T2R04 Inhibitors

The "Tas2r" designation typically refers to the family of Type 2 taste receptors (T2Rs), which are G protein-coupled receptors (GPCRs) involved in the detection of bitter compounds.The T2R family in humans is encoded by a cluster of genes located on various chromosomes, and each gene is denoted by a unique number, such as TAS2R1, TAS2R10, and so forth. These receptors are expressed in the taste receptor cells of the tongue and are responsible for the perception of bitterness, a taste modality that can trigger aversion and is thought to have evolved as a protective mechanism against the ingestion of toxic substances.

T2R proteins are characterized by their seven transmembrane domains, a hallmark of GPCRs, which allow them to span the cell membrane and transmit extracellular ligand-binding events into intracellular responses. Upon binding to bitter compounds, T2Rs activate a G protein, specifically gustducin, which in turn leads to the activation of downstream signaling pathways. This results in an increase in intracellular calcium levels and neurotransmitter release, ultimately conveying the taste signal to the brain for perception.