Cyclic Peptides for Skin Anti-Aging via UPR Stimulation

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Solution Overview

Problem

Current anti-aging treatments for skin face challenges such as poor efficacy due to conformational flexibility and digestion by proteases, difficulty in membrane transport, and poor solubility, leading to inadequate prevention and treatment of skin aging signs.

Innovation Solution

Development of cycled peptides that increase ER chaperones expression, specifically CALR, to enhance protein folding, reduce apoptosis, and upregulate extracellular matrix components, improving skin firmness and elasticity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If linear peptides are used as anti-aging agents, then they can improve skin aging signs through collagen synthesis, but they suffer from poor efficacy due to conformational flexibility and easy digestion by proteases

Engineering Contradiction:
ImproveefficacyVSAvoidconformational flexibility
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by transforming the peptide structure from linear to cyclic configuration. This structural parameter change reduces conformational flexibility and enhances protease resistance, thereby improving efficacy while maintaining biological activity for collagen synthesis and anti-aging effects.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If peptides are used to treat skin aging, then they can stimulate collagen synthesis, but they face difficulty in transport across skin membranes and poor solubility in cosmetic vehicles

Engineering Contradiction:
Improvebiological activityVSAvoidmembrane transport
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The cyclic peptide structure represents a parameter change that improves membrane permeability and solubility characteristics. The cyclic configuration alters the physical properties of the peptide, enabling better transport across skin membranes and improved compatibility with cosmetic vehicle formulations while preserving biological activity.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP4417190A1Cyclic peptides with Anti-aging efficacy
Publication Date: 2024.08.21 LIPOTRUE SL
  • EP4417190A1 patent drawingFigure 1
  • EP4417190A1 patent drawingFigure 2A~2B
  • EP4417190A1 patent drawingFigure 3~4

AI summary

The present invention refers to cycled peptides with anti-aging activity, capable of regulate UPR in endoplasmic reticulum (ER) in response to aging, stress or ROS. Said peptides are capable of affect the expression of genes involving protein misfolding or apoptosis in the ER. Also is disclosed herein, compositions comprising said peptides and their uses in the field of cosmetics, especially against aging signs in the skin.