Broad Bitter Antagonist Compound C for T2R Receptor Modulation
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Solution Overview
Problem
Current methods lack effective identification and modulation of human bitter taste receptors, particularly for bitter compounds in coffee, limiting the ability to alleviate bitter taste in food and beverages.
Innovation Solution
Discovery of a broad bitter antagonist compound (Compound C) that inhibits multiple human bitter taste receptors, including hT2R3, 7, 10, 14, 16, 44, 51, 55, 61, 63, 64, 65, and 71, and others, reducing bitter taste perception in coffee and other foods and beverages.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If specific human bitter taste receptors (hT2Rs) are identified and targeted, then the ability to modulate bitter taste perception is improved, but the complexity of the system increases due to the need to characterize multiple receptors and their ligands
Solution Approach 1:
The patent identifies and characterizes multiple human bitter taste receptors (hT2Rs) that can be activated by diverse bitter compounds, creating a universal receptor family that mediates bitter taste perception across different ligands. This multi-functionality allows a single receptor family to handle various bitter substances, improving taste modulation precision without proportionally increasing system complexity.
Solution Approach 2:
The patent segments the bitter taste reception system into specific receptor subtypes (hT2R1, hT2R2, hT2R3, etc.), each with potentially different ligand specificities. This segmentation allows for targeted modulation of bitter taste by identifying which specific receptor subtypes are activated by particular compounds, enabling precise taste control while managing complexity through systematic classification.
2Adaptability or versatility
If a broad spectrum bitter antagonist is developed, then the effectiveness in blocking bitter taste across multiple receptors is improved, but the difficulty in identifying and validating such compounds increases
Solution Approach 1:
The patent employs receptor expression systems as intermediaries to detect and measure bitter compound activity. By expressing hT2R receptors in cell-based assay systems, the patent creates a measurable response that can be used to screen for bitter antagonists. This intermediary system simplifies the detection process and enables high-throughput identification of compounds that block multiple receptor subtypes, improving versatility while reducing identification difficulty.
3Reliability
If multiple bitter taste receptors are characterized, then the comprehensiveness of bitter taste modulation is improved, but the time required for receptor identification and validation increases
Solution Approach 1:
The patent performs preliminary characterization of hT2R receptors and their ligand specificities before developing therapeutic or food applications. By pre-identifying which receptor subtypes are activated by specific bitter compounds, the patent establishes a foundation that can be used for rapid validation in subsequent applications. This preliminary action improves reliability through thorough initial characterization while reducing the time needed for later validation stages.
Data Source
AI summary
The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.