Interestingly, bitter taste receptors can be found outside of the mouth, such as in the airways, and other parts of the body. These receptors are a possible target for the treatment of asthma and chronic obstructive pulmonary disease because activating them widens the airways in the lungs (COPD). Currently, scientists announce in the Journal of Medicinal Chemistry of the American Chemical Society that they have created a potent and selective molecule that may pave the way for such treatments.
The TAS2R14 subtype is one of the 25 distinct types of bitter taste receptors and is most prevalent in tissues outside of the mouth. The exact composition or “ligand” in the body that triggers the receptor is unknown to scientists, who are also unsure of its shape. However, some artificial substances, including the nonsteroidal anti-inflammatory drug (NSAID) flufenamic acid, are known to bind to and activate TAS2R14s. But these compounds aren’t very potent, and they don’t have similar structural features.
The researchers created numerous additional varieties based on their past discoveries that particular types of architecture boosted potency. They put these substances to the test using a cell-based technique to gauge receptor activation. This method demonstrated that a promising technique consisted of replacing a phenyl ring with a 2-aminopyrimidine and a carboxylic acid group with a tetrazole. One of the novel ligands had a potency that was six times more than flufenamic acid, requiring less of the substance to provide an effect comparable to that of the NSAID. Also, compared to non-bitter taste receptors, this ligand was extremely selective for TAS2R14, which may help to reduce adverse effects. The novel chemicals will direct the creation of drug candidates and give light on the composition, mechanism, and physiological operation of bitter taste receptors.
