Modified Gamma-MSH Peptides for Skin Photo-Protection

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current methods for preventing UV damage and skin cancer, such as using lotions with organic compounds, are inadequate due to inefficiencies and improper use, and there is a need for a more effective internal stimulation of skin protection.

Innovation Solution

Development of modified melanocortin 1 receptor (MC1R) peptide ligands, specifically derivatives of γ-MSH, that are more selective, stable, and bioavailable for topical or transdermal delivery to stimulate melanin production and provide internal photo-protection without the need for sunlight exposure.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If modified γ-MSH peptides are used, then selectivity for MC1R and stability are improved, but complexity of peptide modification increases

Engineering Contradiction:
Improveselectivity and stabilityVSAvoidpeptide modification complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by systematically modifying specific amino acid residues in the γ-MSH peptide sequence (positions 2, 3, 5, 6, 8, 10) to optimize selectivity for MC1R and enhance stability. These targeted parameter changes in the peptide structure resolve the contradiction by improving reliability through controlled modifications rather than comprehensive complexity.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If conventional sunscreen lotions are used, then UV absorption is provided, but effectiveness is reduced due to inadequate application and short duration

Engineering Contradiction:
ImproveUV damage protectionVSAvoidprotection duration
Core Design Contradiction:
Object-affected harmful factorsVSDuration of action of moving object

Solution Approach 1:

The modified γ-MSH peptides enable self-service protection by directly stimulating melanocytes to produce endogenous melanin, which provides long-lasting internal protection. This eliminates the need for repeated external application of sunscreen lotions, resolving the contradiction between protection effectiveness and duration by making the protective mechanism self-sustaining through biological activation.

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent applies preliminary action by pre-stimulating melanin production before UV exposure occurs. The modified peptides activate MC1R receptors in advance, triggering melanin synthesis that provides protective pigmentation prior to and during UV exposure, thereby extending the effective protection duration beyond what conventional lotions can provide.

Inventive Principle:
Principle #10Preliminary action

3Object-generated harmful factors

If γ-MSH is modified for improved selectivity, then side effects are reduced, but bioavailability challenges increase

Engineering Contradiction:
Improveside effectsVSAvoidbioavailability
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent resolves this contradiction by carefully selecting amino acid substitutions that simultaneously improve MC1R selectivity (reducing side effects) and maintain or enhance peptide stability and bioavailability. Specific parameter changes in the peptide sequence are optimized to balance selectivity improvements with bioavailability requirements.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The modified γ-MSH peptides can be formulated as composite delivery systems or conjugates that enhance bioavailability while maintaining selectivity. The patent explores composite approaches to deliver the modified peptides effectively to target tissues, resolving the bioavailability challenge without compromising the reduced side effect profile.

Inventive Principle:
Principle #40Composite materials

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 MC1R peptide ligands effectively stimulate melanin production, offering enhanced protection against UV damage and reducing the risk of skin cancer with improved stability and selectivity for the MC1R receptor, providing a more effective and long-lasting solution compared to traditional sunscreens.

Implementation Method 1

The melanocortin 1 receptor (MC1R), also known as a melanocyte-stimulating hormone receptor, a melanin-activating peptide receptor, or a melanotropin receptor, is a protein that can bind to MSH

Methodology Applied
Scientific EffectReceptor binding:

Implementation Method 2

eumelanin, which is a type of melanin that can protect the skin from damage caused by UV radiation in sunlight

Methodology Applied
Scientific EffectUV absorption: Absorption (EM radiation)

Data Source

PatentEP3297655B1Enhanced melanoma cancer prevention by novel melanotropins
Publication Date: 2020.04.15 THE ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIV OF ARIZONA
  • EP3297655B1 patent drawingFigure 1~2
  • EP3297655B1 patent drawingFigure 3
  • EP3297655B1 patent drawing

AI summary

A gamma-melanocyte stimulating hormone (γ-MSH) derivative having improved stability, selectivity and bioavailabilty. The γ-MSH derivative is selective for the melanocortin-1 receptor (MC1 R) and is deliverable to skin cells via topical or transdermal delivery. The γ-MSH derivative is made up of naturally occurring amino acids for stimulating melanin from within for photo- protection of human skin against ultraviolet radiation damage.