Fragment-Based Lead Discovery: Bridging the Gap Between Screening and Hit-to-Lead Medchem using NMR Affinity Ranking

Challenge: One of the most promising strategies for discovering our future medications is via fragment-based lead discovery (FBLD). FBLD involves the screening of libraries of small molecules to first identify weak binders, essential to activate or inhibit a target protein involved in a particular disease. These binders are then synthetically matured to larger, more potent inhibitors/leads via medicinal chemistry design … Read More


A platform for in vivo nuclear receptor (NR) drug screening and the discovery of new pathways in metabolic disease and cancer

  Competition: Québec / Ontario Program 2012 Funding: $550,000 / 3 years Beginning: September 2014 Drug discovery is long and expensive, and many drugs that pass through traditional screening fail in development or after approval. Pharmaceutical companies are looking for ways to make the screening process more accurate and cost-effective, thereby enhancing the drug development success rate. We have developed a novel, … Read More


IPPER, the Integrated Platform for the Pharmacology of the Endoplasmic Reticulum and protein trafficking diseases

Challenge: Endoplasmic reticulum (ER) stress occurs when the folding of secreted proteins within the ER lumen is disturbed. The unfolded protein response (UPR) comprises several mechanisms. These adaptive responses attempt to overcome ER protein folding disturbances to promote cellular homeostasis and cell survival. ER stress and the UPR are implicated in many diseases such as neurodegenerative and cardiovascular diseases, diabetes … Read More


Measuring cardiac cell contraction to identify new therapies and predict cardiac toxicity

  Competition: EXPLORE Program 2015 Funding: $300,000 / 2 years Beginning: April 2016 Current therapies for heart failure primarily relieve disease symptoms, but most fail to correct the underlying organ dysfunction. New therapies, which are able to target and improve cardiomyocyte function, are challenging to develop, owing significantly to the complex functions of heart muscle and the difficultly in modeling … Read More


New GPCR-Specific Biosensor Technology to Monitor Cellular Events Associated with Drugs Efficacy and Side Effects

Challenge: G protein-coupled receptors (GPCRs) form the largest family of cell surface receptors involved in signal transduction of many hormones and transmitters. It follows that drugs targeting GPCRs represent close to 40% of all drugs on the market today. Recent discoveries regarding their function and mechanism of action help pave the way for the development of more selective therapeutics for … Read More


Mammalian Membrane Two Hybrid (MaMTH), an innovative technology for drug discovery

  Competition: EXPLORE Program 2014 Funding: $300,000 / 2 years Beginning: June 2015 Igor Stagljar and his team have worked over the last 12 years to understand how interactions among a special class of proteins, called membrane proteins, produce either healthy or diseased cells. These proteins, which make up approximately one-third of all proteins in a cell, are responsible for … Read More


Zebrafish HTS platforms for nuclear receptor related drug discovery and pathway elucidation

  Competition: CQDM / CIHR Program 2014 Funding: $1,000,000 / 2 years Beginning: July 2015 Drug discovery is a long and expensive process, and many potential drugs discovered by traditional screening using cells in petri dishes fail in late development or after approval due to unforeseen side effects. Henry Krause’s team has developed a novel drug screening platform that can visualize potential … Read More


Monitoring the Signaling Pathways of G Protein Coupled Receptors in Living Animals to Accelerate Drug Discovery

Challenge: Because they are involved in so many physiological processes, G protein coupled receptors (GPCRs) are engaged by roughly 40% of marketed drugs and remain a prime target for the development of new therapeutics. To test the activity of drug candidates, understanding their action on their target in living animals is essential. However, this goal represents a significant challenge due … Read More


Three-Dimensional Liver Tissue Models for High-Throughput Screening of the Efficacy and Hepatotoxicity of Drugs

Challenge: Poor efficacy and unpredictable toxic effects are leading causes for the removal of drugs from the market. Many drugs act unpredictably in patients because the preclinical studies fail to accurately model human biology. In particular, the liver requires special attention as it is responsible for metabolizing drugs. Thus, improved liver models could identify and eliminate toxic and ineffective drugs … Read More


A screening technology to improve the discovery of function modifying antibodies

  Competition: Quantum Leap 2017 Funding: $1,000,000 / 1 year Beginning: December 2017 Challenge: Antibody (Ab)-based therapeutics are the fastest growing class of drugs, with approximately 60 approved molecules that represent a market of over $80B. To date, the growth of this market has been due to new therapeutics against targets that can be prepared as soluble antigens. Attention is … Read More