Dr. Giguère’s long-standing research focus is in the field of G protein-coupled receptor (GPCR) signaling and pharmacology. He has extensive experience in structure-based drug discovery and drug screening, and his research uses pharmacological, biochemical and structural approaches to uncover a new level of understanding of GPCR molecular recognition as well as pharmacological and functional selectivity, with the ultimate goal to generate better therapeutics with reduced side-effects. He has made key discoveries that provided new ways to pharmacologically manipulate GPCR functions and signaling outcomes, and which have increased our understanding of GPCR activation and regulation, paving the way to design better therapeutics with fewer side effects (Nature 2014, Neuron 2015). Dr. Giguère was first introduced to GPCRs during his Ph.D. studies under the supervision of Dr. Jean-Luc Parent at the University of Sherbrooke.

            Dr. Giguère was then recruited to the laboratory of Dr. David Siderovski at the University of North Carolina at Chapel Hill (UNC-CH), where he carried out his postdoctoral studies. As a postdoctoral fellow, he discovered and characterized a novel regulator of chemokine receptor signaling (Mol Immunol. 2012), GPSM3, which was found to have key role in disease sequelae of rheumatoid arthritis (RA) through its restricted expression in monocytes – a key inflammatory cell-type central to many inflammatory diseases.

           Then, Dr. Giguère joined the laboratory of Dr. Bryan L. Roth, in the Department of Pharmacology of UNC-CH. Dr. Roth is an internationally recognized leader in GPCR signaling and drug discovery. During his time in the Roth lab, Dr. Giguère acquired extensive expertise in drug discovery, molecular pharmacology and structural biology. He made the seminal discovery that the presence of a sodium ion in a conserved cavity within the delta-opioid receptor (δ-OR) selectively modulates arrestin recruitment at the receptor. This work has profound implications on our understanding of how sodium regulates opioid receptor signaling, as well as other GPCRs. It opened the door to the generation of pharmacologically distinct therapeutics which act through the allosteric modulation of this site. His works were published as a Full Article in Nature (2014) and was featured in Science Signaling. The impact of this work has been widely recognized, with highlights as a 2014: Signaling Breakthroughs of the Year (Sci. Signal., 2015), by F1000Research, as well as by more than 50 national and international news outlets.

             Dr. Giguère’s scientific path has been through some of the best laboratories in the world in the field of GPCRs, and this training has positioned him as one of the top young leaders in the field for structure/function guided pharmacological developments for GPCR targeting. This has not only been recognized through top tier publications, press coverage, and invitation to international meetings, but also through the development of long lasting collaborations with world experts in receptor modeling and medicinal chemistry. With the support of a Tier 2 Canadian Research Chair in molecular pharmacology and drug discovery and a Canada Foundation of Innovation, Dr. Giguère has acquired state of the art equipment and his research is fully devoted to GPCR R&D.