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Lin, Xi; Li, Mingyue; Wang, Niandong; Wu, Yiran; Luo, Zhipu; Guo, Shimeng; Han, Gye-Won; Li, Shaobai; Yue, Yang; Wei, Xiaohu; Xie, Xin; Chen, Yong; Zhao, Suwen; Wu, Jian; Lei, Ming; Xu, Fei
Nature (London), 03/2020, Letnik: 579, Številka: 7797Journal Article
GPR52 is a class-A orphan G-protein-coupled receptor that is highly expressed in the brain and represents a promising therapeutic target for the treatment of Huntington's disease and several psychiatric disorders . Pathological malfunction of GPR52 signalling occurs primarily through the heterotrimeric G protein , but it is unclear how GPR52 and G couple for signal transduction and whether a native ligand or other activating input is required. Here we present the high-resolution structures of human GPR52 in three states: a ligand-free state, a G -coupled self-activation state and a potential allosteric ligand-bound state. Together, our structures reveal that extracellular loop 2 occupies the orthosteric binding pocket and operates as a built-in agonist, conferring an intrinsically high level of basal activity to GPR52 . A fully active state is achieved when G is coupled to GPR52 in the absence of an external agonist. The receptor also features a side pocket for ligand binding. These insights into the structure and function of GPR52 could improve our understanding of other self-activated GPCRs, enable the identification of endogenous and tool ligands, and guide drug discovery efforts that target GPR52.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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in: SICRIS
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