Tetrapeptide Compositions for Dermal Collagen Protection

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Solution Overview

Problem

Existing cosmeceutical products lack effective inhibitors of serine proteases to prevent or treat signs of skin aging, particularly focusing on dermal collagen degradation, without causing cellular proliferation effects.

Innovation Solution

Development of novel tetrapeptides with a specific formula, comprising D-series amino acids, acylated at the N-terminus and optionally amidated at the C-terminus of lysine, which act as potent inhibitors of serine proteases to protect dermal collagen, formulated in cosmeceutical and pharmaceutical compositions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If MMP family enzymes are targeted as inhibitors to prevent dermal collagen degradation, then collagen degradation is inhibited, but serine protease degradation is not effectively addressed

Engineering Contradiction:

Improvecollagen degradation inhibitionVSAvoidprotease inhibition coverage

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The peptide compounds of the invention are designed to inhibit multiple protease families simultaneously, including both MMPs and serine proteases. This multi-functional inhibition approach allows a single compound to address multiple degradation pathways of dermal collagen, thereby resolving the contradiction between targeted MMP inhibition and broader protease coverage.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The invention employs peptide compounds with specific composite structures containing D-amino acids and particular side chain configurations that enable simultaneous binding to different protease families. This composite molecular design allows the single compound to function against multiple enzyme types, achieving both MMP and serine protease inhibition.

Inventive Principle:

Principle #40Composite materials

2Quantity of substance

If collagen biosynthesis is stimulated to compensate for collagen lack, then dermal collagen concentration increases, but fibroblast intervention in delicate biosynthesis processes is required

Engineering Contradiction:

Improvedermal collagen concentrationVSAvoidbiosynthesis intervention complexity

Core Design Contradiction:

Quantity of substanceVSDevice complexity

Solution Approach 1:

Instead of attempting to stimulate the complex and delicate collagen biosynthesis process in fibroblasts, the invention converts the approach to inhibit the harmful degradation processes. By targeting proteases that break down collagen, the compound allows natural collagen levels to be maintained or increased through reduced degradation, avoiding the need to intervene in complex biosynthesis pathways.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The invention inverts the conventional approach of stimulating collagen production by instead focusing on inhibiting collagen degradation. This reverse strategy achieves the same goal of increasing dermal collagen concentration but through a simpler mechanism that does not require intervention in fibroblast biosynthesis processes.

Inventive Principle:

Principle #13The other way round (Inversion)

3Reliability

If existing serine protease inhibitors are used to protect dermal collagen, then collagen degradation is reduced, but cellular proliferation effects are induced

Engineering Contradiction:

Improvecollagen protectionVSAvoidcellular proliferation effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention modifies the chemical parameters of serine protease inhibitors by incorporating D-amino acids and specific side chain configurations. These parameter changes in the molecular structure alter the interaction profile with cellular receptors, maintaining effective protease inhibition while eliminating the harmful cellular proliferation effects associated with existing inhibitors.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The peptide compounds feature specific local structural qualities, including D-amino acid residues and particular side chain arrangements, that enable selective inhibition of proteases without triggering cellular proliferation. These localized structural modifications create a differential effect where protease activity is blocked but cellular growth pathways remain unaffected.

Inventive Principle:

Principle #3Local quality

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 novel tetrapeptides demonstrate high inhibitory activity against dermal collagen degradation, enhancing collagen production and maintaining stability in vivo, effective for both physiological and pathological skin aging conditions, without inducing cellular proliferation.

Implementation Method 1

The Applicants have synthesised novel peptides having a surprisingly high inhibitory activity of serine proteases... act as potent inhibitors of serine proteases to protect dermal collagen

Methodology Applied

Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS20260008811A1Bioactive peptides and compositions comprising them

Publication Date: 2026.01.08 ESPIKEM SRL

AI summary

The present invention relates to bioactive peptides and to the cosmeceutical compositions containing them, useful for the prevention and treatment of the signs of skin aging, such as wrinkles, fine lines and loss of firmness and elasticity of the skin, thanks to their efficacy in the protection of the dermal collagen.