BRUCE H. MORIMOTO
Executive Director, Applied Translational Medicine, Celerion, Inc., USA

Abstract

Over 115 years have passed since Emil Fischer synthesized glycylglycine, a dipeptide (1), and it has been more than 50 years since Bruce Merrifield’s Nobel Prize winning paper was published on solid-phase synthesis of peptides (2). Progress in developing peptide therapeutics requires continuous innovation in multiple areas, including basic research discoveries, development of novel chemistries, and improvements in manufacturing. This issue contains articles on the recent achievements in peptides through the eyes of several industry leaders.

BIGGER AND MORE
Solid-phase synthesis revolutionized peptide chemistry and allowed for longer peptides to be made (3).  However, to make more complex and biologically active molecules, ligation chemistry enabled peptides to be linked together.   In this issue, Dr Michael Pennington, Peptides International and Daniel Bourgin from Dr Reddy’s write about the need to develop and refine new chemistries to synthesize longer and more complex peptides.  Chemical ligation and “click-chemistry” are some of the methods to join shorter synthetic fragments.
Large scale, commercial peptide synthesis emerged nearly 20 years ago with enfuvirtide also known as Fuzeon™ as explained by Dr Gary Erickson from CBL Biopharma.  This required improvements in scale-up which included a significant chemical engineering effort in developing uniform mixing, rapid transfer of intermediates and solvents, and the optimization of producing the amino acid building blocks (fmoc-amino acids).
In addition to making more peptide, it is critical to develop manufacturing processes that are robust, reproducible and cost-effective. Anders Tsirk and Jon Rasmussen from PolyPeptid ...