Bivalent Binding Agent for Specific Polypeptide Detection

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Solution Overview

Problem

Current methods for detecting posttranslationally modified polypeptides face challenges such as difficulty in obtaining antibodies with high specificity and affinity, cross-reactivity issues, and the need for reproducible and high-quality binding agents that can specifically target posttranslational modifications.

Innovation Solution

A bi-valent binding agent comprising two monovalent binders linked via a linker, where the first binder targets a polypeptide epitope and the second binder targets a posttranslational modification, with each monovalent binder having a dissociation rate constant (Kdiss) in the range of 5x10^-3 to 10^-4 seconds, and the bi-valent agent having a Kdiss of 3x10^-5 seconds or less, allowing for specific detection of posttranslationally modified polypeptides.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If standard immunization and screening methods are used to generate antibodies, then binding agents can be obtained, but they show cross-reactions to other polypeptides, do not exhibit required affinity, and show cross-reactivity to non-modified polypeptide

Engineering Contradiction:
Improvespecificity of antibody bindingVSAvoiddifficulty in obtaining required immunogen in sufficient purity and quantity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The invention divides the binding task into two separate monovalent binders: one that recognizes the posttranslational modification and another that recognizes the polypeptide sequence. This segmentation allows each binder to be optimized for its specific target, improving overall specificity and reducing cross-reactivity while simplifying the manufacturing process for each individual binder.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite binding agent by combining two distinct monovalent binders (one for the modification, one for the sequence) into a single bivalent structure. This composite approach leverages the specific advantages of each binder type, achieving high specificity for modified polypeptides while avoiding the limitations of single-antibody approaches.

Inventive Principle:
Principle #40Composite materials

2Reliability

If monoclonal antibodies are produced to bind strongly to epitopes consisting of secondary modification and parts of the polypeptide, then high affinity binding is achieved, but it turns out very demanding to obtain such antibodies with reproducible and consistent quality

Engineering Contradiction:
Improvereproducibility and consistency of antibody qualityVSAvoidcomplexity of obtaining highly specific monoclonal antibodies
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention separates the recognition functions into two independent monovalent binders, eliminating the need to generate complex monoclonal antibodies that recognize combined epitopes. Each simpler binder can be produced with more consistent quality and easier reproducibility, while the bivalent combination achieves the desired high affinity and specificity.

Inventive Principle:
Principle #1Segmentation

3Measurement precision

If various types of separation and fragmentation techniques are combined with mass spectroscopy to identify posttranslationally modified polypeptide, then identification is achieved, but sophisticated tools and techniques are required

Engineering Contradiction:
Improvedetection capability of posttranslationally modified polypeptideVSAvoidsophistication of detection tools and techniques
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The invention introduces a specialized bivalent binding agent as an intermediary that specifically captures posttranslationally modified polypeptides. This binding agent serves as a selective mediator that simplifies detection by providing high-specificity binding, eliminating the need for complex separation and mass spectrometry workflows while achieving comparable or superior detection precision.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Measurement precision

If multiple antibodies with specificity for each position potentially carrying posttranslational modification are used to assess glycosylation status, then comprehensive detection is achieved, but the process becomes more complex requiring several different antibodies

Engineering Contradiction:
Improvecompleteness of glycosylation status detectionVSAvoidnumber of different antibodies required
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The bivalent binding agent design provides a universal solution where one agent can detect multiple glycosylation sites through its two binding sites: one recognizing the glycosylation modification itself and the other recognizing the polypeptide sequence. This multi-functional approach reduces the need for multiple specialized antibodies while maintaining comprehensive detection capability.

Inventive Principle:
Principle #6Universality (Multi-functionality)

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 bi-valent binding agent enables efficient and specific detection of posttranslationally modified polypeptides, reducing cross-reactivity and improving the reproducibility and quality of binding, thereby enhancing the accuracy of histological staining procedures.

Implementation Method 1

the first monovalent binder binds to a polypeptide epitope of a target polypeptide

Methodology Applied
Scientific EffectMolecular recognition:

Implementation Method 2

the second monovalent binder binds to a posttranslational polypeptide modification on the target polypeptide

Methodology Applied
Scientific EffectMolecular recognition:

Implementation Method 3

The bi-valent binding agent enables efficient and specific detection of posttranslationally modified polypeptides

Methodology Applied
Scientific EffectSpecific binding:

Data Source

PatentEP2659269B1Detection of a posttranslationally modified polypeptide by a bi-valent binding agent
Publication Date: 2016.10.26 ROCHE DIAGNOSTICS GMBH
  • EP2659269B1 patent drawingFigure 1a~1d
  • EP2659269B1 patent drawingFigure 2
  • EP2659269B1 patent drawingFigure 3

AI summary

The present invention relates to a bi-valent binding agent consisting of a first monovalent binder that binds to a polypeptide epitope of a target polypeptide, a second monovalent binder that binds to a posttranslational polypeptide modification on the target polypeptide and a linker. Further disclosed is a method for the detection of a posttranslationally modified target polypeptide by aid of such bi-valent binding agent, a method of making such bi-valent binding agent and the use of such bi-valent agent in histological staining procedures.