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This lecture covers the fundamentals of G protein-coupled receptors (GPCRs), focusing on their structure, signalling pathways, and diverse functions. It starts with an introduction to GPCRs and their classical signalling scheme, followed by a historical overview of key discoveries in GPCR research. The lecture then delves into the structural biology of GPCRs, including recent advancements in GPCR structures and small molecule binders. It also discusses the role of GPCRs as drug targets, highlighting their significance in the pharmaceutical industry. The lecture concludes with a detailed exploration of GPCR signalling mechanisms, such as ligand-induced GDP-GTP exchange and GTP hydrolysis, as well as the regulation of G-protein signalling by RGS proteins.