Nature, Published online: 05 November 2025; doi:10.1038/s41586-025-09677-6
Structures of GDP-bound MOR–Gi conformational states combined with pharmacological assays show an inverse correlation between ligand efficacy and GDP affinity, where agonists decrease GDP affinity, promoting GTP exchange, and antagonists increase GDP affinity, dampening activation, thus providing structural and mechanistic insights into G protein activation.
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