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• W2791091229 abstract "Abstract 5-hydroxytryptamine (5-HT, also known as serotonin) regulates many physiological processes through the 5-HT receptor family. Here we report the crystal structure of 5-HT 1B subtype receptor (5-HT 1B R) bound to the psychotropic serotonin receptor inverse agonist methiothepin (MT). Crystallization was facilitated by replacing ICL3 with a novel optimized variant of BRIL (OB1) that enhances the formation of intermolecular polar interactions, making OB1 a potential useful tool for structural studies of membrane proteins. Unlike the agonist ergotamine (ERG), MT occupies only the conserved orthosteric binding pocket, explaining the wide spectrum effect of MT on serotonin receptors. Compared with ERG, MT shifts toward TM6 and sterically pushes residues W327 6.48 , F330 6.50 and F331 6.51 from inside the orthosteric binding pocket, leading to an outward movement of the extracellular end and a corresponding inward shift of the intracellular end of TM6, a feature shared by other reported inactive G protein-coupled receptor (GPCR) structures. Together with the previous agonist-bound serotonin receptor structures, the inverse agonist-bound 5-HT 1B R structure identifies a basis for the ligand-mediated switch of 5-HT 1B R activity and provides a structural understanding of the inactivation mechanism of 5-HT 1B R and some other class A GPCRs, characterized by ligand-induced outward movement of the extracellular end of TM6 that is coupled with inward movement of the cytoplasmic end of this helix." @default.
• W2791091229 created "2018-03-29" @default.
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• W2791091229 date "2018-03-13" @default.
• W2791091229 modified "2023-10-13" @default.
• W2791091229 title "Crystal structure of the human 5-HT1B serotonin receptor bound to an inverse agonist" @default.
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• W2791091229 doi "https://doi.org/10.1038/s41421-018-0009-2" @default.
• W2791091229 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5847559" @default.

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