Antisense Molecules Targeting Staphylococcus aureus Ribosomal Proteins

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Solution Overview

Problem

Current treatments for Staphylococcus aureus infections, particularly methicillin-resistant Staphylococcus aureus (MRSA), are inadequate in effectively inhibiting bacterial growth and do not provide sufficient therapeutic options for targeting ribosomal proteins.

Innovation Solution

Development of antisense molecules that target Staphylococcus aureus ribosomal proteins, comprising natural and non-natural nucleic acid polymers, which hybridize to specific coding regions, are used to inhibit bacterial growth by administering them topically or systemically, often in conjunction with cell-penetrating peptides for enhanced delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for Staphylococcus aureus infections are used, then existing therapeutic options are available, but they are inadequate in effectively inhibiting bacterial growth particularly MRSA

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidtherapeutic options
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the molecular target parameter by designing antisense molecules that specifically target ribosomal protein coding regions of S. aureus, rather than using conventional antibiotics. This parameter change enables effective inhibition of bacterial growth including MRSA strains that are resistant to traditional antibiotics

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite molecular structures combining antisense oligonucleotides with cell-penetrating peptides to create a dual-function therapeutic agent. This composite approach enables both specific targeting of ribosomal proteins and effective delivery into bacterial cells, providing a versatile therapeutic option for treating S. aureus infections

Inventive Principle:
Principle #40Composite materials

2Reliability

If antisense molecules are designed to target ribosomal proteins, then specific inhibition of bacterial growth is achieved, but delivery into bacterial cells becomes challenging

Engineering Contradiction:
Improvespecificity of targetingVSAvoiddelivery efficiency
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent merges two functional components: antisense molecules for specific ribosomal protein targeting and cell-penetrating peptides for efficient cellular delivery. This combination resolves the contradiction by maintaining high targeting specificity while dramatically improving delivery efficiency into bacterial cells

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The cell-penetrating peptide acts as an intermediary that facilitates the entry of antisense molecules into bacterial cells. This mediator overcomes the cell membrane barrier, enabling the antisense molecule to reach its target ribosomal protein coding region inside the cell

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 antisense molecules effectively inhibit Staphylococcus aureus growth by specifically targeting ribosomal proteins, demonstrating significant growth inhibition in MRSA cultures, even at low concentrations, without apparent toxicity to host cells.

Implementation Method 1

hybridizes to said coding region under physiological conditions

Methodology Applied
Scientific EffectHybridization:

Data Source

PatentUS9909123B2Antisense molecules for treatment of <i>Staphylococcus aureus </i>infection
Publication Date: 2018.03.06 TECHULON
  • US9909123B2 patent drawing
  • US9909123B2 patent drawing
  • US9909123B2 patent drawing

AI summary

Disclosed are antisense molecules and compositions for the treatment of Staphylococcus aureus infection. The antisense molecules and compositions comprise nucleic acid molecules, such as RNA, DNA, or nucleic acid molecules with modified backbones, such as PNA. The antisense molecules and compositions inhibit gene expression in Staphylococcus aureus; are optionally conjugated to cell penetration molecules such as peptides; and are optionally administered in the form of a nanoparticle composition.