Fucosylated Oligosaccharides Inhibit Coronavirus ACE2 Binding

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Solution Overview

Problem

Current treatments lack effectiveness in preventing or attenuating coronavirus infections, particularly SARS-CoV-2, which bind to the ACE2 receptor in the respiratory system and gastrointestinal tract, highlighting the need for a targeted approach to inhibit viral binding.

Innovation Solution

Administration of fucosylated oligosaccharides, such as human milk oligosaccharides (HMOs) like 2′-fucosyllactose, 3-fucosyllactose, and Lacto-N-fucopentaose, which act as competitive inhibitors by binding to the ACE2 receptor, reducing the risk of symptomatic infection through inhalation, pulmonary lavage, oral ingestion, or injection.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If fucosylated oligosaccharides are administered to prevent coronavirus infection, then the binding of coronaviruses to the ACE2 receptor is inhibited, but the complexity of the treatment composition increases

Engineering Contradiction:
Improveeffectiveness in preventing coronavirus infectionVSAvoidcomplexity of treatment composition
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

Fucosylated oligosaccharides act as intermediary molecules that compete with the ACE2 receptor for binding to the coronavirus spike protein. These oligosaccharides serve as soluble decoy receptors, intercepting the virus before it can bind to cellular ACE2 receptors, thereby preventing infection while maintaining a relatively simple composition of naturally occurring sugar molecules

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention uses simplified copies of the natural fucosylated glycans found on the ACE2 receptor surface. By replicating the critical fucosylated oligosaccharide structures that the virus recognizes, the treatment creates artificial binding sites that mimic the natural receptor without requiring the full complexity of the actual ACE2 protein structure

Inventive Principle:
Principle #26Copying

2Reliability

If multiple types of fucosylated oligosaccharides are used to enhance inhibitory effect, then the prevention effectiveness increases, but the manufacturing complexity increases

Engineering Contradiction:
Improveprevention effectivenessVSAvoidmanufacturing complexity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent identifies several different fucosylated oligosaccharides (2'-FL, 3-FL, LNF I, LNF II, LNF III, LDFT, LDFH I, LDFH II) that all share the common functional feature of containing fucose residues. Each oligosaccharide type can independently function as a viral binding inhibitor, allowing for manufacturing flexibility where any of these compounds can be produced separately or in combination, with each serving the same protective function through different molecular structures

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

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 use of fucosylated oligosaccharides effectively inhibits the binding of coronaviruses to the ACE2 receptor, thereby attenuating or preventing infections and promoting recovery by competing with the virus for receptor binding sites in the respiratory and gastrointestinal systems.

Implementation Method 1

These oligosaccharides function as competitive inhibitors of host receptor binding by the virus, thereby reducing risk of symptomatic infection

Methodology Applied
Scientific EffectCompetitive inhibition:

Data Source

PatentUS11331329B2Fucosylated oligosaccharides for prevention of coronavirus infection
Publication Date: 2022.05.17 GLYCOSYN LLC
  • US11331329B2 patent drawing
  • US11331329B2 patent drawing
  • US11331329B2 patent drawing

AI summary

The invention provides compositions and methods for utilizing oligosaccharides, such as isolated human milk oligosaccharides, to attenuate a respiratory pathogen infection and/or to promote recovery from a respiratory pathogen infection in the respiratory system and/or the GI tract of a subject.