ArticlePloS one2016
The Pharmacochaperone Activity of Quinine on Bitter Taste Receptors.
Article in PloS one, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 37 citations in OpenAlex.
- GengricinInternational journal of molecular sciences · 2024Trial
- Beef-Derived Peptides Mediated Desensitization of Bitter Taste Receptor T2R14 Through GPCR Kinase 2.Nutrients · 2026Article
- Ethanol Regulates Bitterness Perception of the Trp-Ile-Lys-Lys (WIKK) Peptide by Activating the Human Bitter Receptor T2R47.Foods (Basel, Switzerland) · 2026Article
- Defining the Critical Role of α-Gustducin for NF-κB Inhibition and Anti-Inflammatory Signal Transduction by Bitter Agonists in Lung Epithelium.International journal of molecular sciences · 2026Article
- Regulation of Ras p21 and RalA GTPases activity by quinine in mammary epithelial cells.Molecular and cellular biochemistry · 2024Article
- Genetic variants in taste genes play a role in oral microbial composition and severe early childhood caries.iScience · 2022Article
- Extraoral expression and characterization of bitter taste receptors inFASEB bioAdvances · 2022Article
- Critical cysteines in the functional interaction of adenylyl cyclase isoform 6 with Gαs.FASEB bioAdvances · 2022Article
- Pharmacology of T2R Mediated Host-Microbe Interactions.Handbook of experimental pharmacology · 2022Article
- Structure-Function Analyses of Human Bitter Taste Receptors-Where Do We Stand?Molecules (Basel, Switzerland) · 2020Review
- Article
- Association study of the three functional polymorphisms (TAS2R46G>A, OR4C16G>A, and OR4X1A>T) with recurrent pregnancy loss.Genes & genomics · 2019Article
- Article
- Effects of Quinine, Quinidine and Chloroquine on Human Muscle Nicotinic Acetylcholine Receptors.Frontiers in pharmacology · 2018Article
- Role of Taste Receptors as Sentinels of Innate Immunity in the Upper Airway.Journal of pathogens · 2018Review
- Toward Improving Medication Adherence: The Suppression of Bitter Taste in Edible Taste Films.Advances in pharmacological sciences · 2018Article
- The Role of Quinine-Responsive Taste Receptor Family 2 in Airway Immune Defense and Chronic Rhinosinusitis.Frontiers in immunology · 2018Article
- Analysis of the expression of human bitter taste receptors in extraoral tissues.Molecular and cellular biochemistry · 2017Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Bitter taste is one of the five basic taste sensations which is mediated by 25 bitter taste receptors (T2Rs) in humans. The mechanism of bitter taste signal transduction is not yet elucidated. The cellular processes underlying T2R desensitization including receptor internalization, trafficking and degradation are yet to be studied. Here, using a combination of molecular and pharmacological techniques we show that T2R4 is not internalized upon agonist treatment. Pretreatment with bitter agonist quinine led to a reduction in subsequent quinine-mediated calcium responses to 35 ± 5% compared to the control untreated cells. Interestingly, treatment with different bitter agonists did not cause internalization of T2R4. Instead, quinine treatment led to a 2-fold increase in T2R4 cell surface expression which was sensitive to Brefeldin A, suggesting a novel pharmacochaperone activity of quinine. This phenomenon of chaperone activity of quinine was also observed for T2R7, T2R10, T2R39 and T2R46. Our results suggest that the observed action of quinine for these T2Rs is independent of its agonist activity. This study provides novel insights into the pharmacochaperone activity of quinine and possible mechanism of T2R desensitization, which is of fundamental importance in understanding the mechanism of bitter taste signal transduction.
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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.