Target intelligence / Profile preview

Taste 2 Receptor Family (TAS2Rs)

Target
TAS2Rs
Molecular classification
G protein-coupled receptor, GPCR, Receptor
01

Overview

Taste 2 receptors (TAS2Rs), also known as bitter taste receptors, are a family of approximately 25 seven-transmembrane GPCRs that detect bitter compounds. They are primarily expressed in taste receptor cells but also found in other tissues like airways and the gastrointestinal tract, where they mediate responses to irritants or regulate physiological processes. TAS2Rs activate a signaling cascade involving G proteins (α-gustducin), PLCβ2, IP3, and TRPM5, leading to neurotransmitter release and the perception of bitterness. Genetic variations in TAS2R genes, such as *TAS2R38*, influence individual sensitivity to bitter substances. Drugs can interact with TAS2Rs, affecting palatability or causing off-target effects.

Other names
Bitter Taste ReceptorsT2Rs
02

Mechanism of action

Ligand binding activates G proteins, leading to PLCβ2 activation, IP3 production, Ca2+ release, TRPM5 activation, and neurotransmitter release (ATP). Some drugs can directly activate or block these receptors.

03

Biological functions

Sensory perception of bitternessSignal transductionDetection of bitter compoundsChemosensingImmune response regulationHormone secretion regulation
04

Disease associations

Infectious diseaseAirway inflammationGastrointestinal disorders
05

Safety considerations

Off-target effects due to extraoral expressionDrug palatability issues
06

Interacting drugs

Phenylthiocarbamide (PTC)

4 more in the full profile.

07

Biomarkers

TAS2R38 genotype (for PTC/PROP tasting ability)

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