Antimicrobial Peptide Sequences Targeting Drug-Resistant Pathogens

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Solution Overview

Problem

Current antimicrobial agents are ineffective against single- or multi-drug resistant pathogens, particularly carbapenem-resistant Enterobacteriaceae, which cause significant infections and deaths, necessitating the development of new therapeutic and prophylactic strategies.

Innovation Solution

Development of antimicrobial peptides with specific amino acid sequences, including FRWRRFFRKAKRFLKRHGVSIAIGTVRLLRRFG and RRWRRFFQKAKRFVKRHGVSIAVGAYRIIG, and their variants, which can be administered to treat infections, prevent biofilm growth, promote wound healing, and diagnose or treat endotoxemia by binding to lipopolysaccharide.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antimicrobial agents are used, then they are effective against susceptible pathogens, but they are ineffective against drug-resistant pathogens including carbapenem-resistant Enterobacteriaceae

Engineering Contradiction:
Improveantimicrobial effectivenessVSAvoidspectrum of activity against resistant pathogens
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by modifying the chemical structure of antimicrobial agents through the development of novel peptides with specific amino acid sequences. These structural parameter changes enable the peptides to effectively target and disrupt drug-resistant pathogens including carbapenem-resistant Enterobacteriaceae, thereby expanding the spectrum of activity while maintaining reliability.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes composite materials by creating peptides composed of specific combinations of amino acids (such as cationic amino acids like arginine and lysine combined with hydrophobic amino acids). This composite structure at the molecular level enables the peptides to interact with and disrupt bacterial membranes of resistant pathogens, achieving both broad-spectrum activity and reliable antimicrobial effectiveness.

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If new antimicrobial peptides are developed, then broad-spectrum activity against resistant pathogens is achieved, but complexity of peptide sequence design increases

Engineering Contradiction:
Improvebroad-spectrum antimicrobial activityVSAvoidpeptide sequence design complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by establishing specific quantitative parameters for peptide design, including amino acid composition ratios (e.g., cationic amino acids comprising 20-50 mol%), peptide length (10-50 amino acids), and charge density. These defined parameter ranges simplify the design process while enabling broad-spectrum activity against resistant pathogens.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent implements local quality by incorporating specific functional regions within the peptide sequence, such as cationic amino acid-rich domains for electrostatic interaction with bacterial membranes and hydrophobic regions for membrane insertion. This localized functional organization achieves broad-spectrum activity while maintaining manageable design complexity through modular structure.

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 peptides effectively target and disrupt microbial organisms, including drug-resistant pathogens, reduce biofilm formation, and provide diagnostic capabilities, demonstrating broad-spectrum antimicrobial activity and therapeutic potential.

Implementation Method 1

The peptides effectively target and disrupt microbial organisms... by binding to lipopolysaccharide

Methodology Applied
Scientific EffectElectrostatic interaction: Electrostatics

Data Source

PatentUS12384821B2Antimicrobial peptides and compositions, methods, articles and kits relating thereto
Publication Date: 2025.08.12 GEORGE MASON UNIVERSITY
  • US12384821B2 patent drawing
  • US12384821B2 patent drawing
  • US12384821B2 patent drawing

AI summary

Peptides are described herein, in particular peptides having antimicrobial properties, as are compositions, articles, and kits comprising such peptides, and methods for using the peptides.