Medication non-compliance caused by bitter tasting medications contributes to mortality from preventable illnesses among infants and young children in the developing world. Broad spectrum, transient suppression of bitter taste perception could improve medication compliance, with life-saving results. Bitter taste receptors (T2AR) are G-protein-coupled receptors (GPCRs) that promote intracellular calcium flux upon ligand binding, resulting in bitter taste perception. Although the multiplicity of bitter taste receptors complicates the development of traditional orthosteric antagonists, inhibiting the intracellular protein-protein interaction between T2ARs and the conserved G-protein α-gustducin provides an alternative approach to universal bitter taste blocking. Structure-activity relationship (SAR) studies were performed using sequence derived from the C-terminus of α-gustducin to determine the amino acid length and composition necessary for inhibition of bitter taste receptor T2R14-dependent calcium flux. This SAR data provided the foundation for synthesis of stapled peptides and pepducins to antagonize the intracellular protein-protein interaction between α-gustducin and T2ARs. Synthetic antagonists were analyzed for potency, stability, broad spectrum activity, onset of action and duration of action.<br/>

Development of cell-permeable peptide antagonists of TAS2R/α-gustducin interaction for universal suppression of bitter taste perception

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.