Olfactory Receptor Compounds for Endogenous Hormone Secretion
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Solution Overview
Problem
Current treatments for type-2 diabetes mellitus and obesity using GLP-1 analogs and dual GLP-1/GIP analogs are associated with high risks of adverse events, significant side effects, and high costs, including hypoglycemia, nausea, vomiting, diarrhea, abdominal pain, and costly weekly injections.
Innovation Solution
Compositions and methods that modulate olfactory receptor activity to induce secretion of endogenous GLP-1 and GIP, using receptor activating compounds such as 3-methylpentanoic acid, farnesol, and medium-chain free fatty acids, to increase insulin secretion and suppress appetite with minimal side effects, offering alternative administration routes like oral, sublingual, and inhalation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If GLP-1 analogs are administered to treat type-2 diabetes and obesity, then insulin secretion is induced and appetite is suppressed, but the risk of adverse events and side effects increases
Solution Approach 1:
The patent uses olfactory receptor activating compounds as intermediaries to indirectly stimulate endogenous GLP-1 and GIP secretion. Instead of directly administering GLP-1 analogs that cause adverse effects, the invention employs compounds that activate olfactory receptors (such as OR51E1) to trigger the body's natural production of incretin hormones, thereby achieving therapeutic effects with reduced side effects
Solution Approach 2:
The invention enables the body to produce its own therapeutic agents (endogenous GLP-1 and GIP) through olfactory receptor activation. By stimulating the endocrine system to self-generate the necessary hormones rather than relying on external analogs, the treatment achieves better tolerance and reduced adverse events while maintaining effectiveness
2Reliability
If GLP-1 analogs are administered weekly via injection, then treatment effectiveness is achieved, but treatment convenience and patient compliance decrease
Solution Approach 1:
The patent replaces the mechanical injection administration system with alternative delivery methods including oral, sublingual, buccal, inhalation, and transdermal routes. This substitution eliminates the need for needle injections while maintaining therapeutic effectiveness through activation of olfactory receptors via various non-invasive pathways
3Reliability
If GLP-1 analogs are used to treat diabetes and obesity, then metabolic benefits are achieved, but treatment costs increase
Solution Approach 1:
The invention employs relatively inexpensive olfactory receptor activating compounds (such as 3-methylpentanoic acid, farnesol, and medium-chain free fatty acids) that can be administered through cost-effective routes like oral or inhalation. These compounds are metabolized and eliminated naturally, avoiding the high costs associated with proprietary GLP-1 analog formulations and their complex delivery systems
4Reliability
If multiple receptor activating compounds are combined to enhance治疗效果, then therapeutic efficacy is improved, but composition complexity increases
Solution Approach 1:
The patent combines multiple olfactory receptor activating compounds (such as 3-methylpentanoic acid, farnesol, eugenol, and medium-chain free fatty acids) into a single composition that targets different olfactory receptors including OR51E1. This merging approach enhances therapeutic efficacy through synergistic effects while maintaining a unified formulation that is easier to administer than multiple separate treatments
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 approach effectively induces insulin secretion and appetite suppression with reduced side effects and costs, providing a safer and more convenient treatment option for type-2 diabetes and obesity.
Implementation Method 1
a first compound adapted to bind to and activate at least one first receptor selected from the group consisting of: olfactory receptor family 51 subfamily E member 1 (OR51E1), olfactory receptor family 1 subfamily A member 1 (OR1A1), olfactory receptor family 2 subfamily C member 1 (OR2C1), and olfactory receptor family 10 subfamily J member 5 (OR10J5)
Implementation Method 2
a second compound adapted to bind to and activate at least one second receptor selected from the group consisting of: free fatty acid receptor 1 (FFAR1), free fatty acid receptor 4 (FFAR4), olfactory receptor family 2, subfamily W, member 1 (OR2W1), olfactory receptor family 2, subfamily B, member 11 (OR2B11), olfactory receptor family 2 subfamily J member 3 (OR2J3), and transient receptor potential cation channel, subfamily A, member 1 (TRPA1)
Implementation Method 3
insulin secretion is induced by pancreatic β-cells when glucagon-like peptide-1 (GLP-1) binds to and activates GLP-1 receptor proteins on endogenous gastrointestinal (GI) cells
Data Source
AI summary
Disclosed herein are compounds and ligands, and compositions formed therewith, that modulate insulin secretion and suppress appetite by activating ectopic olfactory receptors. Also disclosed herein are methods for using the compositions to treat endocrine diseases, such as type-2 diabetes, and disorders, such as abnormal insulin secretion.