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Bitter taste receptors

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https://www.readbyqxmd.com/read/28932739/agonist-binding-to-chemosensory-receptors-a-systematic-bioinformatics-analysis
#1
Fabrizio Fierro, Eda Suku, Mercedes Alfonso-Prieto, Alejandro Giorgetti, Sven Cichon, Paolo Carloni
Human G-protein coupled receptors (hGPCRs) constitute a large and highly pharmaceutically relevant membrane receptor superfamily. About half of the hGPCRs' family members are chemosensory receptors, involved in bitter taste and olfaction, along with a variety of other physiological processes. Hence these receptors constitute promising targets for pharmaceutical intervention. Molecular modeling has been so far the most important tool to get insights on agonist binding and receptor activation. Here we investigate both aspects by bioinformatics-based predictions across all bitter taste and odorant receptors for which site-directed mutagenesis data are available...
2017: Frontiers in Molecular Biosciences
https://www.readbyqxmd.com/read/28931063/plant-flavones-enhance-antimicrobial-activity-of-respiratory-epithelial-cell-secretions-against-pseudomonas-aeruginosa
#2
Benjamin M Hariri, Derek B McMahon, Bei Chen, Nithin D Adappa, James N Palmer, David W Kennedy, Robert J Lee
Flavones are a class of natural plant secondary metabolites that have anti-inflammatory and anti-bacterial effects. Some flavones also activate the T2R14 bitter taste receptor, which is expressed in motile cilia of the sinonasal epithelium and activates innate immune nitric oxide (NO) production. Flavones may thus be potential therapeutics for respiratory infections. Our objective was to examine the anti-microbial effects of flavones on the common sinonasal pathogens Candida albicans, Staphylococcus aureus, and Pseudomonas aeruginosa, evaluating both planktonic and biofilm growth...
2017: PloS One
https://www.readbyqxmd.com/read/28923290/use-of-adult-sensory-panel-to-study-individual-differences-in-the-palatability-of-a-pediatric-hiv-treatment-drug
#3
Julie A Mennella, Phoebe S Mathew, Elizabeth D Lowenthal
PURPOSE: The recommended first-line treatment for young children infected with HIV includes the liquid formulation of the co-formulated protease inhibitors lopinavir/ritonavir (Kaletra(®) [Abbott Laboratories, Chicago, Illinois]). Clinical reports indicate that some children readily accept the taste of Kaletra, whereas others strongly reject it, which can deter therapeutic adherence and outcomes. METHODS: As a proof-of-concept approach, a sensory panel of genotyped adults was used to document the range of individual differences in the taste and palatability (hedonics) of the liquid formulation of Kaletra and other taste stimuli, including common excipients...
September 15, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28919036/blends-of-non-caloric-sweeteners-saccharin-and-cyclamate-show-reduced-off-taste-due-to-tas2r-bitter-receptor-inhibition
#4
Maik Behrens, Kristina Blank, Wolfgang Meyerhof
Non-caloric sweeteners are widely used for the formulation of calorie-reduced beverages for health-conscious consumers. However, disadvantages such as undesired off-tastes limit the use of non-nutritive sweeteners. Therefore, the food industry is constantly searching for novel sweeteners and frequently resorts to using blends combining non-caloric sweeteners in a single formulation. The earliest blend allowing higher sweetness levels with reduced bitter off-taste combined saccharin with cyclamate. However, the mechanism by which sweetener blends become superior to single compounds remained obscure...
August 23, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28915899/association-between-polymorphisms-of-tas2r16-and-susceptibility-to-colorectal-cancer
#5
Jonathan Barontini, Marco Antinucci, Sergio Tofanelli, Maurizio Cammalleri, Massimo Dal Monte, Federica Gemignani, Pavel Vodicka, Roberto Marangoni, Ludmila Vodickova, Juozas Kupcinskas, Veronika Vymetalkova, Asta Forsti, Federico Canzian, Angelika Stein, Victor Moreno, Nicola Mastrodonato, Francesca Tavano, Anna Panza, Roberto Barale, Stefano Landi, Daniele Campa
BACKGROUND: Genetics plays an important role in the susceptibility to sporadic colorectal cancer (CRC). In the last 10 years genome-wide association studies (GWAS) have identified over 40 independent low penetrance polymorphic variants. However, these loci only explain around 1‑4% of CRC heritability, highlighting the dire need of identifying novel risk loci. In this study, we focused our attention on the genetic variability of the TAS2R16 gene, encoding for one of the bitter taste receptors that selectively binds to salicin, a natural antipyretic that resembles aspirin...
September 15, 2017: BMC Gastroenterology
https://www.readbyqxmd.com/read/28910546/could-hop-derived-bitter-compounds-improve-glucose-homeostasis-by-stimulating-the-secretion-of-glp-1
#6
Luigi Barrea, Giuseppe Annunziata, Giovanna Muscogiuri, Angela Arnone, Gian Carlo Tenore, Annamaria Colao, Silvia Savastano
Hops (Humulus lupulus L.) is by far the greatest contributors to the bitter property of beer. Over the past years, a large body of evidence demonstrated the presence of taste receptors in different locations of the oral cavity. In addition to the taste buds of the tongue, cells expressing these receptors have been identified in olfactory bulbs, respiratory and gastrointestinal tract. In the gut, the attention was mainly directed to sweet Taste Receptor (T1R) and bitter Taste Receptor (T2R) receptors. In particular, T2R has shown to modulate secretion of different gut hormones, mainly Glucagon-like Peptide 1 (GLP-1), which are involved in the regulation of glucose homeostasis and the control of gut motility, thereby increasing the sense of satiety...
September 14, 2017: Critical Reviews in Food Science and Nutrition
https://www.readbyqxmd.com/read/28902853/the-human-bitter-taste-receptor-t2r38-is-broadly-tuned-for-bacterial-compounds
#7
Christophe Verbeurgt, Alex Veithen, Sébastien Carlot, Maxime Tarabichi, Jacques E Dumont, Sergio Hassid, Pierre Chatelain
T2R38 has been shown to be a specific bacterial detector implicated in innate immune defense mechanism of human upper airway. Several clinical studies have demonstrated that this receptor is associated with the development of chronic rhinosinusitis (CRS). T2R38 was previously reported to bind to homoserine lactones (HSL), quorum sensing molecules specific of Pseudomonas Aeruginosa and other gram negative species. Nevertheless, these bacteria are not the major pathogens found in CRS. Here we report on the identification of bacterial metabolites acting as new agonists of T2R38 based on a single cell calcium imaging study...
2017: PloS One
https://www.readbyqxmd.com/read/28889974/ionotropic-receptors-mediate-drosophila-oviposition-preference-through-sour-gustatory-receptor-neurons
#8
Yan Chen, Hubert Amrein
Carboxylic acids are present in many foods, being especially abundant in fruits. Yet, relatively little is known about how acids are detected by gustatory systems and whether they have a potential role in nutrition or provide other health benefits. Here we identify sour gustatory receptor neurons (GRNs) in tarsal taste sensilla of Drosophila melanogaster. We find that most tarsal sensilla harbor a sour GRN that is specifically activated by carboxylic and mineral acids but does not respond to sweet- and bitter-tasting chemicals or salt...
August 31, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28888429/taste-receptors-in-the-gut-a-new-target-for-health-promoting-properties-in-diet
#9
REVIEW
Bo Ekstrand, Jette Feveile Young, Martin Krøyer Rasmussen
In this review we describe a new target for food functionality, the taste receptors in the gastrointestinal tract. These receptors are involved in an intricate signalling network for monitoring of taste and nutrient intake, homeostasis and energy metabolism, and they are also an early warning system for toxic substances in our diet. Especially the receptors for bitter taste provide a new possibility to activate a number of health related signalling pathways, already at low concentrations of the active substance, without requiring uptake into the body and transport via the circulation...
October 2017: Food Research International
https://www.readbyqxmd.com/read/28874606/bacterial-d-amino-acids-suppress-sinonasal-innate-immunity-through-sweet-taste-receptors-in-solitary-chemosensory-cells
#10
Robert J Lee, Benjamin M Hariri, Derek B McMahon, Bei Chen, Laurel Doghramji, Nithin D Adappa, James N Palmer, David W Kennedy, Peihua Jiang, Robert F Margolskee, Noam A Cohen
In the upper respiratory epithelium, bitter and sweet taste receptors present in solitary chemosensory cells influence antimicrobial innate immune defense responses. Whereas activation of bitter taste receptors (T2Rs) stimulates surrounding epithelial cells to release antimicrobial peptides, activation of the sweet taste receptor (T1R) in the same cells inhibits this response. This mechanism is thought to control the magnitude of antimicrobial peptide release based on the sugar content of airway surface liquid...
September 5, 2017: Science Signaling
https://www.readbyqxmd.com/read/28846687/%C3%AE-catenin-is-required-for-taste-bud-cell-renewal-and-behavioral-taste-perception-in-adult-mice
#11
Dany Gaillard, Spencer G Bowles, Ernesto Salcedo, Mingang Xu, Sarah E Millar, Linda A Barlow
Taste stimuli are transduced by taste buds and transmitted to the brain via afferent gustatory fibers. Renewal of taste receptor cells from actively dividing progenitors is finely tuned to maintain taste sensitivity throughout life. We show that conditional β-catenin deletion in mouse taste progenitors leads to rapid depletion of progenitors and Shh+ precursors, which in turn causes taste bud loss, followed by loss of gustatory nerve fibers. In addition, our data suggest LEF1, TCF7 and Wnt3 are involved in a Wnt pathway regulatory feedback loop that controls taste cell renewal in the circumvallate papilla epithelium...
August 2017: PLoS Genetics
https://www.readbyqxmd.com/read/28835712/association-between-taste-receptor-tas-genes-and-the-perception-of-wine-characteristics
#12
Maura Carrai, Daniele Campa, Pavel Vodicka, Riccardo Flamini, Irene Martelli, Jana Slyskova, Katerina Jiraskova, Alexandra Rejhova, Sona Vodenkova, Federico Canzian, Alberto Bertelli, Antonio Dalla Vedova, Luigi Bavaresco, Ludmila Vodickova, Roberto Barale
Several studies have suggested a possible relationship between polymorphic variants of the taste receptors genes and the acceptance, liking and intake of food and beverages. In the last decade investigators have attempted to link the individual ability to taste 6-n-propylthiouracil (PROP) and the sensations, such as astringency and bitterness, elicited by wine or its components, but with contradictory results. We have used the genotype instead of the phenotype (responsiveness to PROP or other tastants), to test the possible relation between genetic variability and the perception of wine characteristic in 528 subjects from Italy and the Czech Republic...
August 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28834122/bitter-substances-from-plants-used-in-traditional-chinese-medicine-exert-biased-activation-of-human-bitter-taste-receptors
#13
Maik Behrens, Ming Gu, Shengjie Fan, Cheng Huang, Wolfgang Meyerhof
The number and variety of bitter compounds originating from plants is vast. Whereas some bitter chemicals are toxic and should not be ingested, other compounds exhibit health beneficial effects, which is manifest in the cross-cultural believe that the bitterness of medicine is correlated with the desired medicinal activity. The bitter taste receptors in the oral cavity serve as sensors for bitter compounds and, since they are expressed in numerous extraoral tissues throughout the body, may also be responsible for some physiological effects exerted by bitter compounds...
August 21, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28833098/caffeine-may-reduce-perceived-sweet-taste-in-humans-supporting-evidence-that-adenosine-receptors-modulate-taste
#14
Ezen Choo, Benjamin Picket, Robin Dando
Multiple recent reports have detailed the presence of adenosine receptors in sweet sensitive taste cells of mice. These receptors are activated by endogenous adenosine in the plasma to enhance sweet signals within the taste bud, before reporting to the primary afferent. As we commonly consume caffeine, a powerful antagonist for such receptors, in our daily lives, an intriguing question we sought to answer was whether the caffeine we habitually consume in coffee can inhibit the perception of sweet taste in humans...
August 23, 2017: Journal of Food Science
https://www.readbyqxmd.com/read/28829355/the-herbal-bitter-drug-gentiana-lutea-modulates-lipid-synthesis-in-human-keratinocytes-in-vitro-and-in-vivo
#15
Ute Wölfle, Birgit Haarhaus, Jasmin Seiwerth, Anja Cawelius, Kay Schwabe, Karl-Werner Quirin, Christoph M Schempp
Gentiana lutea is a herbal bitter drug that is used to enhance gastrointestinal motility and secretion. Recently we have shown that amarogentin, a characteristic bitter compound of Gentiana lutea extract (GE), binds to the bitter taste receptors TAS2R1 and TAS2R38 in human keratinocytes, and stimulates the synthesis of epidermal barrier proteins. Here, we wondered if GE also modulates lipid synthesis in human keratinocytes. To address this issue, human primary keratinocytes were incubated for 6 days with GE...
August 22, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28828281/genomic-evidence-of-bitter-taste-in-snakes-and-phylogenetic-analysis-of-bitter-taste-receptor-genes-in-reptiles
#16
Huaming Zhong, Shuai Shang, Xiaoyang Wu, Jun Chen, Wanchao Zhu, Jiakuo Yan, Haotian Li, Honghai Zhang
As nontraditional model organisms with extreme physiological and morphological phenotypes, snakes are believed to possess an inferior taste system. However, the bitter taste sensation is essential to distinguish the nutritious and poisonous food resources and the genomic evidence of bitter taste in snakes is largely scarce. To explore the genetic basis of the bitter taste of snakes and characterize the evolution of bitter taste receptor genes (Tas2rs) in reptiles, we identified Tas2r genes in 19 genomes (species) corresponding to three orders of non-avian reptiles...
2017: PeerJ
https://www.readbyqxmd.com/read/28811937/association-between-salivary-leptin-levels-and-taste-perception-in-children
#17
Lénia Rodrigues, Rosa Espanca, Ana Rodrigues Costa, Célia Miguel Antunes, Clarinda Pomar, Fernando Capela-Silva, Cristina Conceição Pinheiro, Francisco Amado, Elsa Lamy
The satiety inducing hormone leptin acts not only at central nervous system but also at peripheral level. Leptin receptors are found in several sense related organs, including the mouth. A role of leptin in sweet taste response has been suggested but, until now, studies have been based on in vitro experiments, or in assessing the levels of the hormone in circulation. The present study investigated whether the levels of leptin in saliva are related to taste perception in children and whether Body Mass Index (BMI) affects such relationship...
2017: Journal of Nutrition and Metabolism
https://www.readbyqxmd.com/read/28811548/ligand-binding-modes-from-low-resolution-gpcr-models-and-mutagenesis-chicken-bitter-taste-receptor-as-a-test-case
#18
Antonella Di Pizio, Louisa-Marie Kruetzfeldt, Shira Cheled-Shoval, Wolfgang Meyerhof, Maik Behrens, Masha Y Niv
Bitter taste is one of the basic taste modalities, warning against consuming potential poisons. Bitter compounds activate members of the bitter taste receptor (Tas2r) subfamily of G protein-coupled receptors (GPCRs). The number of functional Tas2rs is species-dependent. Chickens represent an intriguing minimalistic model, because they detect the bitter taste of structurally different molecules with merely three bitter taste receptor subtypes. We investigated the binding modes of several known agonists of a representative chicken bitter taste receptor, ggTas2r1...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28801754/expression-profiling-of-tas2r-genes-reveals-a-complex-pattern-along-the-mouse-gi-tract-and-the-presence-of-tas2r131-in-a-subset-of-intestinal-paneth-cells
#19
Simone Prandi, Anja Voigt, Wolfgang Meyerhof, Maik Behrens
The chemical variability of the intestinal lumen requires the presence of molecular receptors detecting the various substances naturally occurring in the diet and as a result of the activity of the microbiota. Despite their early discovery, intestinal bitter taste receptors (Tas2r) have not yet been assigned an unambiguous physiological function. Recently, using a CRE-recombinant approach we showed that the Tas2r131 gene is expressed in a subset of mucin-producing goblet cells in the colon of mice. Moreover, we also demonstrated that the expression of the Tas2r131 locus is not restricted to this region...
August 11, 2017: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/28798468/the-bitter-taste-receptor-tas2r16-achieves-high-specificity-and-accommodates-diverse-glycoside-ligands-by-using-a-two-faced-binding-pocket
#20
Anu Thomas, Chidananda Sulli, Edgar Davidson, Eli Berdougo, Morganne Phillips, Bridget A Puffer, Cheryl Paes, Benjamin J Doranz, Joseph B Rucker
Although bitter taste receptors (TAS2Rs) are important for human health, little is known of the determinants of ligand specificity. TAS2Rs such as TAS2R16 help define gustatory perception and dietary preferences that ultimately influence human health and disease. Each TAS2R must accommodate a broad diversity of chemical structures while simultaneously achieving high specificity so that diverse bitter toxins can be detected without all foods tasting bitter. However, how these G protein-coupled receptors achieve this balance is poorly understood...
August 10, 2017: Scientific Reports
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