ArticleNature communications2024
A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR.
Article in Nature communications, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
What it found
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Who cites it
25 citing papers in PubMed.
- Article
- Bitter taste TAS2R14 and TAS2R46 receptors bound to G proteins: comparison of cryo-EM, AlphaFold, and molecular dynamics structures.European biophysics journal : EBJ · 2026Article
- The structure and function of taste G protein-coupled receptors and their implications in diseases.International journal of oral science · 2026Review
- Bile Canalicular Bitter Taste Receptors Inhibit β-Adrenergic Receptor-Induced Lipolysis in Steatotic Hepatocytes.International journal of molecular sciences · 2026Article
- Many ligands and states of bitter taste GPCRs.Nature structural & molecular biology · 2026Article
- Structural insights into coffee bitter taste perception by TAS2R43 receptor.Nature structural & molecular biology · 2026Article
- Ligand binding modes of the bitter taste receptor T2R14 and T2R46.Nature structural & molecular biology · 2026Article
- Intracellular and dual-site inhibition of a bitter taste GPCR.Cellular and molecular life sciences : CMLS · 2026Article
- Computational analysis of umami and bitter taste interactions: orthogonality in receptor-ligand binding.RSC advances · 2026Article
- T2R5 Agonist Phendione Decreases Cell Viability and Induces Apoptosis in Head and Neck Squamous Cell Carcinoma.Molecular cancer therapeutics · 2026Article
- Innate immune functions of bitter taste receptors across physiological systems.Journal of translational medicine · 2026Review
- Article
- Accelerating GPCR drug discovery through computation and experiment integrated with direct detection of ligand binding events.npj drug discovery · 2026Review
- Homoeriodictyol, targeting the bitter taste receptor TAS2R14, lowers the secretion of pro-inflammatory chemokines upon treatment with SARS-CoV-2 peptide pools in human peripheral blood mononuclear cells.Frontiers in immunology · 2026Article
- Identification of Bitter Peptides inFoods (Basel, Switzerland) · 2025Article
- Quercetin as a Bitter Taste Receptor Agonist with Anticancer Effects in Head and Neck Cancer Cells.Nutrients · 2025Article
- Bitopic AJournal of medicinal chemistry · 2025Article
- Chemosensory role of intracellular TAS2Rs, the activation of which triggers drug excretion by ABCB1 in cancer cells.Scientific reports · 2025Article
- Chemosensory Receptors in Vertebrates: Structure and Computational Modeling Insights.International journal of molecular sciences · 2025Review
- Spatiotemporal calcium signaling patterns underlying opposing effects of histamine and TAS2R agonists in airway smooth muscle.American journal of physiology. Lung cellular and molecular physiology · 2025Article
Corrections and comments
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Authors and funding
15 authors.
Funding
Abstract
Bitter taste receptors (TAS2Rs), a subfamily of G-protein coupled receptors (GPCRs) expressed orally and extraorally, elicit signaling in response to a large set of tastants. Among 25 functional TAS2Rs encoded in the human genome, TAS2R14 is the most promiscuous, and responds to hundreds of chemically diverse ligands. Here we present the cryo-electron microscopy (cryo-EM) structure of the human TAS2R14 in complex with its signaling partner gustducin, and bound to flufenamic acid (FFA), a clinically approved nonsteroidal anti-inflammatory drug. The structure reveals an unusual binding mode, where two copies of FFA are bound at distinct pockets: one at the canonical receptor site within the trans-membrane bundle, and the other in the intracellular facet, bridging the receptor with gustducin. Together with a pocket-specific BRET-based ligand binding assay, these results illuminate bitter taste signaling and provide tools for a site-targeted compound design.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.