Semaphorin 3A Peptide for Mast Cell Apoptosis in Atopic Dermatitis

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Current therapeutic agents for atopic dermatitis and other allergic reactions have significant side effects due to long-term use, and natural proteins are unstable and costly, necessitating the development of more effective and stable alternatives.

Innovation Solution

A semaphorin 3A-derived peptide with enhanced stability and bioactivity, capable of inducing mast cell-specific apoptosis and inhibiting FcεRI signaling, is synthesized to suppress mast cell activity and reduce histamine secretion.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If natural proteins are used as therapeutic agents, then biocompatibility is improved, but stability and production costs worsen

Engineering Contradiction:

ImprovebiocompatibilityVSAvoidstability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent segments the natural protein (semaphorin 3A) into a smaller peptide fragment (amino acid sequence WVPYQARVPYPR) that retains the essential bioactivity. This segmentation maintains biocompatibility while improving stability and reducing production costs, as the peptide is more stable and easier to produce than the full-length protein.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent extracts the functional active site or critical region from the natural protein semaphorin 3A to create a minimized peptide sequence. This extracted peptide (WVPYQARVPYPR) preserves the key therapeutic function of inducing mast cell apoptosis and inhibiting FcεRI signaling while eliminating the instability and high cost associated with producing the complete protein.

Inventive Principle:

Principle #2Taking out (Extraction)

2Reliability

If steroids are used for long-term treatment, then anti-inflammatory effects are improved, but side effects worsen

Engineering Contradiction:

Improveanti-inflammatory effectsVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent employs a stable peptide therapeutic agent that can be administered repeatedly without the cumulative side effects of long-term steroid use. The peptide (WVPYQARVPYPR) provides effective anti-inflammatory action through mast cell apoptosis induction while maintaining a favorable safety profile, replacing the need for long-term steroid therapy that causes hair growth, skin thinning, and bacterial infections.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

3Reliability

If antihistamines are used for long-term treatment, then histamine blocking effects are improved, but side effects worsen

Engineering Contradiction:

Improvehistamine blocking effectsVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent provides an alternative therapeutic approach using a stable peptide that addresses the underlying mast cell activation rather than merely blocking histamine receptors. The peptide (WVPYQARVPYPR) induces mast cell apoptosis and inhibits FcεRI signaling, providing effective allergy treatment without the CNS side effects of insomnia, anxiety, and appetite loss associated with long-term antihistamine use.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

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 peptide effectively induces mast cell-specific apoptosis, inhibits mast cell activity, and improves stability and production costs, making it suitable for long-term use in medicines and cosmetics while minimizing side effects.

Implementation Method 1

The peptide effectively induces mast cell-specific apoptosis

Methodology Applied

Scientific EffectApoptosis:

Implementation Method 2

increased the expression level of caspase-3, an apoptosis-inducing protein

Methodology Applied

Scientific EffectCaspase activation:

Implementation Method 3

inhibiting FcεRI signaling

Methodology Applied

Scientific EffectReceptor signaling inhibition:

Implementation Method 4

IgE, attached to α-subunits of FcεRI, which is a IgE receptor of mast cells

Methodology Applied

Scientific EffectIgE-FcεRI binding:

Implementation Method 5

reducing histamine secretion

Methodology Applied

Scientific EffectHistamine secretion:

Implementation Method 6

the degranulation of mast cells is induced to activate the secretion of histamine

Methodology Applied

Scientific EffectDegranulation:

Data Source

PatentEP2998313B1Peptide for inducing mast cell-specific apoptosis and use thereof

Publication Date: 2018.10.10 CAREGEN

Figure 1~2a
Figure 2b~2c
Figure 3a~3b

AI summary

A peptide according to the present invention can perform a function identical or similar to the function of natural CTLA-4 and has an excellent degree of skin penetration due to a small size. The peptide according to the present invention effectively binds to antigen presenting cell surface proteins (CD80 and CD86) to inhibit activity of T cells and thus is capable of inhibiting the expression of inflammatory cytokines (for example, IL-2 and IFN-γ). As a result, a composition comprising the peptide according to the present invention exhibits excellent effects in terms of preventing, treating, or improving Th1-mediated immune diseases. Therefore, the superior activity and stability of the peptide according to the present invention can be useful when applied to medicine, quasi-drugs, and cosmetics.