Target intelligence / Profile preview

Bitter taste receptor type 2 member 2 (TAS2R2)

Target
TAS2R2
Molecular classification
G protein-coupled receptor (GPCR), Receptor, Bitter taste receptor family (TAS2R)
01

Overview

Bitter taste receptor type 2 member 2 (TAS2R2) is one of ~25 human bitter taste receptors and is part of the G protein-coupled receptor (GPCR) family. Its primary role is the detection of bitter substances in the oral cavity, aiding in aversion to potentially harmful compounds. TAS2R2 was long believed to be a pseudogene—non-functional—in most populations but has been shown to exist as a functional variant among specific groups. The receptor is tuned to respond to a moderate number of bitter substances, including several pharmacological agents not typically considered food-related. Upon activation by agonists such as phenylbutazone, TAS2R2 initiates cellular signal transduction through calcium release and membrane depolarization, culminating in transmission of taste signals to the brain. The function and pharmacological relevance of TAS2R2 are limited primarily to taste biology, with little evidence supporting direct disease association or therapeutic modulation in current practice.

Other names
T2R2T2R02PS9TAS2R2Ptaste receptor Ps9 pseudogenetaste receptor, type 2, member 2, pseudogene"Taste 2 receptor member 2"
02

Mechanism of action

Agonists (e.g., phenylbutazone) bind to TAS2R2 and activate the canonical GPCR cascade: - Activation of heterotrimeric G protein (Gα-gustducin, Gβ3, Gγ13) - Phospholipase Cβ2 activation → IP3/DAG production - Release of calcium from ER via IP3 receptor - Activation of TRPM5 channel, cell depolarization, action potential, and neurotransmitter (ATP) release leading to signal transmission to the brainstem

03

Biological functions

Detection of bitter compounds in foodsSignal transduction (through taste bud cells)Potential influence on food choice and avoidance of harmful substances
04

Disease associations

Other (no definitive disease association; role in dietary behavior and risk avoidance)Possible relevance to polymorphisms affecting taste sensation, which can impact nutrition and potentially metabolic or toxicological profilesNo direct involvement in classic disease categories such as cancer, inflammation, etc.
05

Safety considerations

Null as a therapeutic target; no drugs are clinically designed to modulate TAS2R2.Testing for bitter responses may vary due to population polymorphism and gene copy-number variationsPhenylbutazone and other agonists relevant for taste but not as systemically administered drugs through TAS2R2
06

Interacting drugs

Phenylbutazone

3 more in the full profile.

07

Biomarkers

None specific for patient selection or efficacy monitoring. TAS2R2 genotype or presence/absence of its functional variant could act as a genetic biomarker for taste sensitivity to bitter drugs/compounds in populations where functional alleles exist.

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