Room: Roger Guindon Hall, Room 4212 (office), 4210 (lab)
Office: 613-562-5800 ext. 8402
B.Sc., University of Sherbrooke (1998)
Ph.D., University of Sherbrooke (2007)
Postdoctoral Fellowship, UNC-Chapel Hill (2012)
Substances addressing the opioid receptor system are widely used pharmaceuticals for treatment of chronic pain and addictive disorders. Given the difficulties associated with opioid therapy (overdose, tolerance, addiction, respiratory depression and constipation) there is a need for safer narcotic analgesics. The delta-opioid receptor (δ-OR), a member of the G protein-coupled receptor (GPCR) opioid family, is well described for its role in pain perception and management. Interestingly, in clinical models, it also showed great potential as anti-depressor and also for the treatment of symptoms associated with spasmodic movements in the Parkinson's disease. However, the clinical use of δ-OR agonists is limited due to the generation of potentially life-threatening side effects (e.g. epileptic-like seizures). Therapeutic targeting of GPCR function has been one of the most successful approaches for drug discovery supported by the fact that nearly 50 % of prescribed therapeutics target GPCRs.
Most recently, Dr. Giguère made the discovery that the presence of a sodium ion in a conserved cavity within the δ-OR selectively modulates arrestin recruitment at the receptor. Importantly, accumulating evidence suggests a prominent role of the arrestin-dependent signaling pathway in triggering most of the deleterious effects observed by targeting the opioid system.
Dr. Giguère's research program seeks to:
- Use pharmacological, biochemical and structural approaches to develop a new level of understanding of opioid receptor molecular recognition, pharmacological and functional selectivity;
- Drug screening and design of novel functionally selective allosteric modulators of the opioid receptors;
- GPCR's enhanced tool box by the development of a novel synthetic biology platform and cell-based assay.
The ultimate objective of his research is to generate distinct therapeutics that will uniquely modify their pharmacology in a medically meaningful way increasing their therapeutic efficacy with reduced harmful side effects.