Vasculotide Peptide Targets Tie2 Receptor to Reduce Allergic Inflammation

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Solution Overview

Problem

Current treatments for allergic diseases, particularly those involving eosinophils and basophils, often lead to general immunosuppression and do not effectively address the underlying inflammatory responses, with existing therapies failing to specifically target these cells for reduction.

Innovation Solution

Administration of a multimeric Tie2 binding peptide, Vasculotide, which inhibits the expansion of granulocyte colony-forming units (CFU-G), thereby reducing eosinophils and basophils, using a method that specifically targets the Tie2 receptor to treat allergic diseases without causing general immunosuppression.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If current treatments for allergic diseases are used, then eosinophils and basophils are reduced, but general immunosuppression occurs

Engineering Contradiction:
Improveeosinophils and basophilsVSAvoidimmunosuppression
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent applies local quality by using a Tie2-specific peptide agonist that selectively targets the Tie2 receptor on hematopoietic progenitor cells to reduce eosinophils and basophils. This localized action at the Tie2 receptor level allows reduction of specific allergic inflammatory cells without causing general immunosuppression, as the peptide acts specifically on Tie2-expressing cells rather than broadly suppressing the immune system.

Inventive Principle:
Principle #3Local quality

2Quantity of substance

If general immunosuppression is used to treat allergic diseases, then eosinophils and basophils are reduced, but the underlying inflammatory responses are not addressed

Engineering Contradiction:
Improveeosinophils and basophilsVSAvoidtarget specificity
Core Design Contradiction:
Quantity of substanceVSManufacturing precision

Solution Approach 1:

The patent extracts the specific mechanism of Tie2 receptor activation from general immunosuppression. By using a peptide agonist that specifically binds to and activates Tie2, the invention isolates and targets the specific pathway responsible for eosinophil and basophil production. This extraction allows precise reduction of these cells through Tie2 activation without the broad, non-specific effects of general immunosuppression.

Inventive Principle:
Principle #2Taking out (Extraction)

3Quantity of substance

If existing therapies are used, then eosinophils and basophils are reduced, but side effects increase

Engineering Contradiction:
Improveeosinophils and basophilsVSAvoidside effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent changes the parameter of target specificity by shifting from non-specific immunosuppression to Tie2 receptor-specific activation. The peptide agonist is designed to bind with high affinity to Tie2, changing the interaction parameter from broad immune suppression to targeted receptor activation. This parameter change reduces side effects by limiting the therapeutic action to Tie2-expressing hematopoietic progenitor cells.

Inventive Principle:
Principle #35Parameter changes

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

Vasculotide effectively reduces eosinophils and basophils, ameliorating conditions such as atopic dermatitis and asthma by specifically targeting the Tie2 receptor, thereby minimizing side effects and improving disease outcomes without general immunosuppression.

Implementation Method 1

when configured as a tetramer results in the clustering of the receptor and its activation

Methodology Applied
Scientific EffectReceptor clustering:

Implementation Method 2

activate Tie2 receptor tyrosine kinase activity

Methodology Applied
Scientific EffectTyrosine kinase activation:

Implementation Method 3

inhibit the expansion of CFU-G cells, resulting in a reduction in eosinophils and basophils

Methodology Applied
Scientific EffectHematopoietic cell differentiation inhibition:

Data Source

PatentUS9186390B2Methods and uses of TIE2 binding and/or activating agents
Publication Date: 2015.11.17 SUNNYBROOK HEALTH SCI CENT
  • US9186390B2 patent drawing
  • US9186390B2 patent drawing
  • US9186390B2 patent drawing

AI summary

The present disclosure provides methods and uses of Tie2 binding and/or activating agents. In particular, the present disclosure provides methods and uses for inhibiting the expansion of colony forming unit-granulocytes, reducing eosinophils and/or basophils, for treating allergic disease or response or eosinophil/basophil associated condition and for reducing inflammatory cytokine and/or chemokine levels.