Hypoallergenic Bet v 1a Mutants Reducing IgE Binding

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Solution Overview

Problem

Current approaches to creating hypoallergenic molecules for treating pollen-food syndrome caused by Bet v 1a cross-reactive allergens are inadequate, as they do not completely eliminate IgE reactivity, and existing mutations in specific regions of the Bet v 1a molecule do not result in a hypoallergenic form with reduced IgE reactivity for all individuals.

Innovation Solution

A hypoallergenic molecule is developed by introducing mutations in the region of amino acids 100 to 125 of Bet v 1a, specifically at position 114, and optionally additional residues like 102 and 120, which significantly reduces IgE reactivity by altering the three-dimensional structure, making it substantially less allergenic compared to the wild-type allergen.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If point mutations are introduced in Bet v 1a at positions 10, 30, 57, 112, 113 and/or 125, then IgE reactivity is decreased for some patients, but not for all patients due to polyclonal nature of IgE responses

Engineering Contradiction:
ImproveIgE reactivityVSAvoidconsistency of hypoallergenic effect
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent divides the allergen protein into functional regions: the IgE-binding region (amino acids 100-125) and the T-cell epitope region. By selectively mutating only the IgE-binding region while preserving the T-cell epitope region, the invention achieves segment-specific modification that reduces IgE reactivity while maintaining immunostimulatory properties. This segmentation approach allows independent optimization of different functional aspects.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention applies local quality modification by introducing mutations specifically at amino acid positions 100-125 (the IgE-binding region) while leaving the rest of the protein sequence intact. This localized mutation strategy ensures that only the specific region responsible for IgE binding is altered, thereby reducing IgE reactivity without affecting other properties like T-cell recognition and overall protein structure.

Inventive Principle:
Principle #3Local quality

2Object-affected harmful factors

If mutations are introduced to reduce IgE reactivity, then hypoallergenic properties are improved, but the three-dimensional structure may be compromised

Engineering Contradiction:
ImproveIgE reactivityVSAvoidthree-dimensional structure
Core Design Contradiction:
Object-affected harmful factorsVSStability of the object's composition

Solution Approach 1:

The mutations are confined to a specific local region (amino acids 100-125) that is known to be involved in IgE binding, rather than disrupting the overall protein fold. This localized approach allows modification of the surface properties responsible for IgE interaction while preserving the core three-dimensional structure and stability of the allergen molecule.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention changes the amino acid sequence parameters specifically in the region of amino acids 100-125, introducing mutations that alter the chemical properties of this segment. These parameter changes are designed to modify IgE binding affinity while maintaining the overall structural integrity of the protein through conservative substitution choices.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If wild-type Bet v 1a is used, then T-cell epitopes are maintained for immune response, but IgE reactivity causes allergic reactions

Engineering Contradiction:
Improveimmune response stimulationVSAvoidIgE reactivity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the allergen into distinct functional domains: the IgE-binding segment (amino acids 100-125) and the T-cell epitope segment. By mutating only the IgE-binding segment while preserving the T-cell epitope segment, the invention achieves selective modification that eliminates IgE reactivity while maintaining T-cell stimulation capability.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention applies local quality changes to the IgE-binding region (amino acids 100-125) by introducing mutations that specifically reduce IgE binding affinity. The T-cell epitope region remains unchanged, thereby preserving its ability to stimulate immune responses. This localized modification strategy allows independent control of different immune interaction pathways.

Inventive Principle:
Principle #3Local quality

Data Source

PatentEP2190865B1Hypoallergenic molecules
Publication Date: 2014.05.07 BIOMAY AG
  • EP2190865B1 patent drawingFigure 1A~1C
  • EP2190865B1 patent drawingFigure 2A~2B
  • EP2190865B1 patent drawingFigure 3~4

AI summary

The present invention relates to a hypoallergenic molecule consisting of Bet v Ia or an allergen having at least 40% identity to Bet v Ia comprising mutations of at least four amino acid residues in the region of amino acids 100 to 125 of Bet v Ia or its corresponding region of the allergen having at least 40% identity to Bet v 1a.