,A new era for GPCR research: structures, biology anddrug discovery

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Cells in a living organism must communicate with each other through continuously sending and receiving messages.G-protein coupled receptors (GPCRs) are the largest family of communicating molecules at the cell surface.They transmit diverse extracellular signals,ranging from light and small chemical hormones to large peptide and protein hormones,and as such they play crucial roles in numerous physiological and pathological processes.More importantly,GPCRsare the most successful class of drug targets that are relevant to many major diseases,including cancer,heart failure,and inflammatory diseases.Over 50% of currently used drugs are targeted to GPCRs.However,these drugs target only 50-60 GPCRs,leaving the majority of human GPCRs,exceeding 800,unexplored for drug discovery.Given the prominent roles of GPCRs in biology and their successful track records as drug targets,GPCRs have become a hot frontier in basic research of life science and therapeutic discovery of translational medicines.
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