Database of articles cited by EMDB/PDB/SASBDB data

Keywords
Structure methods	All X-ray diffraction NMR electron microscopy small angle scattering neutron diffraction fiber diffraction powder diffraction infrared spectroscopy EPR fluorescence transfer theoretical model Hybrid
Author
Journal
IF	>30 >20 >10 >5 all

Title	Bitter taste TAS2R14 activation by intracellular tastants and cholesterol.
Journal, issue, pages	Nature, Year 2024
Publish date	May 22, 2024
Authors	Xiaolong Hu / Weizhen Ao / Mingxin Gao / Lijie Wu / Yuan Pei / Shenhui Liu / Yiran Wu / Fei Zhao / Qianqian Sun / Junlin Liu / Longquan Jiang / Xin Wang / Yan Li / Qiwen Tan / Jie Cheng / Fan Yang / Chi Yang / Jinpeng Sun / Tian Hua / Zhi-Jie Liu /
PubMed Abstract	Bitter taste receptors, particularly TAS2R14, play central roles in discerning a wide array of bitter substances, ranging from dietary components to pharmaceutical agents. TAS2R14 is also widely ...Bitter taste receptors, particularly TAS2R14, play central roles in discerning a wide array of bitter substances, ranging from dietary components to pharmaceutical agents. TAS2R14 is also widely expressed in extragustatory tissues, suggesting its extra roles in diverse physiological processes and potential therapeutic applications. Here we present cryogenic electron microscopy structures of TAS2R14 in complex with aristolochic acid, flufenamic acid and compound 28.1, coupling with different G-protein subtypes. Uniquely, a cholesterol molecule is observed occupying what is typically an orthosteric site in class A G-protein-coupled receptors. The three potent agonists bind, individually, to the intracellular pockets, suggesting a distinct activation mechanism for this receptor. Comprehensive structural analysis, combined with mutagenesis and molecular dynamic simulation studies, elucidate the broad-spectrum ligand recognition and activation of the receptor by means of intricate multiple ligand-binding sites. Our study also uncovers the specific coupling modes of TAS2R14 with gustducin and G proteins. These findings should be instrumental in advancing knowledge of bitter taste perception and its broader implications in sensory biology and drug discovery.
External links	Nature / PubMed:38776963
Methods	EM (single particle)
Resolution	2.77 - 3.3 Å
Structure data	38580 EMDB entry, No image 8xql EMDB-38580, PDB-8xql: Structure of human class T GPCR TAS2R14-miniGs/gust complex with Aristolochic acid A. Method: EM (single particle) / Resolution: 2.99 Å 38582 EMDB entry, No image 8xqn EMDB-38582, PDB-8xqn: Structure of human class T GPCR TAS2R14-DNGi complex with Aristolochic acid A. Method: EM (single particle) / Resolution: 3.05 Å 38583 EMDB entry, No image 8xqo EMDB-38583, PDB-8xqo: Structure of human class T GPCR TAS2R14-Gi complex with Aristolochic acid A. Method: EM (single particle) / Resolution: 2.77 Å 38584 EMDB entry, No image 8xqp EMDB-38584, PDB-8xqp: Structure of human class T GPCR TAS2R14-Gustducin complex with Aristolochic acid A. Method: EM (single particle) / Resolution: 3.29 Å 38586 EMDB entry, No image 8xqr EMDB-38586, PDB-8xqr: Structure 2 of human class T GPCR TAS2R14-miniGs/gust complex with Flufenamic acid. Method: EM (single particle) / Resolution: 3.2 Å 38587 EMDB entry, No image 8xqs EMDB-38587, PDB-8xqs: Structure of human class T GPCR TAS2R14-DNGi complex with Flufenamic acid. Method: EM (single particle) / Resolution: 3.3 Å 38588 EMDB entry, No image 8xqt EMDB-38588, PDB-8xqt: Structure of human class T GPCR TAS2R14-Gi complex. Method: EM (single particle) / Resolution: 2.94 Å 39376 EMDB entry, No image 8yky EMDB-39376, PDB-8yky: Structure of human class T GPCR TAS2R14-Ggustducin complex with agonist 28.1 Method: EM (single particle) / Resolution: 2.99 Å
Chemicals	ChemComp-GOQ: 8-methoxy-6-nitro-naphtho[1,2-e][1,3]benzodioxole-5-carboxylic acid ChemComp-CLR: CHOLESTEROL ChemComp-FLF: 2-[[3-(TRIFLUOROMETHYL)PHENYL]AMINO] BENZOIC ACID / antiinflammatory, inhibitorYM PDB-1aei*: CRYSTAL STRUCTURE OF THE ANNEXIN XII HEXAMER
Source	homo sapiens (human) synthetic construct (others) clostridium perfringens (bacteria)
Keywords	SIGNALING PROTEIN / GPCR / Tas2R14 / miniGsg / GOQ / DNGi / Bitter receptor / Gi / Bitter Receptor. / Gustducin / GPCR Tas2R14 miniGsg FLF Bitter receptor / FLF / Ggustducin / 28.1 / TASTE RECEPTOR.