Therapeutic Production

Scalable Linkage Formation Boosts Protein Engineering

Application

Efficient scalable method for creating peptide or amide linkages and generating peptides, proteins, or glycoproteins.

Key Benefits

Reactions involved are simple, mild, generalizable, and efficient, potentially reducing production costs.
Starting materials needed for this synthesis can also be produced easily and can be generated in situ.

Technical Summary

Manufacturing peptide or protein-based therapeutics can often be challenging and expensive, particularly when compared to small molecule-based therapies. These challenges are even greater for larger peptides and proteins whose manufacturing processes can be quite complex. Despite these challenges, the number of peptide drugs on the market and in development continues to grow.

This invention addresses the challenges to producing peptide therapies by providing a novel synthesis method which is simple, mild, and efficient. Specifically, this method is capable of generating amide, peptide, and glycopeptides linkages. The starting materials used during this method are O-silylthionoesters, which themselves can be easily made from readily available carboxyilic acids. Beyond the production of therapeutics, this method also could be applied to produce quantities of peptides or proteins for research or industrial uses.