GPCRs and other receptor-based screening platforms

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 […]

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VIPER, the lentiviral IPPER platform for drug discovery in trafficking diseases. IPPER-accelerated development of pharmacological correctors for cystic fibrosis

Challenge: Drug discovery by high-throughput screening of candidate compounds faces challenges and needs the development and validation of specific platforms. An example of complex diseases that would benefit from such platforms is cystic fibrosis, a lung disease caused by genetics and aggravated by air pollution. An immediate response of bronchial epithelial cells to pollution is the downregulation of

VIPER, the lentiviral IPPER platform for drug discovery in trafficking diseases. IPPER-accelerated development of pharmacological correctors for cystic fibrosis Read More »

Development of pharmacological correctors for Alpha-1 antitrypsin deficiency (ATD) using VIPER

Challenge: Drug discovery by high-throughput screening of candidate compounds is usually limited in efficacy as their functional potential is not assessed in relevant biological systems, such as patient cells, during this first selection; new platforms are needed that enable functional testing within specific biological systems. An example of protein trafficking that would benefit from such platforms is Alpha-1 antitrypsin deficiency (ATD), an orphan disease, whose behaviour in the endoplasmic reticulum (ER) is complex, rendering the design of therapeutic candidates difficult. Solution:

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A 150-plex affinity proteomics platform for high throughput and high content phenotypic cell screening

Challenge: Proteins are the main effectors of cell activity and cardinal indicators of cell phenotype and response to stimuli such as drugs.  Whereas sequencing technologies currently allow for broad and efficient genomic and transcriptomic profiling, multiplexed protein detection technologies are either prohibitively slow and expensive, limited in scope due to reagent cross-reactivity, or both.  Critically,

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FlAsH-Walk Mapping: An Innovative Step-by-Step Approach to G Protein-Coupled Receptor Conformation Cartography

Challenge: G protein-coupled receptors (GPCRs) are the largest target class for approved drugs. Identification of new drug candidates has relied exclusively on high-throughput assays which track binding properties and are limited to a restricted number of signaling pathways. GPCRs are highly dynamic proteins that undergo numerous conformational changes upon receptor association with ligands and related

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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

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Using Patient’s Blood to Develop a Sensory Neuron-Based Platform to Treat Chemotherapy-Induced Peripheral Neuropathy

Challenge: The sensory neuron damage referred as “Chemotherapy-Induced Peripheral Neuropathy” (CIPN) affects 30-40% of cancer patients in Canada. Sensory neurons transmit information from the brain to every other part of the body allowing movement and awareness of our environment. The deterioration of these cells from chemotherapy causes severe pain often leading to the interruption of

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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

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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

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Novel Methods to Evaluate Cardiac Activity of Pharmaceuticals: Identifying New Therapies and Predicting Cardiac Toxicity

Challenge: Current therapies for heart failure primarily relieve symptoms, but most fail to correct organ dysfunction. New therapies, to target and improve cardiomyocyte function, are challenging to develop because of the complex functions of the heart muscle and the difficulty in modeling heart cell behavior. The same problems underlie the difficulty in assessing the cardiotoxic

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