Cyclic Peptides for Selective MCR-1 Agonism
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Solution Overview
Problem
There is a need for highly selective and specific melanocortin-1 receptor (MCR-1) agonist peptides for pharmaceutical applications, as existing peptides lack sufficient selectivity and specificity.
Innovation Solution
Development of cyclic peptides with specific structural formulas, including variations in amino acid sequences and substitutions, which act as selective MCR-1 ligands, allowing for effective treatment of MCR-1-mediated diseases through various administration routes, including pulmonary, nasal, and oral delivery systems.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Measurement precision
If existing melanocortin receptor peptides are used, then they can bind to melanocortin receptors, but they lack sufficient selectivity and specificity for MCR-1
Solution Approach 1:
The patent applies local quality by introducing specific amino acid substitutions at particular positions within the peptide sequence. For example, substituting naphthylalanine at position 9 and specific residues at positions 3, 6, and 10 creates localized chemical properties that confer MCR-1 selectivity while maintaining overall peptide function and stability.
Solution Approach 2:
The patent employs parameter changes by systematically varying amino acid sequences, cyclic structures, and side chain configurations to optimize MCR-1 binding affinity and selectivity. These parameter modifications transform generic melanocortin agonists into highly specific MCR-1 ligands with enhanced therapeutic properties.
2Reliability
If high doses of existing peptides are administered, then therapeutic effects can be achieved, but side effects and toxicity increase
Solution Approach 1:
The patent utilizes parameter changes by optimizing peptide sequences to achieve high MCR-1 affinity and selectivity, enabling effective therapy at low doses. This reduces exposure to off-target effects and minimizes toxicity while maintaining therapeutic efficacy through enhanced receptor specificity.
Solution Approach 2:
The patent introduces cyclic peptide structures and specific amino acid configurations that act as intermediaries to enhance MCR-1 binding selectivity. These structural modifications serve as mediators that differentiate MCR-1 from other melanocortin receptors, reducing cross-reactivity and associated side effects.
3Ease of operation
If conventional administration routes are used, then systemic delivery is achieved, but rapid local effect is limited
Solution Approach 1:
The patent applies local quality by developing peptides with optimized properties for specific administration routes. The cyclic structures and amino acid compositions are designed to facilitate rapid absorption and local action when administered via inhalation, nasal, or topical routes, while maintaining systemic availability when needed.
Solution Approach 2:
The patent employs dynamics by creating peptides with flexible yet stable cyclic structures that can adapt to different administration routes. The dynamic molecular configuration allows rapid local uptake through mucosal surfaces while maintaining stability for systemic circulation, enabling versatile and rapid therapeutic delivery.
Data Source
AI summary
Methods preventing, ameliorating or treating cytokine storm or inflammatory disease, indications, conditions and syndromes by administration of a therapeutically effective amount of a melanocortin-1 receptor-specific cyclic peptide or pharmaceutically acceptable salt thereof.