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X-ray crystallography established the first three-dimensional structure of the ghrelin receptor in an inactive conformation using its high-affinity antagonist Compound 21 and a ghrelin receptor-specific antibody in 2020 (Figure 2A) ( Figure 2 The ghrelin receptor adopts a typical GPCR architecture, featuring seven transmembrane helices (TM17) and a short amphipathic helix8 on the intracellular side