Peptides Inhibiting Neuronal Exocytosis via SNARE Disruption
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Solution Overview
Problem
Existing treatments for skin conditions mediated by neuronal exocytosis, such as botulinum toxin derivatives, require repeated injections, cause immune reactions, and have high costs and side effects, necessitating the development of more stable and simpler molecular structures to inhibit neurotransmitter release.
Innovation Solution
Development of peptides derived from the primary structure of SNARE core complex proteins, specifically sequences of up to 20 amino acids, which inhibit neuronal exocytosis by disrupting SNARE complex assembly, including sequences like HYWRELQYR, MQVWLRMWIDYRAT, RRVVLVNNIL, LRVQMVNMFL, and WEQEFLRR, and their derivatives or salts, optionally modified with alkyl carbonyl groups or anions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If botulinum toxin derivatives are used to inhibit neurotransmitter release, then neuronal exocytosis is blocked, but immune reactions occur and repeated injections are required
Solution Approach 1:
The patent extracts the essential functional domain of botulinum toxin (inhibition of neurotransmitter release) and implements it through smaller peptide molecules that mimic the toxin's action on SNARE proteins without triggering immune responses. The peptides comprise sequences derived from the primary structure of SNARE core complex proteins, specifically targeting the SNARE complex assembly process.
Solution Approach 2:
The patent creates simplified copies of the botulinum toxin's mechanism of action using peptide sequences that replicate the toxin's ability to disrupt SNARE complex formation. These peptide copies achieve the same therapeutic effect (inhibition of acetylcholine and neuropeptide release) with significantly reduced molecular complexity and immunogenicity.
2Reliability
If botulinum toxin derivatives are used to treat skin conditions, then symptoms are improved, but treatment costs are high
Solution Approach 1:
The patent employs short-lived peptide molecules that are inexpensive to produce through synthetic methods. These peptides, comprising only 5-50 amino acids, can be manufactured cost-effectively compared to large protein toxins, enabling affordable treatment options for skin conditions while maintaining therapeutic efficacy.
Solution Approach 2:
The patent changes the molecular parameters from large protein toxins (botulinum toxin) to small peptides (5-50 amino acids), fundamentally altering the production cost structure. This parameter change enables scalable, cost-effective manufacturing while preserving the core mechanism of action for treating skin conditions.
3Reliability
If botulinum toxin derivatives are used to inhibit neurotransmitter release, then neuronal exocytosis is blocked, but side effects occur
Solution Approach 1:
The patent applies local quality by designing peptides with specific sequences derived from SNARE core complex proteins that target particular aspects of the exocytosis process. The peptides comprise sequences like HYWRELQYR, MQVWLRMWIDYRAT, RRVVLVNNIL, LRVQMVNMFL, and WEQEFLRR, which are optimized to disrupt SNARE complex assembly with minimal off-target effects.
4Object-affected harmful factors
If simple peptide structures are used to inhibit neuronal exocytosis, then immune reactions are reduced, but molecular stability may be compromised
Solution Approach 1:
The patent creates composite peptide structures that combine sequences derived from multiple SNARE core complex proteins (synaptobrevin, SNAP-25, syntaxin) into single peptide molecules. These composite peptides, comprising 5-50 amino acids, achieve enhanced stability and prolonged activity while maintaining low immunogenicity through their simplified architecture compared to full-length proteins.
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
These peptides effectively inhibit neurotransmitter release, reducing symptoms of skin conditions like wrinkles, excessive sweating, pruritus, inflammation, and wound healing without the drawbacks of existing treatments, offering a stable and cost-effective alternative.
Implementation Method 1
SNARE protein cleavage by botulinum toxins (BoNTs) disrupts vesicle fusion and neurotransmitter release. Peptides having length equal to or lower than 20 amino acids, and comprising the sequence no. ID 1, or a sequence having at least 70% sequence identity with the sequence no. ID 1, are able to inhibit, or at least reduce, the release of neurotransmitters
Data Source
AI summary
The invention relates to peptides capable of inhibiting neuronal exocytosis and to products comprising such peptides, in particular pharmaceutical and cosmetic products useful for ameliorating skin conditions, disorders and/or diseases mediated by neuronal exocytosis, such as wrinkles, excessive perspiration, pruritus, cutaneous inflammation, dermatitis, atopia, psoriasis, vascular hyperreactivity, rosacea, acne, hair growth, wound healing, calluses, warts, or sensitive skin conditions, such as ulcers and lesions on the skin..