Scalable Linkage Formation Boosts Protein Engineering


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.

Developmental Stage

This synthesis method has been used in a laboratory setting for research purposes.

Patent Information

App Type Country Serial No. Patent No. File Date Issued Date Patent Status
Utility (parent) United States 13/280,991 8,921,599 10/25/2011 12/30/2014 Issued
Divisional United States 14/583,850 9,382,193 12/29/2014 7/5/2016 Issued
Tech ID: 10123
Published: 1/7/2011