Chain-Length-Tuned Nucleic Acid Binders for Pathogen Selectivity

Solution Overview

Problem

Existing nucleic acid binders (NABs) lack sufficient selectivity between pathogenic organisms and host cells, limiting their effectiveness as therapeutic agents, particularly in antimicrobial treatments and cancer therapy.

Innovation Solution

Modifying the structure of NABs by adjusting chain lengths within the compound design to enhance selectivity, resulting in improved DNA and RNA binding and potent anti-infective activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If NABs are designed to bind to both DNA and RNA of pathogenic organisms, then anti-infective activity is improved, but selectivity between pathogen and host deteriorates

Engineering Contradiction:

Improveanti-infective activityVSAvoidselectivity index

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing NABs with specific structural features (planar aromatic core with particular substituents) that enable selective binding to pathogen nucleic acids while excluding host nucleic acids. The compounds have optimized hydrophobic and hydrophilic regions that match the unique structural characteristics of bacterial or viral DNA/RNA, allowing differential binding affinity between pathogen and host targets.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying molecular parameters of the NAB structure including chain length, aromatic ring substitution patterns, and functional group composition. These parameter optimizations tune the binding affinity and selectivity, achieving compounds with enhanced pathogen selectivity while maintaining potent anti-infective activity against bacterial and viral infections.

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If broad-spectrum anti-infective agents are used, then coverage of multiple pathogen types is improved, but development of antimicrobial resistance and side effects worsen

Engineering Contradiction:

Improvebroad-spectrum coverageVSAvoidantimicrobial resistance and side effects

Core Design Contradiction:

Adaptability or versatilityVSObject-generated harmful factors

Solution Approach 1:

The patent achieves universality by designing NABs that can bind to and inhibit both DNA and RNA of diverse pathogenic organisms including bacteria, fungi, and viruses. The compounds possess dual mechanism of action (DNA binding and RNA binding) enabling them to effectively target multiple pathogen types with a single agent, providing broad-spectrum coverage while maintaining selectivity.

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Reliability

If NABs with potent activity are developed, then anti-infective effectiveness is improved, but selectivity between pathogen and host deteriorates

Engineering Contradiction:

Improvepotent anti-infective activityVSAvoidselectivity index

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing NABs with specific structural features (planar aromatic core with particular substituents) that enable selective binding to pathogen nucleic acids while excluding host nucleic acids. The compounds have optimized hydrophobic and hydrophilic regions that match the unique structural characteristics of bacterial or viral DNA/RNA, allowing differential binding affinity between pathogen and host targets.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The patent employs parameter changes by systematically varying molecular parameters of the NAB structure including chain length, aromatic ring substitution patterns, and functional group composition. These parameter optimizations tune the binding affinity and selectivity, achieving compounds with enhanced pathogen selectivity while maintaining potent anti-infective activity against bacterial and viral infections.

Inventive Principle:

Principle #35Parameter changes

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 modified NABs exhibit increased selectivity, allowing for effective treatment of various infections and cancers with reduced side effects and lower development of antimicrobial resistance.

Implementation Method 1

DNA intercalators are typically planar, aromatic compounds and are able to fit in between the base pairs of DNA

Methodology Applied

Scientific EffectIntercalation: Absorption (physical)

Implementation Method 2

groove binders are typically aromatic compounds and are able to bind to either or both of the two channels on the outer surface of double-helical DNA

Methodology Applied

Scientific EffectGroove binding: Absorption (physical)

Data Source

PatentUS20250313546A1Nucleic acid binders

Publication Date: 2025.10.09 UNIV OF STRATHCLYDE

AI summary

The present invention concerns compounds suitable as RNA or DNA binders. RNA or DNA binders are useful in the treatment of various conditions, including those caused by microbial infection and cancer. The present invention concerns specific compounds, and such compounds for use in methods of treatment, such as the treatment of antimicrobial infection and/or cancer.