Polypeptide Ligand Modulating GAG Binding Specificity

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Solution Overview

Problem

Current methods for controlling interactions between glycosaminoglycans (GAGs) and their effector molecules, such as Otx2 or Semaphorin, are inefficient and lack specificity, hindering the modification of critical periods and nervous system plasticity.

Innovation Solution

Development of a polypeptide ligand comprising a specific sequence of amino acids, including glutamic acid, aspartic acid, cysteic acid, and neutral amino acids, which can interact with GAGs to modulate the binding of effector molecules, thereby controlling critical periods and plasticity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current methods are used to control interactions between GAGs and effector molecules, then the process is simple, but the efficiency and specificity are insufficient

Engineering Contradiction:
Improvespecificity of interaction controlVSAvoidcomplexity of ligand structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The ligand is designed as a segmented polypeptide structure with repeating units of specific amino acid sequences (e.g., (ECCA)n or (ECAC)n where n=3-6). Each segment contains charged amino acids that interact with GAGs, allowing modular control of binding specificity and affinity while maintaining a relatively simple overall structure

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention controls interaction parameters by varying the amino acid sequence composition, charge distribution, and repetition number (n=3-6) of the polypeptide ligand. These parameter changes enable precise modulation of binding affinity and specificity for different GAG types without requiring complex structural modifications

Inventive Principle:
Principle #35Parameter changes

2Adaptability or versatility

If natural GAG interactions are allowed to proceed without intervention, then the system remains simple, but the ability to modify critical periods and plasticity is limited

Engineering Contradiction:
Improveability to modify critical periodsVSAvoidcontrol over effector molecule binding
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The polypeptide ligand acts as an intermediary molecule that competes with effector molecules (such as Otx2 or Semaphorin) for binding to GAGs. By introducing this mediator, the system gains control over critical period timing and nervous system plasticity while maintaining reliable and specific interactions through the ligand's designed amino acid sequence

Inventive Principle:
Principle #24Intermediary (Mediator)

3Manufacturing precision

If highly specific ligands are designed to interact with GAG-binding sites, then binding control improves, but the manufacturing complexity increases

Engineering Contradiction:
Improveprecision of binding interactionVSAvoidease of polypeptide synthesis
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

The ligand achieves high binding precision through controlled parameter changes in the amino acid sequence, specifically the repetition number (n=3-6) and composition (ECCA or ECAC units). These parameters can be precisely controlled during standard polypeptide synthesis methods, maintaining ease of manufacture while achieving the required binding precision

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

The ligand effectively interacts with GAG-binding sites on proteins like Otx2, reducing their binding to GAGs, which can reopen critical periods and enhance nervous system plasticity, offering potential therapeutic benefits for neurological disorders.

Implementation Method 1

These negatively charged groups are believed to figure prominently in the biological properties attributed to glycosaminoglycans... X comprises an amino acid selected from the group consisting of glutamic acid and aspartic acid

Methodology Applied
Scientific EffectElectrostatic interaction: Electrostatics

Data Source

PatentEP3807295B1Ligand controling interaction between gags with their effector molecules and use thereof
Publication Date: 2025.02.12 COLLEGE DE FRANCE
  • EP3807295B1 patent drawingFigure 1a~2c
  • EP3807295B1 patent drawingFigure 3a~3e
  • EP3807295B1 patent drawingFigure 4a~4c

AI summary

The invention relates to new compounds that mimic Glycosaminoglycans and are able to control interaction between Glycosaminoglycans with their effector molecules. The compounds of the invention are peptides and are able to prevent or reduce the binding of at least one effector molecule with at least one glycosaminoglycan. The compounds according to the invention can be used as drug, in particular for the stimulation of the neurogenesis and more generally to treat nervous system related pathologies.