ArticleCellular and molecular life sciences : CMLS2020
Rational design of agonists for bitter taste receptor TAS2R14: from modeling to bench and back.
Article in Cellular and molecular life sciences : CMLS, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 66 citations in OpenAlex.
- Bitter taste TAS2R14 and TAS2R46 receptors bound to G proteins: comparison of cryo-EM, AlphaFold, and molecular dynamics structures.European biophysics journal : EBJ · 2026Article
- Intracellular and dual-site inhibition of a bitter taste GPCR.Cellular and molecular life sciences : CMLS · 2026Article
- Identification of Bitter Peptides inFoods (Basel, Switzerland) · 2025Article
- Unraveling molecular mechanisms of cigarette smoke bitterness via chemical profiling and bitter taste receptor activation analysis.Scientific reports · 2025Article
- Emerging paradigms for target discovery of traditional medicines: A genome-wide pan-GPCR perspective.Innovation (Cambridge (Mass.)) · 2025Review
- Bitter taste receptor agonists induce vasorelaxation in porcine coronary arteries.Frontiers in pharmacology · 2025Article
- A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR.Nature communications · 2024Article
- Membrane-bound chemoreception of bitter bile acids and peptides is mediated by the same subset of bitter taste receptors.Cellular and molecular life sciences : CMLS · 2024Article
- Article
- VirtuousPocketome: a computational tool for screening protein-ligand complexes to identify similar binding sites.Scientific reports · 2024Article
- Exploring TAS2R46 biomechanics through molecular dynamics and network analysis.Frontiers in molecular biosciences · 2024Article
- Structure-Based Discovery of Mouse Trace Amine-Associated Receptor 5 Antagonists.Journal of chemical information and modeling · 2023Article
- Relevance of Phytochemical Taste for Anti-Cancer Activity: A Statistical Inquiry.International journal of molecular sciences · 2023Review
- Predicted structure and cell signaling of TAS2R14 reveal receptor hyper-flexibility for detecting diverse bitter tastes.iScience · 2023Article
- Modeling the Orthosteric Binding Site of the G Protein-Coupled Odorant Receptor OR5K1.Journal of chemical information and modeling · 2023Article
- Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor ligands.Cellular and molecular life sciences : CMLS · 2023Article
- Bioactive and Sensory Di- and Tripeptides Generated during Dry-Curing of Pork Meat.International journal of molecular sciences · 2023Review
- BitterMatch: recommendation systems for matching molecules with bitter taste receptors.Journal of cheminformatics · 2022Article
- The bitter end: T2R bitter receptor agonists elevate nuclear calcium and induce apoptosis in non-ciliated airway epithelial cells.Cell calcium · 2022Article
- New strategies for identifying and masking the bitter taste in traditional herbal medicines: The example of Huanglian Jiedu Decoction.Frontiers in pharmacology · 2022Article
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
Abstract
Human bitter taste receptors (TAS2Rs) are a subfamily of 25 G protein-coupled receptors that mediate bitter taste perception. TAS2R14 is the most broadly tuned bitter taste receptor, recognizing a range of chemically diverse agonists with micromolar-range potency. The receptor is expressed in several extra-oral tissues and is suggested to have physiological roles related to innate immune responses, male fertility, and cancer. Higher potency ligands are needed to investigate TAS2R14 function and to modulate it for future clinical applications. Here, a structure-based modeling approach is described for the design of TAS2R14 agonists beginning from flufenamic acid, an approved non-steroidal anti-inflammatory analgesic that activates TAS2R14 at sub-micromolar concentrations. Structure-based molecular modeling was integrated with experimental data to design new TAS2R14 agonists. Subsequent chemical synthesis and in vitro profiling resulted in new TAS2R14 agonists with improved potency compared to the lead. The integrated approach provides a validated and refined structural model of ligand-TAS2R14 interactions and a general framework for structure-based discovery in the absence of closely related experimental structures.
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Registered trials
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.