Segmented Peptidic Compounds for Proteasome Activation
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Solution Overview
Problem
Current cosmetic compositions struggle with the effectiveness of large-sized peptidic compounds as proteasome activators, making them difficult to use in the cosmetics industry for preventing and treating skin aging and UV radiation-related issues.
Innovation Solution
Development of peptidic compounds with the general formula R1—X1-Arg-Lys-Gly-X2—R2, where X1 and X2 can be specific amino acids, and R1 and R2 are protected by certain groups, which activate proteasome activity, allowing for smaller, more effective compounds for skin and keratinous appendages treatment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If large-sized peptidic compounds are used as proteasome activators, then proteasome activation effectiveness is improved, but ease of use in cosmetics and manufacturability deteriorate
Solution Approach 1:
The large peptidic compound is segmented into a smaller active core sequence (Arg-Lys-Gly with 3 amino acids) surrounded by variable amino acid residues (X1 and X2) that can be optimized for stability and activity. This segmentation allows the molecule to maintain proteasome activation effectiveness while reducing overall size for better cosmetic applicability.
Solution Approach 2:
The patent optimizes specific parameters of the peptidic compound including the identity of amino acids at positions X1 and X2, the protection groups R1 and R2, and the overall molecular size. By changing these parameters, the compound achieves both high proteasome activation effectiveness and improved ease of use in cosmetic formulations.
2Reliability
If peptidic compounds are designed for proteasome activation, then anti-aging effect is improved, but molecular size increases making them difficult to use
Solution Approach 1:
The peptidic compound is designed with a compact segmented structure where the core proteasome-active sequence (Arg-Lys-Gly) is flanked by only two variable amino acid residues (X1 and X2). This minimal segmentation maintains the essential anti-aging function while keeping the molecular length small enough for cosmetic use.
Solution Approach 2:
The patent uses protected amino acid sequences that replicate the essential functional features of larger natural peptides while being simplified copies with reduced molecular size. The protected groups R1 and R2 serve as simplified versions that maintain stability without adding excessive size.
3Reliability
If proteasome activity is increased to degrade damaged proteins, then skin aging prevention is improved, but complexity of compound structure increases
Solution Approach 1:
The compound structure is segmented into distinct functional regions: protected N-terminus (R1), variable amino acid (X1), core Arg-Lys-Gly sequence, variable amino acid (X2), and protected C-terminus (R2). This segmentation simplifies the overall structure by clearly defining each region's role while maintaining the complexity needed for selective proteasome activation.
Solution Approach 2:
The patent optimizes structural parameters including the specific amino acid identities at X1 and X2 positions, the type of protection groups R1 and R2, and the overall molecular weight. By carefully controlling these parameters, the compound achieves effective skin aging prevention without excessive structural complexity.
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 peptidic compounds increase proteasome activity, effectively degrading damaged proteins, thereby delaying skin aging and protecting against UV radiation, as demonstrated by increased enzymatic activities and cell renewal in experimental models.
Implementation Method 1
The 20S proteasome is a particle in a hollow cylinder shape, composed of 28 alpha and beta subunits, distributed in 4 heptameric rings. Peptidase activities are present on the inner surface of the cylinder and affect one another allosterically. Three proteolytic activities ('trypsin, chymotrypsin and caspase-like') have been associated with the 20S proteasome and help destroy proteins into inactive peptides with 3 to 20 amino acids.
Implementation Method 2
degradation mechanisms of proteins by proteasome are involved in significant cellular mechanisms such as DNA repair, gene expression control, cell cycle progression regulation, neosynthesized protein quality control, apoptosis or immune response
Data Source
AI summary
The present invention relates to peptidic compounds of general formula (I):R1—X1-Arg-Lys-Gly-X2—R2.In addition, the present invention relates to, on the one hand, a cosmetic or pharmaceutical composition comprising at least one peptide of general formula (I), in a cosmetically or pharmaceutically acceptable medium and, on the other hand, its utilization to prevent or treat the cutaneous signs of aging and photo-aging and to protect the skin from aggressions due to UV radiation. Lastly, the invention applies to a cosmetic treatment process intended to prevent and/or combat the cutaneous signs of aging and photo aging.