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 Université 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 Université de Sherbrooke.
The project has received $1 million in seed funding, largely derived
through The Québec Consortium for Drug Discovery's funding programs, and has attracted interest from four pharmaceutical
The joint provincial project is one of two pilot projects undertaken as
part of the Ontario-Québec Life Sciences Corridor, which was announced at the 2011 Bio International Convention to foster
existing strengths within the two provinces and increase innovation,
productivity, investment and job creation.
"In this project, the strong synergy between the investigators from
Québec and Ontario and the high interest from the pharmaceutical
companies is remarkable," says Max Fehlmann, president and CEO of CQDM.
"We strongly believe that this is the first of many successes to flow
through the Ontario-Québec Life Sciences Corridor."
"Encycle Therapeutics' technology will enhance and accelerate the pace
at which disruptive technologies become available to develop novel
therapeutics," said Raphael Hofstein, president and CEO of MaRS
Innovation. "With a consortium of pharmaceutical companies engaged,
Encycle is well-positioned to leverage its platform into novel
therapeutics for unique targets."
Based in part on Encycle's success, and that of another undisclosed
pilot project, CQDM and MaRS Innovation are partnering with the Ontario Centres of Excellence (OCE) and the Ontario Brain Institute (OBI) to launch the Québec/Ontario CQDM Funding Program, which will
support similar collaborative research projects that seek new tools for
About MaRS Innovation
MaRS Innovation (MI) is the commercialization agent for the exceptional discovery
pipeline from 16 leading Ontario academic institutions. As a
single-entry point to total member research activity of $1B in annual
research and development, MI provides an easy gateway for investors and
licensees who wish to access technology assets in Ontario. Supported by
the Government of Canada through the Networks of Centres of Excellence,
by the Government of Ontario through the Ontario Centres of Excellence,
and by its member institutions, MI is a transformational partnership
that turns research strengths into real commercial opportunities. MI's
portfolio includes the most promising assets and advances
commercialization into global markets through industry partnerships,
licensing and company creation.
About the CQDM
The Québec Consortium for Drug Discovery (CQDM) is a meeting ground for all stakeholders in biopharmaceutical
research. Its principal mission is to fund research projects carried
out in partnership between the academic and hospital milieus in the
public sector and the pharmaceutical and biotechnology industries in
the private sector. An innovative Canadian initiative, the CQDM has a
twofold goal: to accelerate the drug discovery process and to develop
safer and more effective drugs. CQDM is funded through contributions
from Pfizer Canada, AstraZeneca, Merck, Boehringer Ingelheim (Canada)
Ltd., GlaxoSmithKline, Eli Lilly Canada Inc., the Business-Led Networks
of Centres of Excellence (BL-NCE), the Ministère du Développement
Économique, de l'Innovation et de l'Exportation (MDEIE) du Québec and
the Fonds de recherche Québec - Santé (FRQS). For more information: www.cqdm.org.
About the Université de Sherbrooke
The Université de Sherbrooke lies in the heart of one of the three major research poles in the
province of Québec. Recognized for its focus on innovation, Université
de Sherbrooke is a premier partner of higher and regional governments,
promoting social, cultural and economic development. It distinguishes
itself by the strong growth of its research activities over the past
few years, its successes in technology transfer, and its initiatives in
open innovation in collaboration with industrial and social
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