Development of robust industrial protocols for the synthesis of peptide derivatives

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Peptide based therapeutics make up a significant portion of the current armory we have against diseases andillnesses. However, unmodified peptides are not suitable as drugs because of their poor chemical and physicalstability, short circulating plasma half-life, and limited oral bioavailability. To circumvent these disadvantages,a significant amount of effort has been put forward to chemically modify unprotected peptides. Thesemodifications add valuable characteristics such as enhanced cell permeability, increased stability to proteases,increased oral bioavailability, extended lifetime in the blood serum, improved specificity and conformationalrigidity to augment potency. Currently, robust rapid modification of unprotected peptide protocols are limitedto solely academic laboratory use. Industry-scale syntheses of peptide derivatives are not common. With thegrowing need in peptide-based therapeutics, TC Scientific Inc. aims to develop a peptide modification protocolthat is suitable for industry level production. The Derda Lab at the University of Alberta has extensiveexperience in robust rapid modification of unprotected peptides in water using readily available modifiers. Bycombining the academic advantage of the Derda group and the industry experience from TC scientific Inc., thegoal of this proposal is to develop robust industrial peptide modification protocols.