselenide-Selenoster Ligation (DSL)
  • ligation junctions
  • ligation methodology
  • modified amino acids
  • Native Chemical Ligation (NCL)
  • native protein
  • orthogonal protection
  • protein total synthesis
  • Selenated amino acids
  • Thiolated amino acids

Cite this