Bitter taste receptors (T2R) are a subfamily of G protein-coupled receptors that enable humans to detect aversive and toxic substances. The ability to discern bitter compounds varies between individuals and is attributed mainly to naturally occurring T2R polymorphisms. T2Rs are also expressed in numerous non-gustatory tissues, including the heart, indicating potential contributions to cardiovascular physiology. In this study. T2Rs that have previously been identified in human cardiac tissues (T2Rs - 10, 14, 30, 31, 46 and 50) and their naturally occurring polymorphisms were functionally characterised. The ligand-dependent signaling responses of some T2R variants were completely abolished (T2R30 Leu252 and T2R46 Met228), whereas other receptor variants had moderate changes in their maximal response, but not potency, relative to wild type. Using a cAMP fluorescent biosensor, we reveal the productive coupling of T2R14, but not the T2R14 Phe201 variant, to endogenous Gai. Modeling revealed...
| Authors | Bloxham, CJ; Hulme, KD; Fierro, F; Fercher, C; Pegg, CL; O'Brien, SL; Foster, SR; Short, KR; Furness, SGB; Reichelt, ME; Niv, MY; Thomas, WG |
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| Journal | BIOCHEMICAL PHARMACOLOGY |
| Pages | 115932 |
| Volume | 219 |
| Date | 19/12/2023 |
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| URL | http://www.ncbi.nlm.nih.gov/pubmed/?term=10.1016/j.bcp.2023.115932 |