IGF-1 Mimicking Peptides for Enhanced Skin Penetration and Stability

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Solution Overview

Problem

Current methods for producing insulin-like growth factor-1 (IGF-1) are time- and cost-consuming due to the need for refolding and purification processes, and IGF-1 mimicking peptides with improved characteristics such as skin penetration and stability are sought for therapeutic and cosmetic applications.

Innovation Solution

Development of IGF-1 mimicking peptides with specific amino acid sequences, including modifications like disulfide bonds and linkers, which are synthesized using solid-phase techniques to enhance stability and skin penetration, and formulated into pharmaceutical and cosmetic compositions for improved skin conditions and periodontal disease treatment.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If recombinant IGF-1 production using E. coli expression systems is used, then mass production capability is achieved, but time-consuming refolding process and complex purification process are required

Engineering Contradiction:

Improvemass production capabilityVSAvoidrefolding process time

Core Design Contradiction:

ProductivityVSLoss of time

Solution Approach 1:

The patent creates simplified copies of IGF-1's functional domains (A and B domains) that replicate the essential biological activity without requiring the complete 70-amino acid structure. These truncated peptides copy the receptor-binding functionality while eliminating the need for complex refolding processes required for full-length recombinant IGF-1 production

Inventive Principle:

Principle #26Copying

Solution Approach 2:

The patent divides the IGF-1 molecule into functional segments, specifically isolating the A domain (amino acids 42-62) and B domain (amino acids 1-29) as separate active units. This segmentation allows each domain to be produced and purified independently through simpler processes, avoiding the time-consuming refolding required for full-length recombinant IGF-1

Inventive Principle:

Principle #1Segmentation

2Productivity

If recombinant IGF-1 production using E. coli expression systems is used, then mass production capability is achieved, but complex purification process to remove E. coli-originated contaminants is required

Engineering Contradiction:

Improvemass production capabilityVSAvoidpurification process complexity

Core Design Contradiction:

ProductivityVSDevice complexity

Solution Approach 1:

The patent extracts only the essential functional domains (A and B domains) from the complete IGF-1 structure, removing the C and D domains that are not required for receptor binding activity. This extraction approach produces smaller peptides that can be purified more easily without the complex contamination removal processes needed for full-length recombinant IGF-1

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent creates simplified copies of IGF-1's functional domains that replicate the essential biological activity without requiring the complete 70-amino acid structure. These truncated peptides copy the receptor-binding functionality while eliminating the need for complex refolding processes required for full-length recombinant IGF-1 production

Inventive Principle:

Principle #26Copying

3Reliability

If natural IGF-1 is used, then identical biological function is achieved, but skin penetration and stability are insufficient

Engineering Contradiction:

Improvebiological function identityVSAvoidpeptide stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent modifies key parameters of the IGF-1 structure, including amino acid substitutions (e.g., position 44 in the A domain), cyclization to form disulfide bonds, and C-terminal modifications. These parameter changes enhance the peptide's resistance to proteolytic degradation and improve stability while preserving receptor-binding activity

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite peptide structures by combining modified amino acid sequences with disulfide bridge formations and various terminal modifications. These composite structures integrate multiple stabilizing features that collectively enhance penetration and stability while maintaining biological function

Inventive Principle:

Principle #40Composite materials

4Reliability

If natural IGF-1 is used, then identical biological function is achieved, but skin penetration capability is limited

Engineering Contradiction:

Improvebiological function identityVSAvoidpeptide length for skin penetration

Core Design Contradiction:

ReliabilityVSLength of moving object

Solution Approach 1:

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP2270039B1Peptides having activities of insulin like growth factor-1 and their uses

Publication Date: 2013.05.29 CAREGEN

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AI summary

The present invention relates to a peptide having the activity of insulin like growth factor-1 (IGF-1) and derived from IGF-1, a composition for improving skin conditions or treating a periodontal disease comprising the peptide. The IGF-I mimicking peptides of this invention have identical functions or actions to natural- occurring IGF-I and much better stability and skin permeation than natural-occurring IGF-1. In these connections, the composition comprising the peptides of this invention can exhibit excellent efficacies on the treatment, prevention and improvement of diseases or conditions demanding IGF-I activities. In addition, the peptides of this invention can be advantageously applied to pharmaceutical compositions, quasi-drugs and cosmetics.