TAS2R43
receptor / receptor-tas2r43
TAS2R43 is a subtype of human bitter taste receptor.
On this page (7 sections)
Reading the bitterness
TAS2R43 is one of the subtypes of human bitter taste receptors. Activation by lactucin and lactucopicrin found in chicory has been confirmed in receptor assays using cultured cells. In vitro potency (EC50) was approximately 14.9 µM for lactucin, whereas lactucopicrin was approximately 0.46 µM, much more potent. The paper reports that potency decreases in the order: lactucopicrin, lactucin, 11β,13-dihydrolactucin. However, this is the order of potency at the cellular level and does not directly determine the intensity of bitterness of the food as a whole.
This TAS2R43 gene is found to be deleted in many people. A genetic analysis of 946 individuals from 52 populations worldwide found gene copy number ranging from 0 to 2, and the global frequency of the deletion allele reached 0.33. The same study reported that over 20% of participants in Europe lacked this gene. Therefore, the order of potency in cultured cells cannot be directly applied to human populations as a whole.
In fact, the bitterness of caffeine is perceived even by people lacking the TAS2R43 gene (estimated at approximately 18-30% in reviews). This is one example that cannot be fully explained by a single receptor alone. However, it should be noted that this 18-30% figure is an estimate from reviews, and the type of quantity it represents differs from the primary data (0.33 above) showing the frequency of gene deletion itself.
Saccharin sodium 2.5 mM activates TAS2R43-expressing cells. This response was shown to be inhibited in a dose-dependent manner by the aromatic compound (R)-(-)-carvone, which has a menthol-like cooling sensation. In the same experiment, carvone inhibited TAS2R31 as well, but did not inhibit TAS2R50.
Caffeine has been reported to trigger calcium signals at multiple human bitter taste receptors including TAS2R7, TAS2R10, TAS2R14, TAS2R43, and TAS2R46. Within the scope of the abstract, the aromatic compound (R)-citronellal is reported to completely block this caffeine-induced response in TAS2R43-expressing cells. From experiments using multiple receptor agonists of different structures, the same abstract reports that (R)-citronellal was identified as a general allosteric inhibitor of TAS2R43.
Sources for this overview
Checked for this overview: Verified EC50 and potency ranking of lactucin and lactucopicrin
Checked for this overview: Verified descriptions of deletion allele frequency 0.33 and over 20% in Europe / Verified the difference between the 18-30% review estimate and primary data
Checked for this overview: Verified review description that caffeine tastes bitter even in individuals with gene deletion
Checked for this overview: Finding that carvone inhibits saccharin response in a dose-dependent manner
Checked for this overview: Finding that citronellal blocks caffeine-induced response
Follow the connections
lactucin →activates→ TAS2R43
caffeine →remains bitter even for peo…→ TAS2R43
saccharin →activates→ TAS2R43
Measured values (1)
| Kind | Compound | Target | Value | Conditions | Source |
|---|---|---|---|---|---|
| receptor EC50 | lactucin | TAS2R43 | 14.9±2.5 µM | HEK293 cell assay | Lang R, 2022 |
Values are the reported values of each source (with units and conditions). Thresholds and EC50 depend on the panel and method; they are not single true values.
Structured claims — open a section to read each claim's confidence, evidence and limits
Mechanism and receptors (4)
Scope: Receptor assay in a cultured-cell system, in the cited study
Note: Receptor activation alone does not determine the intensity of the food as a whole.
Show data
compound-lactucin —activates→ receptor-tas2r43Scope: The correspondence between the frequency of the gene deletion in human populations and perception
Note: An example that a single receptor cannot explain bitterness perception. "About 18-30%" is a review-level figure. Note that the primary data (946 people / 52 populations) give a deletion-allele frequency of 0.33, a different kind of quantity from "the proportion of individuals lacking the gene".
Show data
compound-caffeine —remains_bitter_despite_absence_of→ receptor-tas2r43Scope: Layer: cell. Ca2+ imaging and luminescence assays in HEK293T cells with heterologous expression of TAS2R43.
Show data
compound-saccharin —activates→ receptor-tas2r43Scope: Layer: cell. Cell functional experiments using several human bitter taste receptors reported to be caffeine-sensitive (TAS2R7, TAS2R10, TAS2R14, TAS2R43, TAS2R46).
Note: Suess et al. 2018's full text was not reached because of a subscription restriction; confirmed from an OpenAlex abstract restoration (the paper's own abstract, not a secondary citation).
Show data
compound-caffeine —activates→ receptor-tas2r43