ArticleThe Journal of biological chemistry2011
Structural basis of activation of bitter taste receptor T2R1 and comparison with Class A G-protein-coupled receptors (GPCRs).
Article in The Journal of biological chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
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Who cites it
33 citing papers in PubMed, 90 citations in OpenAlex.
- Article
- The structure and function of taste G protein-coupled receptors and their implications in diseases.International journal of oral science · 2026Review
- Targeting G-protein-coupled receptors and gut microbiota: Ge-Lian Qi-Shen decoction elevates GLP-1 to combat non-alcoholic fatty liver disease.Chinese medicine · 2026Article
- Unravelling the human taste receptor interactome: machine learning and molecular modelling insights into protein-protein interactions.NPJ science of food · 2025Article
- Bitter Taste Receptors in Bacterial Infections and Innate Immunity.Immunity, inflammation and disease · 2025Review
- Ectopic taste receptors in animal physiology: evolutionary conservation and functional diversification.Frontiers in cell and developmental biology · 2025Review
- A Computational Approach to Understanding and Predicting the Edulcorant Profile of Glucosyl Steviol Glycosides.Foods (Basel, Switzerland) · 2024Article
- Exploring TAS2R46 biomechanics through molecular dynamics and network analysis.Frontiers in molecular biosciences · 2024Article
- Fragment-based Drug Discovery Strategy and its Application to the Design of SARS-CoV-2 Main Protease Inhibitor.Current medicinal chemistry · 2024Review
- Genetic variants in taste genes play a role in oral microbial composition and severe early childhood caries.iScience · 2022Article
- Molecular insights into human taste perception and umami tastants: A review.Journal of food science · 2022Review
- Prediction of molecular interactions and physicochemical properties relevant for vasopressin V2 receptor antagonism.Journal of molecular modeling · 2022Article
- Functional molecular switches of mammalian G protein-coupled bitter-taste receptors.Cellular and molecular life sciences : CMLS · 2021Article
- Fragment-based in silico design of SARS-CoV-2 main protease inhibitors.Chemical biology & drug design · 2021Article
- Local Adaptation of Bitter Taste and Ecological Speciation in a Wild Mammal.Molecular biology and evolution · 2021Article
- Positive selection drives the evolution of a primate bitter taste receptor gene.Ecology and evolution · 2021Article
- Predicted structure of fully activated human bitter taste receptor TAS2R4 complexed with G protein and agonists.QRB discovery · 2021Article
- Structure-Function Analyses of Human Bitter Taste Receptors-Where Do We Stand?Molecules (Basel, Switzerland) · 2020Review
- TAS2R20 variants confer dietary adaptation to high-quercitrin bamboo leaves in Qinling giant pandas.Ecology and evolution · 2020Article
- Differential Cerebral Gustatory Responses to Sucrose, Aspartame, and Stevia Using Gustatory Evoked Potentials in Humans.Nutrients · 2020Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The human bitter taste receptors (T2Rs) are non-Class A members of the G-protein-coupled receptor (GPCR) superfamily, with very limited structural information. Amino acid sequence analysis reveals that most of the important motifs present in the transmembrane helices (TM1-TM7) of the well studied Class A GPCRs are absent in T2Rs, raising fundamental questions regarding the mechanisms of activation and how T2Rs recognize bitter ligands with diverse chemical structures. In this study, the bitter receptor T2R1 was used to systematically investigate the role of 15 transmembrane amino acids in T2Rs, including 13 highly conserved residues, by amino acid replacements guided by molecular modeling. Functional analysis of the mutants by calcium imaging analysis revealed that replacement of Asn-66(2.65) and the highly conserved Asn-24(1.50) resulted in greater than 90% loss of agonist-induced signaling. Our results show that Asn-24(1.50) plays a crucial role in receptor activation by mediating an hydrogen bond network connecting TM1-TM2-TM7, whereas Asn-66(2.65) is essential for binding to the agonist dextromethorphan. The interhelical hydrogen bond between Asn-24(1.50) and Arg-55(2.54) restrains T2R receptor activity because loss of this bond in I27A and R55A mutants results in hyperactive receptor. The conserved amino acids Leu-197(5.50), Ser-200(5.53), and Leu-201(5.54) form a putative LXXSL motif which performs predominantly a structural role by stabilizing the helical conformation of TM5 at the cytoplasmic end. This study provides for the first time mechanistic insights into the roles of the conserved transmembrane residues in T2Rs and allows comparison of the activation mechanisms of T2Rs with the Class A GPCRs.
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