Lowered Affinity Antibodies for Specific Binding Control

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current control antibodies used in research and therapeutic applications often suffer from poorly defined variable domains, uncertain antigen specificities, and issues like cross-reactivity, making it difficult to distinguish between specific antigen-antibody interactions and nonspecific effects, which complicates the interpretation of biochemical and biological effects.

Innovation Solution

A method for producing recombinant antibodies with reduced binding affinity by identifying amino acids in the complementarity determining regions (CDRs) capable of interaction with antigens and replacing them with non-interacting amino acids without altering the overall antibody structure, resulting in a dissociation constant (KD) of greater than or equal to 10^-7 M, thereby reducing or eliminating binding interactions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If control antibodies with high binding affinity are used, then specific antigen-antibody interactions are enhanced, but cross-reactivity and nonspecific binding increase making it difficult to distinguish specific effects from nonspecific effects

Engineering Contradiction:
Improvespecificity of antigen-antibody interactionVSAvoidcross-reactivity and nonsspecific binding
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by making targeted amino acid substitutions specifically in the CDR regions of the antibody, while leaving the rest of the antibody structure intact. This allows the antibody to maintain its overall structure and Fc region functions while locally modifying the antigen-binding site to reduce affinity and eliminate cross-reactivity.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent changes the binding affinity parameter by substituting amino acids in the CDR regions with amino acids having different chemical properties (e.g., replacing aromatic amino acids like tyrosine or tryptophan with aliphatic amino acids like alanine or valine). This parameter change reduces the binding strength while maintaining the antibody's structural integrity.

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If amino acid substitutions are made in CDR regions to reduce binding affinity, then cross-reactivity is minimized, but the ability to bind target antigen is reduced

Engineering Contradiction:
Improvecross-reactivityVSAvoidspecific antigen binding
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent applies partial action by making a limited number of amino acid substitutions (typically 1-3 substitutions) in the CDR regions rather than completely eliminating binding capability. This partial modification is sufficient to reduce cross-reactivity while preserving enough binding affinity for the target antigen to maintain experimental utility.

Inventive Principle:
Principle #16Partial or excessive action

Solution Approach 2:

The patent creates modified antibody variants that copy the overall structure and framework of the parent antibody but with altered CDR sequences. These copied structures maintain the essential antibody architecture while the sequence variations eliminate cross-reactivity.

Inventive Principle:
Principle #26Copying

3Object-affected harmful factors

If multiple amino acid substitutions are made in CDR regions, then binding affinity is reduced more effectively, but the complexity of antibody design and production increases

Engineering Contradiction:
Improvenonspecific bindingVSAvoidantibody design and production complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent segments the antibody molecule by focusing modifications only on the CDR regions (specifically CDR1, CDR2, and CDR3) while leaving the framework regions and Fc portions unchanged. This segmentation allows for systematic design of multiple substitutions without overwhelming complexity, as each CDR can be independently modified.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates simplified antibody variants that can be produced through straightforward site-directed mutagenesis techniques. These modified antibodies are designed to be relatively simple to produce and characterize, making them practical tools for control experiments despite the multiple amino acid changes required.

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

Data Source

PatentEP2528948B1Novel lowered affinity antibodies and methods of making the same
Publication Date: 2018.09.19 AB BIOSCIENCES INC
  • EP2528948B1 patent drawingFigure 1
  • EP2528948B1 patent drawingFigure 2
  • EP2528948B1 patent drawingFigure 3

AI summary

The present invention provides methods for making novel, rationally designed lowered affinity antibodies. The methods of the present invention make antibodies that have variable domains that have been designed to reduce or eliminate the antigen binding activity of the parental antibody without altering the overall (3) dimensional antibody structure. Using the antibodies made using methods of the present invention in various assays allows researchers to distinguish effects that result from specific antigen-antibody interactions from other, non-specific antibody effects.