Thioamide ligations: new technologies for peptide and protein synthesis

Abstract

This project aims to develop novel amide-bond forming reactions for the chemical synthesis of peptides and proteins. New peptide ligation strategies, including an asparagine-based ligation and a residue-independent ligation will be developed that exploit the recent discovery of silver-promoted coupling reactions of thioamides. A novel late-stage, chemo-selective assembly of N-glycosylated asparagine residues in peptides and proteins will also be developed. The outcomes of this research will lead to breakthroughs in synthetic methodologies for the assembly and functionalisation of peptides and proteins, thereby enabling access to a range of homogeneous, post translationally modified proteins ..

Related publications (3)

Site Specific Preparation of N‐ Glycosylated Peptides: Thioamide‐Directed Activation of Aspartate

Ameer B Taresh, Craig A Hutton

2022-10-24

Site Specific Preparation of N-Glycosylated Peptides: Thioamide-Directed Activation of Aspartate

Ameer B Taresh, Craig A Hutton

2022-09-21

A site-specific method for the preparation of N-glycosylated peptides is described. Incorporation of a peptide backbone thioamide ..

Backbone thioamide directed macrocyclisation: lactam stapling of peptides

Ameer B Taresh, Craig A Hutton

2022-01-21

A novel method for lactam stapling of Asp/Lys-containing peptides has been developed that does not require coupling agents. A back..