Nobel Laureate Dr. Robert J. Lefkowitz presented his latest research towards developing pharmacological applications for G-protein-coupled receptors (GCPRs) at the University of Montreal Hospital Research Centre (CRCHUM) today. "Dr. Lefkowitz work has revolutionized pharmacological research, since nearly half of all current drugs target these receptors. A better understanding of GPCRs is helping to create more effective and safer drugs, and today we have had the opportunity to discover the practical implications of his scientific breakthrough for our patients," explained Dr. Vincent Poitout, researcher and Director of the CRCHUM. The presentation "Seven-transmembrane receptors" was part of the 6th Journée scientifique du CRCHUM symposium, of which Dr. Lefkowitz was the guest of honour.
G-protein-coupled receptors (GPCRs) are the sensors of our cells. Located on the surface of the cells of all mammals, they act as kind of communication antennae. GPCRs play a role in smell, taste, vision, and the action of hormones and drugs. Dr. Lefkowitz, who is a Professor of Medicine and Biochemistry at Duke University in North Carolina and the Howard Hughes Medical Institute in Chevy Chase, Maryland, and his colleague Dr. Brian Kobilka, Professor of Medicine and Molecular and Cellular Physiology, showed that all GPCRs share the same structure.
A bit like keys in locks, hormones, amino acids, and even photons bind to specific G-receptors on the surface of cells. Simply inserting the key in the appropriate lock causes a conformational change in the G-protein and triggers a cascade of signals within the cell resulting in an appropriate cellular response. Recent studies have shown that defects in these receptors are involved in pathologies as varied as type 2 diabetes, obesity, baldness, and adrenocortical tumors. The research presented at the conference today by Lefkowitz and the other participants looked specifically at these receptors and their applications in developing new therapeutic targets.