Page last updated: 2024-10-24

bitter taste receptor activity

Definition

Target type: molecularfunction

Combining with soluble bitter compounds to initiate a change in cell activity. These receptors are responsible for the sense of bitter taste. [GOC:mah]

Bitter taste receptor activity is a molecular function that describes the ability of a protein to bind and respond to bitter-tasting molecules. These receptors are found on the surface of taste receptor cells, specifically Type II taste receptor cells, located within taste buds on the tongue. They belong to the G protein-coupled receptor (GPCR) superfamily, a large group of transmembrane receptors involved in a wide range of cellular signaling processes. Bitter taste receptors are responsible for detecting a diverse range of bitter compounds, which can include alkaloids, glycosides, and other molecules that are often associated with toxicity. When a bitter compound binds to a taste receptor, it initiates a signaling cascade that ultimately leads to the perception of bitterness. This process involves the activation of a G protein called gustducin, which in turn activates phospholipase C (PLC). PLC hydrolyzes phosphatidylinositol 4,5-bisphosphate (PIP2) into inositol trisphosphate (IP3) and diacylglycerol (DAG). IP3 increases intracellular calcium levels, while DAG activates protein kinase C (PKC). These signaling events ultimately lead to the depolarization of the taste receptor cell and the transmission of a signal to the brain, resulting in the perception of bitterness. The molecular function of bitter taste receptor activity is therefore crucial for the detection and avoidance of potentially harmful substances, playing a key role in protecting organisms from ingesting toxins.'
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Proteins (25)

ProteinDefinitionTaxonomy
Taste receptor type 2 member 9A taste receptor type 2 member 9 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYW1]Homo sapiens (human)
Taste receptor type 2 member 1A taste receptor type 2 member 1/119 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYW7]Homo sapiens (human)
Taste receptor type 2 member 3A taste receptor type 2 member 3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYW6]Homo sapiens (human)
Taste receptor type 2 member 4A taste receptor type 2 member 4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYW5]Homo sapiens (human)
Taste receptor type 2 member 5A taste receptor type 2 member 5 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYW4]Homo sapiens (human)
Taste receptor type 2 member 7A taste receptor type 2 member 7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYW3]Homo sapiens (human)
Taste receptor type 2 member 8A taste receptor type 2 member 8 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYW2]Homo sapiens (human)
Taste receptor type 2 member 10A taste receptor type 2 member 10 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYW0]Homo sapiens (human)
Taste receptor type 2 member 13A taste receptor type 2 member 13 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYV9]Homo sapiens (human)
Taste receptor type 2 member 14A taste receptor type 2 member 14 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYV8]Homo sapiens (human)
Taste receptor type 2 member 16A taste receptor type 2 member 16 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9NYV7]Homo sapiens (human)
Taste receptor type 2 member 42A taste receptor type 2 member 42 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q7RTR8]Homo sapiens (human)
Taste receptor type 2 member 60A taste receptor type 2 member 60/135 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59551]Homo sapiens (human)
Taste receptor type 2 member 50A taste receptor type 2 member 50 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59544]Homo sapiens (human)
Taste receptor type 2 member 20A taste receptor type 2 member 20 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59543]Homo sapiens (human)
Taste receptor type 2 member 19A taste receptor type 2 member 19 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59542]Homo sapiens (human)
Taste receptor type 2 member 30A taste receptor type 2 member 30 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59541]Homo sapiens (human)
Taste receptor type 2 member 46A taste receptor type 2 member 46 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59540]Homo sapiens (human)
Taste receptor type 2 member 45A taste receptor type 2 member 45 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59539]Homo sapiens (human)
Taste receptor type 2 member 31A taste receptor type 2 member 31 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59538]Homo sapiens (human)
Taste receptor type 2 member 43A taste receptor type 2 member 43 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59537]Homo sapiens (human)
Taste receptor type 2 member 41A taste receptor type 2 member 41 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59536]Homo sapiens (human)
Taste receptor type 2 member 40A taste receptor type 2 member 40 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59535]Homo sapiens (human)
Taste receptor type 2 member 39A taste receptor type 2 member 39/139 that is encoded in the genome of human. [PRO:DAN, UniProtKB:P59534]Homo sapiens (human)
Taste receptor type 2 member 38A taste receptor type 2 member 38 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P59533]Homo sapiens (human)

Compounds (34)

CompoundDefinitionClassesRoles
isoproterenolisoprenaline : A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hydrochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.

Isoproterenol: Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
catechols;
secondary alcohol;
secondary amino compound
beta-adrenergic agonist;
bronchodilator agent;
cardiotonic drug;
sympathomimetic agent
potassium chloridepotassium chloride : A metal chloride salt with a K(+) counterion.

Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.
inorganic chloride;
inorganic potassium salt;
potassium salt
fertilizer
saccharinsaccharin : A 1,2-benzisothiazole having a keto-group at the 3-position and two oxo substituents at the 1-position. It is used as an artificial sweetening agent.

Saccharin: Flavoring agent and non-nutritive sweetener.
1,2-benzisothiazole;
N-sulfonylcarboxamide
environmental contaminant;
sweetening agent;
xenobiotic
tyrosinetyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.

Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.
amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine
EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
tetramethylthioureathioureas
denatonium benzoate
phenyl beta-d-glucopyranosidephenylglucoside: RN given refers to (beta-(D))-isomerglycoside
trichlorosucrosesucralose : A disaccharide derivative consisting of 4-chloro-4-deoxy-alpha-D-galactopyranose and 1,6-dichloro-1,6-dideoxy-beta-D-fructofuranose units linked by a glycosidic bond.

trichlorosucrose: sweetness intensity roughly 600 times that of sucrose and is nonnutritive and noncaloric; largely unabsorbed in the gastrointestinal tract
disaccharide derivative;
organochlorine compound
environmental contaminant;
sweetening agent;
xenobiotic
sakuranetinsakuranetin : A flavonoid phytoalexin that is (S)-naringenin in which the hydroxy group at position 7 is replaced by a methoxy group.

sakuranetin: major rice phytoalexin; RN given for ((S)-(-))-isomer; structure in first source
(2S)-flavan-4-one;
4'-hydroxyflavanones;
dihydroxyflavanone;
flavonoid phytoalexin;
monomethoxyflavanone
antimycobacterial drug;
plant metabolite
4-nitrophenyl beta-d-glucoside4-nitrophenyl beta-D-glucoside : A beta-D-glucoside that is beta-D-glucopyranose in which the anomeric hydroxy hydrogen is replaced by a 4-nitrophenyl group.

4-nitrophenyl beta-D-glucoside: RN given refers to (beta)-anomer; see also (alpha)-anomer: 3767-28-0; cpd with unspecified anomer: 5779-46-4
beta-D-glucoside;
C-nitro compound
chromogenic compound
2-nitrophenyl-beta-d-glucopyranoside
4-nitrophenyl-beta-d-mannopyranoside4-nitrophenyl-beta-D-mannopyranoside: see also record for (alpha)-isomer
salicinaromatic primary alcohol;
aryl beta-D-glucoside;
benzyl alcohols
antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug
arbutinhydroquinone O-beta-D-glucopyranoside : A monosaccharide derivative that is hydroquinone attached to a beta-D-glucopyranosyl residue at position 4 via a glycosidic linkage.beta-D-glucoside;
monosaccharide derivative
Escherichia coli metabolite;
plant metabolite
strychninestrychnine : A monoterpenoid indole alkaloid that is strychnidine bearing a keto substituent at the 10-position.

Strychnine: An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison.
monoterpenoid indole alkaloid;
organic heteroheptacyclic compound
avicide;
cholinergic antagonist;
glycine receptor antagonist;
neurotransmitter agent;
rodenticide
brucinebrucine: was heading 1991-94 (see under STRYCHNINE 1975-90); DIMETHOXYSTRYCHNINE was see BRUCINE 1975-94; use STRYCHNINE to search BRUCINE 1975-94; very toxic alkaloid from Nux vomica similar to strychnine; used as reagent in analytical chemistry; was MH 1991-94monoterpenoid indole alkaloid;
organic heteroheptacyclic compound
amygdalin(R)-amygdalin : An amygdalin in which the stereocentre on the cyanohydrin function has R-configuration.amygdalinantineoplastic agent;
apoptosis inducer;
plant metabolite
propylthiouracil6-propyl-2-thiouracil : A pyrimidinethione consisting of uracil in which the 2-oxo group is substituted by a thio group and the hydrogen at position 6 is substituted by a propyl group.

Propylthiouracil: A thiourea antithyroid agent. Propythiouracil inhibits the synthesis of thyroxine and inhibits the peripheral conversion of throxine to tri-iodothyronine. It is used in the treatment of hyperthyroidism. (From Martindale, The Extra Pharmacopeoia, 30th ed, p534)
pyrimidinethioneantidote to paracetamol poisoning;
antimetabolite;
antioxidant;
antithyroid drug;
carcinogenic agent;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
hormone antagonist
phenylthioureaN-phenylthiourea : A member of the class of thioureas that is thiourea in which one of the hydrogens is replaced by a phenyl group. Depending on their genetic makeup, humans find it either very bitter-tasting or tasteless. This unusual property resulted in N-phenylthiourea being used in paternity testing prior to the advent of DNA testing.

Phenylthiourea: Phenylthiourea is a THIOUREA derivative containing a phenyl ring. Depending on their genetic makeup, humans can find it either bitter-tasting or tasteless.
thioureasEC 1.14.18.1 (tyrosinase) inhibitor
6-phenylthiouracil6-phenylthiouracil: inhibits production of thyroxinepyrimidines
diphenylthioureaN,N'-diphenylthiourea : Thiourea in which each nitrogen carries a phenyl substituent.thioureasallergen
thioacetanilidethioacetanilide: structure given in first source
thiouracilthiouracil : A nucleobase analogue that is uracil in which the oxo group at C-2 is replaced by a thioxo group.

Thiouracil: Occurs in seeds of Brassica and Crucifera species. Thiouracil has been used as antithyroid, coronary vasodilator, and in congestive heart failure although its use has been largely supplanted by other drugs. It is known to cause blood dyscrasias and suspected of terato- and carcinogenesis.
nucleobase analogue;
thiocarbonyl compound
antithyroid drug;
metabolite
acetylthioureaacetylthiourea: RN given refers to parent cpd

N-acetylthiourea : A member of the class of thioureas that is thiourea in which one of the hydrogens is replaced by an acetyl group.
acetamides;
thioureas
thiobarbituric acid2-thiobarbituric acid : A barbiturate, the structure of which is that of barbituric acid in which the oxygen at C-2 is replaced by sulfur.

thiobarbituric acid: RN given refers to parent cpd
barbituratesallergen;
reagent
ethylenethioureaEthylenethiourea: A degradation product of ethylenebis(dithiocarbamate) fungicides. It has been found to be carcinogenic and to cause THYROID hyperplasia.imidazolidines
n-methylthioureaN-methylthiourea : A member of the class of thioureas that is thiourea in which one of the hydrogens is replaced by a methyl group.thioureasdrug metabolite;
hepatotoxic agent;
human xenobiotic metabolite
thioacetamidethioacetamide : A thiocarboxamide consiting of acetamide having the oxygen replaced by sulfur.

Thioacetamide: A crystalline compound used as a laboratory reagent in place of HYDROGEN SULFIDE. It is a potent hepatocarcinogen.
thiocarboxamidehepatotoxic agent
n-ethylthioureathioureas
esculinbeta-D-glucoside;
hydroxycoumarin
antioxidant;
metabolite
costunolidegermacranolide;
heterobicyclic compound
anthelminthic drug;
antiinfective agent;
antineoplastic agent;
antiparasitic agent;
antiviral drug;
metabolite
dextromethorphandextromethorphan : A 6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthrene in which the sterocenters at positions 4a, 10 and 10a have S-configuration. It is a prodrug of dextrorphan and used as an antitussive drug for suppressing cough.

Dextromethorphan: Methyl analog of DEXTRORPHAN that shows high affinity binding to several regions of the brain, including the medullary cough center. This compound is an NMDA receptor antagonist (RECEPTORS, N-METHYL-D-ASPARTATE) and acts as a non-competitive channel blocker. It is one of the widely used ANTITUSSIVES, and is also used to study the involvement of glutamate receptors in neurotoxicity.
6-methoxy-11-methyl-1,3,4,9,10,10a-hexahydro-2H-10,4a-(epiminoethano)phenanthreneantitussive;
environmental contaminant;
neurotoxin;
NMDA receptor antagonist;
oneirogen;
prodrug;
xenobiotic
jaceosidinjaceosidin : A trihydroxyflavone that is flavone with hydroxy groups at positions 5, 7 and 4' and methoxy groups at positions 3' and 6. Isolated from Salvia tomentosa and Artemisia asiatica, it exhibits anti-allergic, anti-inflammatory and apoptosis inducing activties.dimethoxyflavone;
trihydroxyflavone
anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
metabolite
acesulfame potassiumsulfuric acid derivative