Caged Hapten Proximity Assay for FFPE Tissue

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Solution Overview

Problem

Current methods for detecting protein-protein interactions in formalin-fixed, paraffin-embedded tissues are not reliable or cost-effective, particularly due to the high expense and limited compatibility with automated systems of existing proximity ligation assays using DNA ligases and Phi29 DNA polymerase.

Innovation Solution

A method involving caged haptens and their conjugates with specific antibodies, where an unmasking enzyme reacts with an enzyme substrate to reveal the hapten, allowing for detection of proximal targets using chromogenic or fluorescent substrates, enabling efficient and cost-effective detection of protein interactions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If proximity ligation assay uses DNA ligases and Phi29 DNA polymerase, then protein-protein interactions can be detected in FFPE tissues, but the cost increases significantly and automation compatibility is limited

Engineering Contradiction:
Improvedetection reliabilityVSAvoidcost-effectiveness
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent replaces expensive, complex enzymes (DNA ligases and Phi29 DNA polymerase) with inexpensive, commercially available antibodies conjugated to caged haptens. The caged hapten system uses simple chemical substrates that can be detected by standard chromogenic or fluorescent methods, eliminating the need for costly proprietary enzyme systems while maintaining detection reliability in FFPE tissues.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The invention extracts and removes the expensive DNA-based enzymatic components from the proximity ligation assay, retaining only the essential function of detecting proximal protein targets. By using caged haptens that can be unmasked by proteolytic cleavage near the target protein, the system eliminates the need for DNA ligases and Phi29 polymerase, achieving cost reduction without sacrificing detection capability.

Inventive Principle:
Principle #2Taking out (Extraction)

2Reliability

If proximity ligation assay uses DNA ligases and Phi29 DNA polymerase, then protein-protein interactions can be detected in FFPE tissues, but compatibility with automated systems is reduced

Engineering Contradiction:
Improvedetection reliabilityVSAvoidautomation compatibility
Core Design Contradiction:
ReliabilityVSExtent of automation

Solution Approach 1:

The patent replaces expensive, complex enzymes (DNA ligases and Phi29 DNA polymerase) with inexpensive, commercially available antibodies conjugated to caged haptens. The caged hapten system uses simple chemical substrates that can be detected by standard chromogenic or fluorescent methods, eliminating the need for costly proprietary enzyme systems while maintaining detection reliability in FFPE tissues.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The invention substitutes the complex biochemical machinery of DNA ligases and Phi29 DNA polymerase with a simpler antibody-based recognition system combined with caged hapten chemistry. This replacement uses standard immunohistochemistry principles that are already well-established in automated pathology systems, thereby improving compatibility with automated processing while maintaining the ability to detect protein-protein interactions.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

3Ease of manufacture

If alternative technologies are used to probe molecular interactions on FFPE tissue, then cost is reduced, but reliability and effectiveness under practical use are not achieved

Engineering Contradiction:
Improvecost-effectivenessVSAvoiddetection reliability
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent segments the detection system into distinct functional components: (1) an antibody conjugated to a caged hapten that binds the first target protein, (2) a second antibody that binds the second target protein and brings it into proximity with the caged hapten, and (3) a detection system that recognizes the unmasked hapten. This segmentation allows each component to be optimized independently, ensuring both cost-effectiveness and reliability.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The caged hapten acts as an intermediary molecule that bridges the two target proteins. When the first antibody binds its target and the second antibody binds its target in proximity, the caged hapten on the first antibody is brought close to the second antibody, enabling detection through hapten-unmasking. This intermediary approach ensures reliable detection of protein-protein interactions while using cost-effective reagents.

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

This approach allows for reliable and cost-effective detection of protein-protein interactions in formalin-fixed, paraffin-embedded tissues, enhancing diagnostic capabilities and reducing the need for expensive enzymes, thereby improving the efficiency and applicability of protein interaction analysis.

Implementation Method 1

an unmasking enzyme of the second antibody-conjugated protein binding entity is capable of reacting with an enzyme substrate portion of the caged hapten to unmask the hapten

Methodology Applied
Scientific EffectEnzyme-substrate reaction: Enzyme

Implementation Method 2

a first antibody-conjugated protein binding entity specific for a first target in a sample is provided, wherein the first antibody-conjugated protein binding entity comprises a caged hapten

Methodology Applied
Scientific EffectAntigen-antibody binding: Adsorption

Implementation Method 3

allowing for detection of proximal targets using chromogenic or fluorescent substrates

Methodology Applied
Scientific EffectChromogenic reaction: Chemical Bonding

Implementation Method 4

allowing for detection of proximal targets using chromogenic or fluorescent substrates

Methodology Applied
Scientific EffectFluorescence: Fluorescence

Data Source

PatentEP3504549B1Protein proximity assay in formalin fixed paraffin embedded tissue using caged haptens
Publication Date: 2024.12.11 VENTANA MEDICAL SYSTEMS INC
  • EP3504549B1 patent drawingFigure 1A~1B
  • EP3504549B1 patent drawingFigure 1C
  • EP3504549B1 patent drawingFigure 2

AI summary

Disclosed herein are caged haptens and caged hapten-antibody conjugates useful for enabling the detection of targets located proximally to each other in a sample.