*MICHEL BOUVIER

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

*IGOR STAGLJAR

Acting on membrane protein-protein interactions: Mammalian Membrane Two Hybrid (MaMTH) as an Innovative Technology for Drug Discovery Against Protein- Protein Interactions

Challenge: Membrane proteins, representing approximately one-third of all proteins in a cell, interact with each other and are responsible for a variety of processes, making them attractive therapeutic targets for many diseases such as hypertension, diabetes, neurological disorders and various cancers. In fact, membrane proteins represent 60% of all clinical drug targets, however, they are still extremely difficult to study … Read More

*MICHEL BOUVIER

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

*CRAIG SIMMONS

Artificial Liver for Safer and more Effective Drugs: 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

*GRACIELA PINEYRO

Monitoring Conformational Changes in Channel Proteins: A Novel Approach for Rapid Screening of Ion Channel Hits

Challenge: Ion channels are involved in numerous physiological functions, and as drug targets have been implicated in a wide range of pathological conditions. However, despite considerable effort, channel-targeted drug discovery has been hampered by the absence of adequate tools to functionally screen molecules that can modulate channel activity. Solution: The researchers have developed an innovative approach to identify compounds that … Read More

ROBERT BATEY

Unlocking a class of challenging drug targets using a next generation screening and lead development platform technology

  Competition: EXPLORE Program 2015 Funding: $300,000 / 2 years Beginning: April 2016 Protein-protein interactions (PPIs) play a crucial role in nearly all cellular processes. Protein complexes have been implicated in many debilitating human diseases, from cancer to viral infections. PPIs generally contain broad, shallow, and relatively featureless binding sites, hence they have historically been perceived as ‘undruggable’ targets in … Read More