T1R2 Receptor Modulators for Skeletal Muscle Metabolic Control
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Solution Overview
Problem
Current methods fail to effectively modulate cell metabolism in skeletal muscle, leading to metabolic dysfunction and muscle mass loss, particularly in conditions like diabetes and obesity, where nutrient sensing mechanisms are uncoupled from muscle plasticity.
Innovation Solution
The use of modulators targeting the T1R2 receptor in skeletal muscle to regulate glucose sensing and metabolism, specifically inhibiting or activating T1R2 to control PARP1 activity and NAD+ levels, thereby enhancing mitochondrial function and glucose utilization.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current metabolic modulation methods are used, then general metabolic regulation is achieved, but skeletal muscle-specific metabolism cannot be effectively modulated leading to muscle mass loss
Solution Approach 1:
The patent applies local quality by targeting T1R2 receptors specifically in skeletal muscle tissue rather than systemically. The composition delivers agents that selectively bind to and modulate T1R2 receptors in muscle cells, achieving tissue-specific metabolic regulation. This localized approach ensures that skeletal muscle metabolism is modulated independently from other tissues, preventing muscle mass loss while maintaining overall metabolic balance.
Solution Approach 2:
The patent uses T1R2 receptors as intermediary molecules to transmit signals that regulate skeletal muscle metabolism. By modulating T1R2 receptor activity, the composition indirectly controls downstream metabolic pathways including glucose uptake, mitochondrial function, and protein synthesis. This intermediary mechanism provides precise control over muscle-specific metabolic processes without requiring direct intervention in multiple cellular pathways.
2Reliability
If nutrient sensing mechanisms are uncoupled from muscle plasticity, then metabolic dysfunction occurs, but effective intervention requires specific receptor targeting
Solution Approach 1:
The patent applies parameter changes by modulating the activity state of T1R2 receptors through selective agonists or antagonists. By changing the activation parameter of T1R2 receptors, the composition restores proper coupling between nutrient sensing and muscle plasticity. This parameter modulation approach corrects metabolic dysfunction by adjusting receptor sensitivity and signaling efficiency without requiring complex structural modifications to the receptor or surrounding tissue.
3Reliability
If T1R2 modulators are administered, then glucose sensing and mitochondrial function are improved, but precise dosing and delivery are required
Solution Approach 1:
The patent employs peptide-based compositions that mimic or bind to T1R2 receptor ligands. These peptide agents serve as simplified copies or analogs of natural signaling molecules, enabling selective T1R2 modulation through relatively simple peptide sequences. This copying approach allows for easier manufacturing compared to small molecule drugs, as peptides can be produced through recombinant expression systems with high purity and consistency, reducing formulation complexity while maintaining therapeutic efficacy.
Data Source
AI summary
Disclosed herein is a method of modulating cell metabolism in skeletal muscle in a subject in need thereof, the method comprising: identifying a subject in need of modulation of cell metabolism in skeletal muscle; and administering to the subject a modulator of skeletal muscle in T1R2. Also disclosed herein is a method of identifying a modulator of T1R2 in skeletal muscle, the method comprising providing muscle-related cells, exposing the cells to a potential modulator of T1R2, and determining modulation, thereby identifying a modulator of T1R2. Further disclosed are compositions identified by this method.