Target intelligence / Profile preview

Taste receptor type 1 member 2 and Taste receptor type 1 member 3 heterodimer (TAS1R2/TAS1R3)

Target
TAS1R2/TAS1R3
Molecular classification
G protein-coupled receptor, Class C GPCR, Heterodimeric receptor, Receptor
01

Overview

The TAS1R2/TAS1R3 Sweet Taste Receptor is a heterodimeric G protein-coupled receptor (GPCR) that serves as the primary sensor for sweet-tasting molecules, including sugars, polyols, and high-intensity sweeteners (UniProt: P59768, Q7RTX0). Beyond its well-known role in the oral cavity for taste perception, this receptor is expressed in various extra-oral tissues, including the gut, pancreas, and hypothalamus, where it acts as a nutrient sensor (PubMed: 21414488). In the gastrointestinal tract, activation of TAS1R2/TAS1R3 by luminal glucose triggers the release of incretin hormones such as glucagon-like peptide-1 (GLP-1), which modulates insulin secretion and gastric emptying (PubMed: 17709750). Because of its central role in glucose homeostasis and energy balance, the receptor is a significant focus in research regarding obesity and type 2 diabetes (PubMed: 28533247). Pharmacological agents interacting with this receptor include a wide range of commercial sweeteners as agonists and compounds like lactisole or gymnemic acids as antagonists (PubChem: CID 109557). Understanding the systemic effects of TAS1R2/TAS1R3 activation is essential for evaluating the metabolic impact of non-nutritive sweeteners and developing novel therapeutic strategies for metabolic syndrome. The receptor's ability to detect diverse chemical structures makes it a unique target for both food science and metabolic pharmacology.

Other names
T1R2/T1R3Sweet taste receptorTAS1R2-TAS1R3 complexG protein-coupled receptor 70/71T1R2+3
02

Mechanism of action

The receptor functions as a heterodimer that, upon binding sweet ligands, activates a G protein signaling cascade involving G-alpha-gustducin or G-alpha-q, leading to the activation of phospholipase C beta 2 (PLC-beta-2) and the opening of TRPM5 ion channels, resulting in cell depolarization and neurotransmitter or hormone release (PubMed: 11830529).

03

Biological functions

Signal transductionSweet taste perceptionGlucose sensingHormone secretion regulationNutrient sensing
04

Disease associations

Diabetes mellitusObesityMetabolic syndromeDental caries
05

Safety considerations

Metabolic disruption from chronic agonist exposureAlteration of gut microbiome compositionPotential for paradoxical weight gainCephalic phase insulin response interferencePotential for glucose intolerance
06

Interacting drugs

Sucralose

13 more in the full profile.

07

Biomarkers

Taste perception thresholdGlucagon-like peptide 1 (GLP-1) levelsPostprandial insulin responseTAS1R3 genetic polymorphisms (e.g., rs307355)

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