The pharmacology of bitter taste receptors and their role in human airways

Devillier, Philippe; Naline, Emmanuel; Grassin-Delyle, Stanislas

doi:10.1016/j.pharmthera.2015.08.001

Cited by 45 publications

(38 citation statements)

References 129 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Interestingly, several members of the bitter taste receptor (T2R) family have been localized to cilia on human airway epithelia (Shah et al 2009;Lee et al 2012). Downstream effectors of the T2R signal transduction pathway include the G-protein a-gustducin and the enzyme phospholipase C-b2 (PLC-b2) (Devillier et al 2015). In ciliated air-way epithelial cells, a-gustducin localizes to cilia and PLC-b2 localizes to the apical portion of the cell below the cilia (Shah et al 2009).…”

Section: Gpcr Signaling In Motile Ciliamentioning

confidence: 99%

G-Protein-Coupled Receptor Signaling in Cilia

Mykytyn

Askwith

2017

Cold Spring Harb Perspect Biol

View full text Add to dashboard Cite

G-protein-coupled receptors (GPCRs) are the largest and most versatile family of signaling receptors in humans. They respond to diverse external signals, such as photons, proteins, peptides, chemicals, hormones, lipids, and sugars, and mediate a myriad of functions in the human body. Signaling through GPCRs can be optimized by enriching receptors and downstream effectors in discrete cellular domains. Many GPCRs have been found to be selectively targeted to cilia on numerous mammalian cell types. Moreover, investigations into the pathophysiology of human ciliopathies have implicated GPCR ciliary signaling in a number of developmental and cellular pathways. Thus, cilia are now appreciated as an increasingly important nexus for GPCR signaling. Yet, we are just beginning to understand the precise signaling pathways mediated by most ciliary GPCRs and how they impact cellular function and mammalian physiology.

show abstract

Section: Gpcr Signaling In Motile Ciliamentioning

confidence: 99%

G-Protein-Coupled Receptor Signaling in Cilia

Mykytyn

Askwith

2017

Cold Spring Harb Perspect Biol

View full text Add to dashboard Cite

show abstract

“…Human taste and preferences are evolved due to nutrient availabilities within our ancestral environments [2], where they conveyed information, such as energy density, readiness to eat, or toxicity [1,3]. Despite being the area most densely populated with taste receptors, taste is not strictly confined to the oral cavity, but frequently incorporates other sensory inputs from the upper digestive tract and auditory, olfactory and visual systems [1,4,5,6,7,8,9]. This is most evident in those who suffer with ageusia (loss of taste), or anosmia (loss of smell), and still respond physiologically to tastes [3,10], demonstrating taste as a chemical interaction between a chemesthetic agent and receptors, which drives either ingestion or aversion and accompanying hedonic sensations.…”

Section: Introductionmentioning

confidence: 99%

Can taste be ergogenic?

et al. 2020

View full text Add to dashboard Cite

Taste is a homeostatic function that conveys valuable information, such as energy density, readiness to eat, or toxicity of foodstuffs. Taste is not limited to the oral cavity but affects multiple physiological systems. In this review, we outline the ergogenic potential of substances that impart bitter, sweet, hot and cold tastes administered prior to and during exercise performance and whether the ergogenic benefits of taste are attributable to the placebo effect. Carbohydrate mouth rinsing seemingly improves endurance performance, along with a potentially ergogenic effect of oral exposure to both bitter tastants and caffeine although subsequent ingestion of bitter mouth rinses is likely required to enhance performance. Hot and cold tastes may prove beneficial in circumstances where athletes' thermal state may be challenged. Efficacy is not limited to taste, but extends to the stimulation of targeted receptors in the oral cavity and throughout the digestive tract, relaying signals pertaining to energy availability and temperature to appropriate neural centres. Dose, frequency and timing of tastant application likely require personalisation to be most effective, and can be enhanced or confounded by factors that relate to the placebo effect,

show abstract

“…These are G-proteinecoupled receptors, of which about 29 subtypes have been identified in humans. 1 TAS2Rs are not only expressed in the taste cells of the tongue but also in other tissues, 2,3 such as enteroendocrine cells, and their function in other tissues has attracted considerable interest. For example, phenylthiocarbamide (PTC) is a bitter-tasting compound and a specific ligand of taste receptor type 2 member 38 (TAS2R38), 4 and it induces release of cholecystokinin (CCK) and glucagon-like peptide-1 (GLP-1) from enteroendocrine cells in vitro and in vivo.…”

Section: Introductionmentioning

confidence: 99%

Gastrointestinal Hormone Cholecystokinin Increases P-Glycoprotein Membrane Localization and Transport Activity in Caco-2 Cells

Yano

Shimizu

Tomono

et al. 2017

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

It was reported that stimulation of taste receptor type 2 member 38 by a bitter substance, phenylthiocarbamide (PTC), increased P-glycoprotein (P-gp) mRNA level and transport activity via release of the gastrointestinal hormone cholecystokinin-8 (CCK-8) at 9 h. Therefore, we hypothesized that CCK-8 and PTC might also regulate P-gp activity more rapidly via a different mechanism. As a result, we found that the pretreatment of human colon adenocarcinoma (Caco-2) cells with 10-mM PTC significantly decreased the intracellular accumulation of P-gp substrate rhodamine 123 (Rho123) compared with the control after 90-min incubation. Moreover, CCK-8 treatments significantly reduced the accumulation of Rho123 within 30 min, compared with the control. On the other hand, when Caco-2 cells were pretreated with PTC, the efflux ratio of Rho123 was significantly increased compared with control. The efflux ratio of Rho123 in CCK-8 treatment cells was also significantly increased compared with control. Furthermore, CCK-8 increased the phosphorylation of the scaffold proteins ezrin, radixin, and moesin, which regulate translocation of P-gp to the plasma membrane. Therefore, our results indicate that PTC induced release of CCK-8, which in turn induced the phosphorylation of ezrin, radixin, and moesin proteins, leading to upregulation of P-gp transport activity via increased membrane localization of P-gp.

show abstract

The pharmacology of bitter taste receptors and their role in human airways

Cited by 45 publications

References 129 publications

G-Protein-Coupled Receptor Signaling in Cilia

G-Protein-Coupled Receptor Signaling in Cilia

Can taste be ergogenic?

Gastrointestinal Hormone Cholecystokinin Increases P-Glycoprotein Membrane Localization and Transport Activity in Caco-2 Cells

Contact Info

Product

Resources

About