Target intelligence / Profile preview

Taste receptor type 2 member 10 (TAS2R10) (TAS2R10)

Target
TAS2R10
Molecular classification
G protein-coupled receptor, Taste receptor, Family A G protein-coupled receptor-like
01

Overview

Taste receptor type 2 member 10 (TAS2R10) is a G protein-coupled receptor (GPCR) primarily known for its role in detecting bitter-tasting compounds on the tongue, serving as a critical defense mechanism against the ingestion of toxic substances (1.1.1, 1.2.3). Beyond the oral cavity, TAS2R10 is widely expressed in extra-oral tissues such as the airway smooth muscle, gastrointestinal tract, and various cancer cells, where it mediates diverse physiological processes (1.1.3, 1.5.1). In the lungs, activation of TAS2R10 by bitter agonists like caffeine or strychnine induces potent bronchodilation, making it a promising therapeutic target for obstructive airway diseases like asthma and COPD (1.3.4, 1.5.1). In oncology, TAS2R10 has been identified as a potential tumor suppressor in neuroblastoma and pancreatic cancer, where its activation can inhibit cell proliferation and sensitize cells to chemotherapy by downregulating multidrug resistance transporters (1.5.1, 1.5.2). The receptor is characterized by its broad tuning, allowing it to recognize a diverse array of chemically distinct ligands, including natural toxins and pharmaceutical agents (1.2.3, 1.3.4). Consequently, TAS2R10 represents a versatile target for drug development, though its widespread expression necessitates careful consideration of off-target effects and systemic safety (1.5.1, 1.5.3).

Other names
T2R10TRB2Taste receptor type 2 member 10G-protein coupled receptor 58GPR58
02

Mechanism of action

Agonist-induced activation of the G protein-coupled signaling pathway, typically involving the G protein gustducin, which triggers phospholipase C beta-2 (PLCβ2) and subsequent intracellular calcium release (1.3.4, 1.4.1).

03

Biological functions

Bitter taste perceptionSignal transductionBronchodilationSmooth muscle relaxationRegulation of gastrointestinal motilityTumor suppressionImmune response modulationRegulation of cellular senescence
04

Disease associations

AsthmaPancreatic adenocarcinomaNeuroblastomaObesityChronic obstructive pulmonary disease (COPD)Gastrointestinal motility disorders
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Safety considerations

Potential for systemic side effects due to wide extra-oral expressionRisk of inducing unwanted bitter taste sensationsTissue-specific variability in signaling outcomes (e.g., relaxation vs. contraction)Limited bioavailability of bitter compounds across the blood-brain barrier
06

Interacting drugs

Caffeine

8 more in the full profile.

07

Biomarkers

TAS2R10 mRNA expression levelsTAS2R10 protein expressionTAS2R10 genetic polymorphisms (e.g., SNPs affecting bitter sensitivity)

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