Dimeric Bacteriophage Lysins for Streptococcus Treatment

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current antibacterial approaches, particularly against Streptococcus bacteria, face challenges such as drug resistance, limited penetration through mucus linings, allergic reactions, and the need for longer treatment times due to the inefficacy of existing antibiotics and the complexity of using bacteriophages for direct treatment.

Innovation Solution

Development of dimeric phage lysins, specifically dimeric pneumococcal phage lysins like Cpl-1, which are chemically cross-linked to enhance stability and activity, allowing for prolonged bacterial killing capability and reduced plasma clearance, thereby improving treatment efficacy for Streptococcus infections.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If monomeric lysins are used, then the structure is simple and easy to manufacture, but the plasma clearance is rapid and stability is reduced

Engineering Contradiction:
Improvelys in production simplicityVSAvoidplasma stability
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent combines two monomeric lysin units to form a dimeric lysin structure. This merging of two identical or similar lysin monomers creates a larger molecular entity that exhibits reduced plasma clearance and enhanced stability compared to the monomeric form, while maintaining the bacterial cell wall targeting capability

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The dimeric lysin can be constructed using composite strategies such as fusing two lysin coding sequences with a linker peptide, or chemically cross-linking two purified lysin monomers. This creates a composite protein structure that leverages the properties of individual monomers while achieving superior pharmacokinetic properties

Inventive Principle:
Principle #40Composite materials

2Stability of the object's composition

If dimeric lysins are used, then plasma stability is improved and clearance is reduced, but the manufacturing complexity increases

Engineering Contradiction:
Improveplasma stabilityVSAvoiddimer construction complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The dimeric lysin is segmented into two distinct lysin monomer units that can be independently produced and then assembled. This segmentation allows for modular manufacturing where each monomer can be optimized separately, and the dimerization can be achieved through controlled chemical cross-linking or fusion protein expression

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

A linker peptide serves as an intermediary element that connects two lysin monomers to form a stable dimeric structure. This intermediary component facilitates the association of monomers while maintaining the functional integrity of each lysin unit, and can be designed to provide appropriate spacing and orientation for optimal activity

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If bacteriophages are used for direct treatment, then bacterial targeting is achieved, but the treatment protocol becomes complex and requires synchronized growth cycles

Engineering Contradiction:
Improvebacterial targetingVSAvoidtreatment protocol complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent extracts the active lysin enzyme from the bacteriophage system and uses it as a standalone therapeutic agent. This extraction eliminates the need for the complex phage replication cycle and synchronized growth requirements, while retaining the lysin's specific bacterial cell wall targeting capability. The lysin can be produced recombinantly and administered directly

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The lysin enzyme inherently possesses self-service capabilities through its natural affinity for bacterial cell wall components. The lysin automatically targets and binds to specific peptidoglycan structures in Streptococcus bacteria without requiring phage-mediated delivery or complex activation sequences, enabling straightforward therapeutic application

Inventive Principle:
Principle #25Self-service

4Ease of operation

If existing antibiotics are used, then treatment is simple to administer, but drug resistance develops and treatment duration increases

Engineering Contradiction:
Improveadministration simplicityVSAvoidtreatment efficacy
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent converts the previously harmful or ineffective situation of antibiotic resistance into a beneficial outcome by using a completely different mechanism of action. Instead of inhibiting bacterial growth like traditional antibiotics, the dimeric lysin directly lyzes the bacterial cell wall, a mechanism to which bacteria have not developed resistance. This transforms the resistance problem into an opportunity for effective treatment

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

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 dimeric lysins demonstrate increased bacterial killing activity and prolonged stability, potentially reducing treatment duration and allergic reactions, while maintaining effective targeting of Streptococcus bacteria, including Streptococcus pneumoniae.

Implementation Method 1

chemically cross-linked to enhance stability and activity

Methodology Applied
Scientific EffectChemical cross-linking: Chemical Bonding

Implementation Method 2

lysins that break bonds in the bacterial wall... rapidly hydrolyzes covalent bonds essential for peptidoglycan integrity

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentEP3369742B1Dimeric bacteriophage lysins
Publication Date: 2020.07.29 THE ROCKEFELLER UNIV
  • EP3369742B1 patent drawingFigure 1
  • EP3369742B1 patent drawingFigure 2(A)~2(C)
  • EP3369742B1 patent drawingFigure 3

AI summary

The present invention provides an isolated dimeric phage lysin comprising two phage lysin monomers specific for bacteria covalently linked to each other and capable of killing at least one or more Streptococcus bacteria.