Chimeric T1R Taste Receptors for Sweet Umami Detection

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Solution Overview

Problem

Current technologies lack effective methods to identify and modulate sweet and umami taste receptors, particularly in distinguishing between sweet and umami taste stimuli and enhancing taste responses to compounds.

Innovation Solution

Development of chimeric taste receptor polypeptides by combining portions of T1R1 and T1R2 genes with T1R3 receptors, expressed in host cells like HEK-293, to create chimeric receptors that respond to sweet and umami taste stimuli or enhance existing taste responses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If chimeric taste receptor polypeptides are developed by combining T1R1 and T1R2 genes with T1R3 receptors, then the ability to identify and modulate sweet and umami taste receptors is improved, but the device complexity increases

Engineering Contradiction:
Improveability to identify and modulate taste receptorsVSAvoidcomplexity of chimeric receptor construction
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The chimeric taste receptor is constructed by segmenting the parental T1R1 and T1R2 receptors into distinct functional domains (extracellular N-terminal domain and transmembrane domain) and recombining these segments to create novel receptor configurations. This segmentation allows systematic exploration of structure-function relationships while managing construction complexity through modular assembly approaches.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The chimeric taste receptor design achieves multi-functionality by combining domains from different parental receptors (T1R1 for umami, T1R2 for sweet) within a single receptor protein. This allows the chimeric receptor to potentially respond to multiple taste modalities or to be used in multiple assay formats (heteromeric and homomeric configurations), thereby improving versatility without proportionally increasing operational complexity.

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Measurement precision

If chimeric taste receptors are used to distinguish between sweet and umami taste stimuli, then measurement precision is improved, but the difficulty of detecting and measuring increases

Engineering Contradiction:
Improvedistinguishing ability between sweet and umami stimuliVSAvoidcomplexity of taste response detection
Core Design Contradiction:
Measurement precisionVSDifficulty of detecting and measuring

Solution Approach 1:

The chimeric taste receptor introduces local quality differentiation by placing specific parental receptor domains in defined positions within the chimera structure. The extracellular N-terminal domain from one parental receptor is combined with the transmembrane domain from another, creating localized functional regions that confer specific ligand binding properties. This local quality approach enables precise distinction between sweet and umami stimuli through targeted domain contributions.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The chimeric taste receptor acts as an intermediary system that translates complex taste stimuli into measurable cellular responses. By creating intermediate receptor structures with defined domain compositions, the system facilitates detection and measurement of taste responses through established cellular assay methods, thereby reducing the overall difficulty of measurement while maintaining precision.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Productivity

If chimeric taste receptor polypeptides are expressed in host cells, then productivity of taste modulator identification is improved, but the device complexity increases

Engineering Contradiction:
Improveefficiency of taste modulator identificationVSAvoidcomplexity of expression system
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The chimeric taste receptor polypeptides are constructed and validated in advance through heteromeric and homomeric expression configurations before being deployed in high-throughput screening assays. This preliminary action of creating predefined receptor expressions in host cells (such as HEK-293 cells) establishes ready-to-use systems that improve productivity during actual modulator identification campaigns, as the complex receptor construction work is completed beforehand.

Inventive Principle:
Principle #10Preliminary action

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 chimeric receptors effectively identify sweet and umami taste modulators and enhancers, demonstrating enhanced responsiveness to various taste compounds, including sweeteners and umami ligands, as shown in calcium imaging experiments.

Implementation Method 1

The T1Rs belong to class-C G protein coupled receptors, and each Class-C GPCR consists of a large N-terminal extracellular domain and a C-terminal 7-transmembrane domain

Methodology Applied
Scientific EffectG protein coupled receptor signaling:

Implementation Method 2

demonstrating enhanced responsiveness to various taste compounds, including sweeteners and umami ligands, as shown in calcium imaging experiments

Methodology Applied
Scientific EffectCalcium imaging:

Data Source

PatentEP3312194A1Cell lines expressing chimeric human sweet-umami and umami-sweet taste receptors
Publication Date: 2018.04.25 FIRMENICH INC
  • EP3312194A1 patent drawingFigure 1
  • EP3312194A1 patent drawingFigure 2
  • EP3312194A1 patent drawingFigure 3

AI summary

This invention relates to chimeric taste receptors comprising the extracellular portion of one T1R or a variant or fragment thereof, either T1R1 or T1R2, and the transmembrane portion of another T1R or a variant or fragment thereof, either T1R1 or T1R2, preferably associated with a T1R3 polypeptide and a suitable G protein. These chimeric taste receptors and cells which express such chimeric taste receptors are useful in assays for identifying sweet and umami ligands as well in assays for identifying sweet and umami enhancers. Additionally, these chimeric taste receptors and cells which express same can be used to map and determine where specific sweet and umami ligands interact with their respective receptors and to elucidate the mechanism of receptor activation.