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G protein-coupled receptors (GPCRs) represent the largest and most diverse protein family of membrane proteins. They comprise seven membrane-spanning domains, which allows for immense structural and functional diversity, and mediate a multitude of biological processes upon activation by various extracellular signals. Given their extensive involvement in numerous physiological functions, GPCRs are implicated in an array of human pathologies. As a result of their diversity, location within the plasma membrane, and druggability, GPCRs are generally regarded as superb drug targets, and drugs affecting these receptors represent the single largest drug class currently on the market. Deeper understanding of the role of GPCRs in disease will help to progress rational drug design. Exploration of the role of these receptors in disease and therapies can be facilitated by increasingly available methods such as CRISPR-Cas 9 gene editing, NMR, single-molecular fluorescence, artificial intelligence.
This Collection presents research that deepen our understanding of the biology and structure of GPCRs, their involvement in physiology and pathology, and also work that further develops GPCRs as therapeutic targets.