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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



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


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


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


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


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


A Novel Platform Combining Transcriptomics and Interaction Proteomics to Better Define Personalized Medicine in Cancer

Challenge: In the last decade, cancer genomics has shown that not all patient tumours are identical, and conversely that they will not respond similarly to anticancer agents. The key, therefore, is personalized (or precision) medicine whereby specific drugs will be given to a patient carrying a gene that will make their tumours sensitive to such drugs. However, the identification of genes … Read More


Dimer Interference: A novel Approach to Develop Galectin-7-Specific Inhibitors to treat Triple-Negative Breast Cancer

Challenge: Galectins are a family of lectin proteins implicated in tumor progression and immune evasion. When produced in excess by cancer cells, galectins can form homodimers and bind glycans on the surface of T cells. This suppresses the local and systemic immune response in patients, helping tumors to escape immune surveillance and limiting the efficacy of immuno-oncology treatments. To date, … Read More


Circumventing the need for predictive biomarkers in personalized ovarian cancer therapies: empirical chemosensitivity testing using a microfluidics-based multiplex platform

Challenge: Ovarian cancer is a leading cause of cancer death in women. Only a fraction of women diagnosed with ovarian cancer will respond to current therapies. In order to better tailor treatment to each patient, personalized medicine has turned to biomarkers that statistically evaluate the chances of a drug to be effective for a patient. Nevertheless, there is currently no … Read More


Facilitating Anti-Cancer Drug Discovery with Selective Inhibitors to Modulate the Protein Ubiquitination Process

Challenge: Human cells eliminate non-functional proteins using a sophisticated degradation pathway named the ubiquitin proteasome system (UPS), in which UPS enzymes attach a small protein called ubiquitin to damaged target proteins to tag them for degradation. However, abnormalities in protein degradation are frequently observed in many diseases, including cancer where aberrant control of protein degradation can lead to uncontrolled cell … Read More



In-vivo Solid Phase Microextraction Integrated with Mass Spectrometry Platform for Untargeted and Targeted Investigation of the Brain

Challenge: One of the major challenges currently faced by the pharmaceutical industry is the development of alternative approaches that allow the gathering of maximum information using a minimum number of animals. With regard to analytical instruments, mass spectrometers offer increasingly sensitive and quantitative determination of biological molecules. However, collected biological samples, especially tissues, require efficient sample preparation prior to mass … Read More


Catecholamine-Regulated Protein 40 (CRP40) as a New Candidate Biomarker for Early Diagnosis of Parkinson’s Disease

Challenge: Parkinson’s disease (PD) is a progressive neurodegenerative movement disorder afflicting 1 to 2% of the population over 65 years of age and for which there is neither a reliable diagnostic test nor cure. Since catecholamine-regulated protein 40 (CRP40) may be involved in regulation of dopamine in the brain, it represents a potential biomarker for early diagnosis of Parkinson’s disease. … Read More


Automated Zebrafish High Throughput Drug Screening Platform: An Automated Zebrafish High Throughput Technology to Accelerate in vivo Screening of Small Molecules in Disease Models

Challenge: Protein misfolding and aggregation are implicated in diverse neurodegenerative diseases, such as Alzheimer’s, frontotemporal dementia, Parkinson’s, amyotrophic lateral sclerosis (ALS) and other chronic diseases such as diabetes. Currently, only cell-based screening assays have been designed and used in the discovery of new therapeutic molecules. However, these assays are limited in representing disease models because they do not consider the … Read More


Non-Invasive Diagnostic Test Using Electroretinography for Profiling Patients with Schizophrenia and Bipolar Disorders

Challenge: Psychiatric disorders such as schizophrenia, bipolar disorder and major depression affect 25 million of individuals in North America. Early identification of risk factors for people with genetic predispositions remains the most promising avenue for improving the treatments for these diseases. However, there are multiple subgroups of patients within a specific disease whose condition is mediated by different molecular pathologies, … Read More


Innovative Optical Imaging and Bio-Simulation Platforms to Accelerate Central Nervous System Drug Discovery

Challenge: The development of efficient drugs targeting central nervous system (CNS) diseases remains a challenge, especially because of a lack of effective methods for studying processes occurring at the synaptic level. Protein interactions at the synapse are known to be modified under pathological conditions and to induce important changes in cellular function. Despite great advances in imaging, it remains difficult … Read More


Cyto-iGluSnFR: A glutamate biosensor platform for brain diseases

Challenge: Glutamate is the principal excitatory neurotransmitter of the human central nervous system (CNS). Disruption of glutamate homeostasis is a central feature of many neurological diseases, including stroke, glaucoma and Alzheimer’s disease. Glutamate levels in CNS are controlled by glial cells which facilitate its recycling and uptake through Excitatory Amino Acid Transporters (EAATs). Consequently, the EAAT proteins are attractive targets … Read More


Alzheimer’s Disease Mouse Model Characterization: Correlation Between MRI and ex vivo Immunohistochemistry

Challenge: Alzheimer’s disease (AD) is a progressive neurodegenerative disorder affecting elderly people. There is currently no early diagnostic method available and there is no effective treatment. Better characterization of new animal models is therefore essential to enable the discovery of new therapeutics for AD. Solution: To maximize the information obtained from MRI and PET imaging studies of animal models for … Read More


The eye: a window to the brain – Detection of Alzheimer’s Disease in the Prodromal Stage from Non-Invasive Hyperspectral Retinal Images

Challenge: Alzheimer’s disease (AD) affects millions of people worldwide, causing an irreversible and debilitating loss of neuro-cognitive functions, with no cure currently available. At the moment, AD diagnosis can be confirmed post-mortem or through complex in vivo imaging approaches (Positron Emission Tomography or PET scanner) by observing two AD hallmarks in the brain, the deposition of β-amyloid (Aβ) plaques and … Read More


Inducible Mouse Models to Accelerate Drug Development for Parkinson’s Disease and Other Synucleinopathies

Challenge: Parkinson’s disease (PD) is characterized by motor symptoms, cognition, speech, mood, and behaviour disorders. While PD is currently diagnosed based on motor impairment, the non-motor deficits (the prodromal stage) typically precede the motor symptoms by several years. PD is associated with the presence of Lewy bodies and neurites composed of misfolded fibrillar α-synuclein. The recent development of animal models … Read More


Targeting the Right Cells: Human MiniPromoters for Restricted Gene Expression in Specific Cells of the Eyes

Challenge: Diseases of the eye, sometimes leading to blindness represent an enormous burden in terms of human suffering and economic cost. New gene therapies where promoters act as switches to modulate gene expression could offer cures, but such expression is difficult to target to the appropriate diseased cells. Due to their size, complexity and regulation, endogenous promoters can rarely be … Read More


ShARP: Screenable Assays for RNA-Binding Proteins Involved in Brain Disorders

Challenge: Brain disorders such as autism, major depressive disorder and Alzheimer’s disease are among the greatest medical challenges of our era. Many drugs targeting the central nervous system (CNS) have been developed to modulate G-protein coupled receptors, ion channels or transporters, with mitigated success. There remains a shortage of disease-relevant targets that can be harnessed for drug discovery to treat the … Read More



PulmoBind: A New Non-Invasive Marker for the Early Diagnosis of Patients with Pulmonary Hypertension

Challenge: Pulmonary hypertension (PH) is a condition associated with loss of blood vessels in the lungs leading to a gradual increase in shortness of breath and substantial disability and mortality. The development of effective drugs is impeded by the lack of non-invasive tests to detect the disease at an early stage and to follow its progression. Solution: The goal of … Read More


Live Cell Imaging System for Protein-Protein Interactions: Multiplexing Fluorescence Lifetime Imaging: a rapid HCS system to study protein-protein interactions in live cells

Challenge: Studies of intracellular protein-protein interactions (PPI) is emerging as an important drug discovery tool. Since many relevant targets can only be affected by drugs candidates in living cells, specific screening methods are implemented using sophisticated microscopy systems. A way to measure these interactions in cellulo is through the implementation of Förster Resonance Energy Transfer (FRET) combined with fluorescence lifetime … Read More


VLPExpress®: Novel high-throughput discovery platform to accelerate the development of new vaccines based on Virus-Like Particles

Challenge: Despite the enormous benefits that traditional vaccines have brought to human health in the last century, preventable diseases continue to claim millions of lives each year. New vaccine technologies that offer speed and versatility in production would have significant impact. The emergence of technologies based on Virus-Like Particles (VLPs) has paved the way for a new generation of vaccines … Read More


Identification of T Cell Receptor Somatic Mutations Driving Autoimmunity in Human Rheumatoid Arthritis

Challenge: Somatic mutations are de novo non-inherited mutations which can be passed down to other cells through the course of cell division. Their role has been well-established in cancer. However, the presence of somatic mutations in non-malignant disease has never been explored since it is unlikely that a single point mutation would be sufficient to cause disease. Linking somatic mutations … Read More


A novel phage-based screening technology for antiviral

Challenge: Infection with herpes viruses is associated with several immunodeficient human diseases including the development of cancers. Patients receiving organ transplants are particularly sensitive to such infections. These patients are treated with antiviral agents; however, approved drugs are often associated with severe side effects and the development of resistance can compromise therapy. There is thus an urgent need to discover … Read More


New Processes Mimicking the Spray drying technique for the Preparation of Thermally Stable Vaccines

Challenge: The storage and worldwide distribution of vaccines represent complex issues for pharmaceutical companies due to vaccine instability at ambient temperatures. Spray drying is an established industrial processing technology for stabilizing many products as dried powders. Although studies have shown spray drying to be promising for preparing thermally stable vaccines in order to alleviate cold chain requirements, to date, no … Read More


A new platform to Assess Antigen Destruction and Evaluate the Efficacy of Immunotherapies and Vaccines

Challenge: The fight against cancer, infectious diseases and chronic disorders has been significantly advanced because of the development of effective immunotherapies, vaccines and immunomodulatory drugs. New pre-clinical tools to enable this new active field of drug discovery are needed further upstream in the discovery process. More functional and physiologically relevant readouts are necessary to address the lack of pre-clinical immunogenicity … Read More


Innervated, Vascularised and Immunocompetent Human Skin Model for Screening the Sensitization Potential of Chemicals

Challenge: One of the major concerns in the development of a new compound by the chemical, pharmaceutical or cosmetic industries is to assess its ability to induce cutaneous allergic reactions. Indeed, the industry must be able to predict such risk and classify it before commercialization of new molecules. To date, these tests are performed on animals, raising issues of both … Read More



Novel in silico-assisted Platform to Rapidly Enhance Specificity and Affinity of Therapeutic Antibodies Against Their Targets

Challenge: The design of superior biologic therapeutics such as monoclonal antibodies, single-domain antibodies, and engineered proteins requires optimizing their ability to bind to disease targets. Antibodies offer many advantages over small molecules in treating diseases, but the process for generating them is complex, expensive and often requires further steps of affinity maturation to achieve the desired level of potency. Molecular … Read More


Detection of Molecular Interaction Field Similarities for the Rational Drug Design of Multi-Functional Inhibitors

Challenge: Binding promiscuity plays a major role in medicine as promiscuous drug interactions may lead to undesirable cross-reactivity effects. This represents a considerable challenge for the pharmaceutical industry. Drugs act by modulating the function of target proteins. However, additional off-site non-target proteins may also be affected due to similarities between binding sites. This unintentional effect may lead to the serendipitous … Read More


Biomarkers Discovery in Diabetes: New Biomarkers for Measurement of Early Stage Diabetes Disease and for Prediction of Response to Therapy

Challenge: Pancreatic islets play a critical role in diabetes development with about 50% of their function being lost by the time pre-diabetic patients are diagnosed. Levels of pancreatic ß-cells are currently approximated through measurements of blood glucose, C-peptide, and insulin levels. There is therefore an urgent need to develop biomarkers that more accurately monitor the physiological status of pancreatic ß-cells, … Read More



A genetic test to predict diabetic nephropathy in Type 2 diabetes patients

Competition: SynergiQc 2017 Funding: $683,665 / 2 years Beginning: July 2017 Challenge: Type 2 diabetes (T2D) affects 1 in 11 individuals worldwide and leads to severe complications such as diabetic nephropathy (DN) that is present in about 40% of T2D patients. DN progresses from subclinical disease (microalbuminuria) to overt nephropathy, end-stage renal disease requiring dialysis or transplantation. Identifying T2D patients … Read More


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