Novel methods of modification and production of peptides & proteins for therapeutic use

Activotec has an extensive ongoing R&D program targeted at developing novel methods for the modification and production of peptides and proteins for therapeutic use. The developed patented methods are available for use in contract research and development programs with pharmaceutical, biotechnology and clinical organisations.

Using an alkoxysilyl moiety as a temporary carboxyl-protecting group, Activotec has been able to offer highly efficient N- to C- directed solid-phase peptide synthesis. The important advantage of the company's novel synthetic strategy is that it allows the preparation of peptide analogues possessing C-terminal modifications (such as esters, thioesters and alcohols) and peptides possessing peptide bond modifications (such as reduced peptide bonds, urea and isosteres) in the solid phase.

N- to C- synthesis has also been utilised to create amino acid analogues in which the carboxyl group is replaced with a diol functionality. This group acts as unique masking group for the sequential ligation of peptide fragments, for the synthesis of artificial proteins, and in the generation of peptide-aldehydes, an important class of peptide/protein therapeutics. Other potential applications for Activotec's novel N- to C- directed solid-phase synthesis methodology include protease resistance, drug delivery tools, vaccine design and peptide-drug conjugates.

In 2005 Activotec was granted a BBSRC research grant of £160,000 over two years. The company is currently developing a novel method for the de novo synthesis of therapeutic proteins to chemical standards of purity not attainable by recombinant means. The new methodology will employ polyethylene glycol as a temporary solubilising agent in the sequential chemical ligation of synthetic peptide fragments to allow the economic synthesis of commercially important therapeutic proteins/peptides (calcitonin, exenatide, beta-amyloid, eotaxin, GM-CSF, and IL-2).

For further information on Activotec contract research and development services for the modification and production of peptides and proteins for therapeutic use please click the above request link.