Gas6-LamininG Peptide Sustained-Release for Retinal Degeneration

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Solution Overview

Problem

Current treatments for retinal neurodegenerative diseases, such as AMD and RP, are ineffective due to the short biological effects of Gas6 proteins, which are prone to inactivation during sustained-release delivery, leading to complications and compliance issues with repeated sub-retinal injections.

Innovation Solution

Development of a small molecular weight active peptide, Gas6-LamininG, with biological characteristics similar to Gas6 full-length proteins, capable of enhancing phagocytic functions of retinal pigment epithelium, suitable for sustained-release delivery and long-term therapeutic effects, combined with MerTK for synergistic promotion of RPE functions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If Gas6 full-length proteins are used for treatment, then therapeutic potential is improved, but biological stability deteriorates due to inactivation during sustained-release delivery

Engineering Contradiction:
Improvetherapeutic potentialVSAvoidbiological stability
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent segments the Gas6 protein into a peptide fragment (residues 1-561) that retains biological activity while improving stability. This segmentation allows the therapeutic substance to maintain its functional properties while avoiding the inactivation issues of the full-length protein during sustained-release delivery.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent changes the molecular weight parameter from the full-length Gas6 protein to a smaller peptide fragment. This parameter change results in a substance that is less susceptible to inactivation during production and delivery processes, while still maintaining the necessary biological activity for enhancing RPE phagocytic functions.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If repeated sub-retinal injections are administered, then therapeutic effect is improved, but harmful factors increase due to complications and compliance issues

Engineering Contradiction:
Improvetherapeutic effectVSAvoidcomplications and compliance issues
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent enables continuous therapeutic action through sustained-release delivery of the peptide fragment. The small molecular weight and improved stability allow the substance to maintain therapeutic effects over extended periods, eliminating the need for repeated injections and reducing compliance burden on patients.

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The patent employs a peptide fragment that can be delivered through a single sustained-release formulation, replacing the need for multiple repeated injections. This approach reduces the cumulative harm from repeated procedures while maintaining effective therapeutic action throughout the treatment period.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Duration of action of moving object

If sustained-release delivery is implemented, then duration of action is improved, but reliability deteriorates due to inactivation of macromolecular substances

Engineering Contradiction:
Improveduration of actionVSAvoidbiological activity
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The patent segments the Gas6 protein into a peptide fragment that is specifically suited for sustained-release delivery. This segmentation creates a molecule that maintains its biological activity throughout the extended release period without the inactivation problems that affect full-length proteins during the same delivery process.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS11040086B2Active peptide for enhancing the phagocytic functions of retinal pigment epithelium and a use thereof
Publication Date: 2021.06.22 BEIJING TONGREN HOSPITAL AFFILIATED TO CAPITAL MEDICAL UNIV
  • US11040086B2 patent drawing
  • US11040086B2 patent drawing
  • US11040086B2 patent drawing

AI summary

An active peptide for enhancing the phagocytic functions of retinal pigment epithelium and a use thereof, which belongs to the technical field of preparing drugs for treating retinal neurodegenerative diseases, are described. The amino acid sequence of the active peptide for enhancing the phagocytic functions of retinal pigment epithelium described in the disclosure was as shown in SEQ ID NO.1. The active peptide of the present invention has biological characteristics similar to those of Gas6 full-length proteins, with an effect of enhancing the phagocytic functions of retinal pigment epithelium.