Bitter Taste Receptor Agonists for Food Palatability
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Solution Overview
Problem
Current understanding of bitter taste transduction mechanisms is limited, particularly in explaining the recognition of a wide variety of bitter compounds by the mammalian gustatory system, with few mammalian TAS2Rs having identified ligands, and existing technologies lack effective methods to suppress or enhance bitter taste for food and pharmaceutical applications.
Innovation Solution
Identification of agonists and antagonists for human bitter taste receptors hTAS2R1, hTAS2R3, hTAS2R7, and hTAS2R40, enabling the design of compounds to suppress or enhance bitter taste responses, thereby improving food palatability and patient compliance with oral pharmaceuticals.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If the bitter taste transduction pathway is manipulated to suppress or eliminate bitter taste, then food palatability is improved and patient compliance with oral pharmaceuticals increases, but the mechanism of bitter taste transduction remains poorly understood
Solution Approach 1:
The patent identifies and characterizes specific agonists for human bitter taste receptors (hTAS2R1, hTAS2R3, hTAS2R7, hTAS2R40) before applying them to suppress bitter taste in foods and pharmaceuticals. This preliminary identification of receptor ligands enables targeted manipulation of the bitter taste pathway while providing foundational knowledge about the transduction mechanism.
Solution Approach 2:
The patent uses identified agonists as intermediary substances to modulate bitter taste receptor activity. These agonists serve as tools to suppress or enhance bitter taste perceptions, enabling applications in food palatability improvement and pharmaceutical compliance while simultaneously providing insights into the transduction mechanism through their interaction with specific receptors.
2Device complexity
If only a limited number of mammalian TAS2R receptors are used, then the genetic repertoire is simplified, but the ability to recognize thousands of different bitter compounds is insufficient
Solution Approach 1:
The patent identifies multiple human bitter taste receptors (hTAS2R1, hTAS2R3, hTAS2R7, hTAS2R40) that can recognize different bitter compounds. Each receptor is characterized with specific agonists, demonstrating that a limited set of receptors can be expanded to recognize diverse ligands through functional characterization and agonist identification, thereby increasing ligand recognition capacity without proportionally increasing the number of receptors.
3Difficulty of detecting and measuring
If few mammalian TAS2R receptors have identified ligands, then the research focus is narrowed, but the understanding of bitter taste transduction remains limited
Solution Approach 1:
The patent replaces the need for complex in vivo bitter taste testing with in vitro receptor characterization systems. By identifying and characterizing agonists for specific human bitter taste receptors in a controlled laboratory setting, the patent enables detailed study of the transduction mechanism without requiring complex behavioral assays, thereby improving detection and measurement capabilities while deepening mechanistic understanding.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The identified agonists and antagonists allow for the development of compounds that can significantly reduce or enhance bitter taste perceptions, addressing the limitations of current technologies in manipulating bitter taste transduction and improving the palatability of foods and pharmaceuticals.
Implementation Method 1
Taste transduction involves the interaction of molecules, i.e. tastants with taste receptor-expressing cells which reside in the taste buds located in the papillae of the tongue
Implementation Method 2
bitter taste transduction is mediated by so-called G-protein coupled receptors (GPCRs). GPCRs are 7 transmembrane domain cell surface proteins that amplify signals generated at a cell surface when the receptor interacts with a ligand (a tastant) whereupon they activate heterotrimeric G-proteins
Implementation Method 3
The Galpha q type couple with GPCRs to activate phospholipase C which leads to an increase in cellular Ca2+
Implementation Method 4
These G-proteins dissociate into alpha and beta-gamma subunits upon activation, resulting in a complex cascade of cellular events that results in the cell producing second messengers, such as calcium ions
Data Source
AI summary
The present invention relates to agonists of the hTAS2R1, hTAS2R3, hTAS2R7 and hTAS2R40 bitter taste receptors, respectively, and their role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block hTAS2R1, hTAS2R3, hTAS2R7 or hTAS2R40 bitter taste transduction or bitter taste response.