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| Title | Structural basis of β-glucopyranoside salicin recognition by a human bitter taste GPCR. |
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| Journal, issue, pages | Cell Rep, Vol. 44, Issue 5, Page 115604, Year 2025 |
| Publish date | May 27, 2025 |
Authors | Xin Wang / Cui Zhou / Weizhen Ao / Lijie Wu / Yiran Wu / Weixiu Xu / Shenhui Liu / Qiwen Tan / Ling Wang / Fei Zhao / Junlin Liu / Yuan Pei / Suwen Zhao / Tian Hua / ![]() |
| PubMed Abstract | The human perception of bitterness is mediated by type 2 taste receptors (TAS2Rs), which recognize a broad array of bitter substances with distinct chemical properties. TAS2R16 exhibits a pronounced ...The human perception of bitterness is mediated by type 2 taste receptors (TAS2Rs), which recognize a broad array of bitter substances with distinct chemical properties. TAS2R16 exhibits a pronounced selectivity for β-glucoside-moiety-containing compounds, such as salicin from willow bark. However, the molecular mechanism of moiety-specific recognition and receptor activation in TAS2R16 remains unclear. Here, we present cryoelectron microscopy structures of the salicin-activated human TAS2R16 complexed with gustducin and G and G proteins. The binding mode of salicin with TAS2R16 and the specific interactions of the β-D-glucopyranoside moiety are detailed. Together with molecular docking and mutagenesis data, this study uncovers the structural underpinnings of TAS2R16's group-specific recognition, receptor activation, and subsequent gustducin and G protein coupling. These findings advance our understanding of human bitter taste receptors and provide a foundation for structural modifications of bitter glycosides, opening potential therapeutic applications. |
External links | Cell Rep / PubMed:40261795 |
| Methods | EM (single particle) |
| Resolution | 2.77 - 3.35 Å |
| Structure data | EMDB-62129, PDB-9k6l: EMDB-62484, PDB-9kpd: EMDB-62485, PDB-9kpe: EMDB-62486, PDB-9kpf: |
| Chemicals | ![]() ChemComp-SA0: |
| Source |
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Keywords | SIGNALING PROTEIN/IMMUNE SYSTEM / Tas2R16 / GPCR / Gi2 / Salicin / SIGNALING PROTEIN / SIGNALING PROTEIN-IMMUNE SYSTEM complex / Complex |
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homo sapiens (human)
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