Platform for cyclizing peptides promises to increase efficiency of early-stage drug discovery

BOSTON , June 18, 2012 /CNW/ - Encycle Therapeutics, a MaRS Innovation spin-off company, has created a ground-breaking chemistry platform for cyclizing peptides that promises to increase the efficiency of the early-stage drug discovery process.

Peptides have long been sought after as therapeutics due to their high specificity they can hit specific cellular targets, especially complex protein-protein interaction targets implicated in cancer, cardiovascular disease and metabolic disorders.

In their linear form, however, peptides are unstable. When used as drug-delivery agents, they break down before reaching therapeutic targets or fail to permeate cell walls, presenting a long-standing challenge to medicinal chemists.

Encycle's breakthrough chemistry platform stabilizes linear peptides for drug development by cyclizing them. This process has demonstrably increased the drug-like properties of these molecules, increasing their stability in the body and providing a higher degree of cell permeability. The platform adapts to any linear peptide input and has the power to generate libraries of compounds to facilitate drug discovery and development.

This technology, discovered in Professor Andrei Yudin 's chemistry laboratory at the University of Toronto , will be developed with the collaboration of Professor Eric Marsault, specialized in medicinal chemistry at the Institut de Pharmacologie de Sherbrooke of Universit de Sherbrooke. Together, they will demonstrate that Encycle's foundational chemistry technology functions for a wide variety of peptides and that the platform can hit therapeutic targets of interest. Encycle will then be well positioned to pursue discovery-stage relationships with the pharmaceutical partners involved in the project around targets of their choosing.

"It costs over $1 billion to bring a new drug to market under the current high through-put pharmaceutical discovery model," says Yudin, professor of Chemistry at U of T and Encycle Founder. "Instead of randomly searching millions of compounds, Encycle's platform will allow us to design a peptide molecule with small molecule properties, such as stability and cell permeability, while remaining more likely to interact with a targeted therapeutic area. In theory, this approach would save time, money and reduce overhead risk."

"The approach pioneered by Andrei Yudin is remarkable for its efficiency in the synthesis of macrocycles, which are otherwise very difficult to reach and thus difficult to exploit in drug discovery," says Marsault. "This collaboration will unlock the potential of this class and provide much-needed new classes of drug candidates able to mimic the natural structural elements of proteins."

"This innovative project is a successful result of our established commitment towards technology transfer of excellent research and partnering with the private and public sectors," says Jacques Beauvais , vice-rector of research at the Universit de Sherbrooke.

The project has received $1 million in seed funding, largely derived through The Qubec Consortium for Drug Discovery's funding programs, and has attracted interest from four pharmaceutical companies.

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Encycle Therapeutics Launches Ground-Breaking Chemistry Platform