Neutrophil-Binding Peptides for Targeted Drug Delivery

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Solution Overview

Problem

There is an unmet need for a safe, versatile, and non-expensive platform for highly specific antibody-independent neutrophil targeting for therapeutic and diagnostic applications, particularly in cancer, infectious diseases, inflammatory diseases, and autoimmune disorders.

Innovation Solution

The development of novel peptide sequences that specifically bind to neutrophils, along with their conjugates and multimeric forms, which can be used as targeting agents for the specific in vivo delivery of therapeutic and/or diagnostic agents to neutrophils.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If antibodies specific to mouse neutrophils are administered in vivo, then neutrophil targeting is achieved, but neutrophil depletion occurs as a harmful side effect

Engineering Contradiction:
Improveneutrophil targeting specificityVSAvoidneutrophil depletion
Core Design Contradiction:
Measurement precisionVSObject-affected harmful factors

Solution Approach 1:

The patent uses peptide copies that mimic the binding specificity of anti-neutrophil antibodies but without the depleting Fc-mediated effector functions. These peptide ligands replicate the targeting capability while eliminating the harmful depletion side effect through molecular copying with modified functionality.

Inventive Principle:
Principle #26Copying

Solution Approach 2:

The invention extracts and isolates the specific binding domain (peptide ligand) from the complete antibody molecule. By taking out only the antigen-recognition portion while removing the Fc region responsible for depletion, the patent achieves selective targeting without the harmful depleting effects.

Inventive Principle:
Principle #2Taking out (Extraction)

2Reliability

If ex vivo manipulation and transplantation of neutrophils is performed, then therapeutic benefits are achieved, but the short lifetime of neutrophils creates major challenges

Engineering Contradiction:
Improvetherapeutic benefitVSAvoidneutrophil lifetime
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent applies preliminary action by conjugating therapeutic agents to neutrophils before their transplantation. This pre-loading ensures that the therapeutic payload is already attached and protected, allowing the neutrophils to deliver their payload effectively within their short lifetime without requiring extended ex vivo manipulation periods.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The invention uses peptide conjugates as intermediaries that link therapeutic agents to neutrophil surfaces. These intermediary conjugates facilitate the transfer and delivery of therapeutic payloads during the neutrophils' brief circulation time, enabling effective therapy despite the short operational window.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If in vivo manipulation of neutrophil function is performed, then therapeutic effects are achieved, but highly specific targeting is required to minimize off-target effects

Engineering Contradiction:
Improvetherapeutic effectVSAvoidtargeting specificity requirement
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies local quality by designing peptide ligands with high local affinity for specific neutrophil surface markers. This concentrated specificity at the molecular binding interface enables highly selective neutrophil targeting without requiring complex systemic targeting strategies, minimizing off-target effects through localized molecular recognition.

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

These peptide sequences and their forms enable targeted delivery to neutrophils without affecting their viability and function, offering a promising approach for treating various diseases associated with neutrophil activity.

Implementation Method 1

novel peptide sequences that specifically bind to neutrophils

Methodology Applied
Scientific EffectMolecular binding: Adsorption

Data Source

PatentEP4172173B1Neutrophil-binding peptides
Publication Date: 2025.02.19 YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD
  • EP4172173B1 patent drawingFigure 1A~1B
  • EP4172173B1 patent drawingFigure 1C~1D
  • EP4172173B1 patent drawingFigure 2A~2B

AI summary

Disclosed are peptides that specifically bind to neutrophils and uses thereof for neutrophil-targeted delivery of drugs or diagnostic agents in medical conditions including cancer as well as infectious, inflammatory and autoimmune diseases or disorders.