Chimeric Peptide Targeting Antibiotic Resistance

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Solution Overview

Problem

Rapid evolution of antibiotic resistance in bacterial pathogens due to overuse and misuse of antibiotics leads to increased economic burden and challenges in treating drug-resistant infections, with existing antibiotics becoming less effective against pathogens like ESBL, MRSA, and VRE.

Innovation Solution

Development of novel targeting peptides and antimicrobial peptides that specifically bind to microorganisms, allowing for the creation of chimeric constructs that preferentially deliver antimicrobial agents or effectors to target organisms, thereby inhibiting their growth or killing them, including the use of peptides with specific amino acid sequences and chemical conjugation methods.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antibiotics are used to treat bacterial infections, then initial treatment effectiveness is high, but bacterial resistance develops rapidly rendering the antibiotics ineffective

Engineering Contradiction:
Improveantibiotic effectivenessVSAvoidduration of antibiotic efficacy
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The invention segments the antibiotic function into two separate components: a targeting peptide that specifically binds to the bacterial surface (providing specificity) and an antimicrobial effector that kills the bacteria (providing killing activity). This segmentation allows the targeting component to guide the effector precisely to the target, reducing off-target effects and delaying resistance development.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite chimeric molecule by covalently linking the targeting peptide to the antimicrobial effector. This composite structure combines the specific recognition capability of the peptide with the potent killing activity of the effector, producing an antibiotic with both high specificity and high efficacy that overcomes existing resistance mechanisms.

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If broad-spectrum antibiotics are used to treat infections, then coverage of multiple pathogens is achieved, but disruption to non-target microbial ecology increases

Engineering Contradiction:
Improvepathogen coverage rangeVSAvoidecological disruption to non-target microbes
Core Design Contradiction:
Adaptability or versatilityVSObject-affected harmful factors

Solution Approach 1:

The invention applies local quality by designing targeting peptides with specific amino acid sequences that recognize and bind to unique surface structures on particular bacterial species or genera. This specificity ensures that only the intended target pathogen is affected, while the surrounding microbial ecology remains preserved, thus achieving high adaptability without broad ecological disruption.

Inventive Principle:
Principle #3Local quality

3Adaptability or versatility

If existing antibiotics are refined to overcome resistance, then treatment options are extended, but the fundamental problem of resistance evolution persists

Engineering Contradiction:
Improvetreatment options availabilityVSAvoidlong-term antibiotic efficacy
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The targeting peptide acts as an intermediary that delivers the antimicrobial effector directly to the bacterial target. This intermediary mechanism bypasses traditional antibiotic resistance pathways (such as efflux pumps or enzymatic degradation) because the peptide-guided delivery system uses a different mode of action, thereby extending treatment options while maintaining long-term efficacy against resistant strains.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 peptides and chimeric constructs effectively target and inhibit a wide range of drug-resistant bacteria and fungi, reducing the growth and proliferation of pathogens such as MRSA, Aspergillus, and Candida, while minimizing disruption to non-target microbial ecology, thus offering a potential solution to the growing antibiotic resistance crisis.

Implementation Method 1

novel targeting peptides and antimicrobial peptides that specifically bind to microorganisms

Methodology Applied
Scientific EffectMolecular recognition:

Implementation Method 2

antimicrobial peptides that can be used to inhibit (e.g., kill and/or inhibit growth and/or proliferation) of certain microorganisms

Methodology Applied
Scientific EffectAntimicrobial activity:

Implementation Method 3

including the use of peptides with specific amino acid sequences and chemical conjugation methods

Methodology Applied
Scientific EffectChemical conjugation: Chemical Bonding

Data Source

PatentUS9597407B2Targeted antimicrobial moieties
Publication Date: 2017.03.21 C3 JIAN LLC
  • US9597407B2 patent drawing
  • US9597407B2 patent drawing
  • US9597407B2 patent drawing

AI summary

This invention provides novel targeted antimicrobial compositions. In various embodiments chimeric moieties are provided comprising an antimicrobial peptide attached to a peptide targeting moiety that binds a bacterial strain or species.