The research team led by Professor Chung Ka-young of the School of Pharmacy at SKKU revealed the specific process in which the G-Protein Coupled Receptor (GPCR) delivers drug components. The fact that drug components are delivered as a result of the action of GPCR and the structure after the activation of G-protein have already been discovered, but this is the first time that the specific step by step procedure of how the components are delivered to the cells has been identified. G-protein is a protein that cells use to transmit information. When GPCR detects external signals like medicine intake, it combines with the G-protein in cells to open the cell membrane. Such a role of GPCR allows it to be considered as the key to drug development studies. In fact, 25% of the top-200 drugs sold worldwide, including antihistamine drugs that treat allergies, and 40% of all drugs sold in the market, target GPCRs. Thus, there have been many attempts to enhance drug effectiveness using the GPCR’s final binding structure in previous studies, but no attempts have been successful. The research team, instead, focused on GPCR’s sequential changes in structure when it combines with G-protein. As a result, the team successfully observed the structural changes GPCR undergoes when it combines with external signals to induce reactions within cells. The results show that the GPCR structure found in previous studies is the structure after the signal transfer in the cell occurs. What actually matters in the transmission process, however, is the initial structure when the GPCR and G-protein are combined. Specifically, the research divides the transmission process into four stages and concludes that the principles of the second and third stages must be identified in order to enhance the effectiveness of drugs targeting GPCR. The research was published in Cell, a world-class journal in the field of life sciences, this May.
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