EphA4 Receptor Inhibitor Peptides for Memory Disorder Treatment

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Solution Overview

Problem

There is a need for an inhibitory peptide specific to the EphA receptor, particularly EphA4, to treat diseases associated with memory formation, such as post-traumatic stress disorder (PTSD), as existing solutions are inadequate in effectively addressing these conditions.

Innovation Solution

The development of peptides derived from the G-H loop of ephrin A4, which specifically bind to EphA receptors, including EphA4, to inhibit memory formation and treat related diseases, with specific sequences such as QRX1TPFX2LGFE, QRYTPFPLGFE, and QRFTPFSLGFE, potentially administered systemically or locally to target memory-related disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing inhibitory peptides are used, then general EphA receptor inhibition may be achieved, but specific and effective treatment of EphA4-related diseases (such as PTSD) is inadequate

Engineering Contradiction:
Improveeffectiveness in treating EphA4-related diseasesVSAvoidspecificity to EphA4 receptor
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies local quality by designing a peptide that specifically targets the EphA4 receptor subtype rather than broadly inhibiting all EphA receptors. The peptide sequence QRX1TPFX2LGFE is engineered to interact with unique structural features of EphA4, providing localized and selective inhibition that addresses PTSD pathology without affecting other EphA receptor functions.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention segments the EphA receptor family by creating a peptide inhibitor that selectively binds to EphA4 rather than the entire EphA family. This segmentation allows for targeted therapy that distinguishes between different EphA receptor subtypes, enabling specific treatment of EphA4-mediated pathological processes while preserving other EphA functions.

Inventive Principle:
Principle #1Segmentation

2Reliability

If peptides are administered systemically to treat memory-related disorders, then broad coverage is achieved, but targeting specific brain regions involved in memory consolidation may be reduced

Engineering Contradiction:
Improvetherapeutic efficacy in treating PTSDVSAvoidlocalization to memory-related brain regions
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The peptide acts as an intermediary molecule that bridges systemic administration and localized brain action. When administered systemically, the peptide selectively crosses the blood-brain barrier and accumulates in memory-related brain regions through receptor-specific binding to EphA4, which is highly expressed in areas such as the amygdala and hippocampus involved in fear memory consolidation.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 peptides effectively bind to EphA4 receptors, inhibiting memory formation and showing promise in treating conditions like PTSD by reducing fear-related memory consolidation, as demonstrated in animal models, indicating their potential therapeutic efficacy in humans.

Implementation Method 1

the peptides are effective in binding to EphA receptors

Methodology Applied
Scientific EffectMolecular binding:

Data Source

PatentUS9765116B2Inhibitors of the Eph-A receptor and uses thereof
Publication Date: 2017.09.19 CARMEL HAIFA UNIV ECONOMIC
  • US9765116B2 patent drawing
  • US9765116B2 patent drawing
  • US9765116B2 patent drawing

AI summary

Eph A receptor inhibitor peptides, and particularly Eph A4 receptor inhibitor peptides, are provided. The peptides comprise a sequence derived from the G-H loop of ephrin A4. Further, pharmaceutical compositions comprising said peptides and use thereof in treating, ameliorating or preventing diseases associated with memory formation are provided.