New process makes linear peptides circular

Peptides and proteins have long been an attractive class of drug candidates because of their natural involvement in cellular processes and fewer potential side effects. Dr. Andrei Yudin, Professor, Department of Chemistry, University of Toronto, has developed a new and effective process that makes linear peptides circular, which allows these molecules, called macrocycles, to enter cells more effectively and increase their stability compared to linear peptides. Given their advantageous properties, macrocycles are emerging as a new class of molecules with potential in drug development.

Dr. Yudin and his group's unique ability to efficiently cyclize a broad range of linear peptides provides the opportunity to build a diverse library of macrocycles as possible drug candidates. The Yudin group will build a targeted library of macrocyles and test it for important properties including cell permeability and stability. This compound library will enable researchers and pharmaceutical organizations to screen for biologically active structures against disease-relevant targets, with the ultimate goal of identifying novel therapeutic macrocycles for new drug development. Dr. Yudin will be working closely with pharmaceutical companies to build a library that will meet the needs of industry.

"This work has the potential to help change the face of drug development and expand the options available in the creation of new therapeutics," commented Dr. Mark Poznansky, President and CEO, OGI. "Dr. Yudin and his group are clearly poised to be key influencers in this area."

"We are delighted to receive the investment from OGI as we move closer to commercialization," commented Dr. Yudin. "Our initial endeavour to generate a library of compounds is based around fundamental properties of drug-like compounds. Our method of cyclizing peptides will allow us to grow our inventory of compounds to eventually compete on a global scale in this emerging area of constrained peptides."

In addition to the PBDF funding, the technology has received investment by MaRS Innovation, the commercialization agent for 16 Ontario-based research institutions.

"We see significant appetite in the market for viable discovery platforms for peptide based therapeutics. It is important that Dr. Yudin receives appropriate support at this early stage to maximize the potential of this work," commented Dr. Rafi Hofstein, President and CEO, MaRS Innovation. "At MaRS Innovation, we work with many of the Province's leading researchers to convert great science into commercial opportunities."

U of T's Innovations and Partnerships Office (IPO) is working in collaboration with MI and Dr. Yudin to commercialize his novel platform technology.

"The University of Toronto is grateful to the Ontario Genomics Institute for this investment in our research," said Dr. Peter Lewis, Associate Vice President, Research at U of T and Acting Assistant Vice President, IPO. "The PBDF award will be vital in helping U of T and MaRS Innovation to bring Dr. Yudin's innovation to the marketplace. Just as importantly, OGI's support will assist greatly in enabling Dr. Yudin's work to make a strong and positive impact on global society."

OGI's PBDF program invests in opportunities - based in genomics, proteomics or associated technologies - that fall in the proof-of-principle (validation) phase of research and that have the short-term potential to secure a significant next step towards the marketplace. Previous recipients have included Ontario universities, research institutes and companies.