Modified Protein A Ligand for Protease-Resistant Chromatography

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Solution Overview

Problem

Recombinant protein A used in affinity chromatography is susceptible to protease cleavage, particularly by serine proteases and thermolysin, leading to decreased immunoglobulin-binding activity and instability as a ligand in affinity chromatography columns.

Innovation Solution

Modifying the amino acid sequence of protein A by deleting or substituting lysine at specific ligation sites and avoiding hydrophobic amino acids in ligation elements to enhance resistance to proteases, thereby maintaining immunoglobulin-binding activity and column durability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If recombinant protein A is used as an affinity ligand in chromatography, then immunoglobulin-binding activity is achieved, but the protein is susceptible to protease cleavage leading to decreased stability

Engineering Contradiction:
Improvestability of protein A as ligandVSAvoidprotease cleavage susceptibility
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the amino acid sequence of protein A at specific positions (particularly in the ligation elements connecting domains). The modification involves substituting or deleting lysine residues and avoiding hydrophobic amino acids at ligation sites, which changes the chemical parameters of the protein structure to resist protease recognition and cleavage, thereby improving stability while maintaining immunoglobulin-binding activity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent extracts and removes the vulnerable ligation elements from the protein A structure that are susceptible to protease cleavage. By identifying and modifying specific amino acid sequences at domain ligation sites (removing lysine residues and hydrophobic amino acids), the patent eliminates the weak points that proteases target, thereby protecting the overall structure from degradation

Inventive Principle:
Principle #2Taking out (Extraction)

2Reliability

If protein A is modified to enhance alkali resistance and antibody elution at weak acidic pH, then ligand function is improved, but immunoglobulin-binding activity may be reduced

Engineering Contradiction:
Improvealkali resistance and elution capabilityVSAvoidimmunoglobulin-binding activity
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent applies local quality by making targeted modifications only at specific ligation sites (domain connection regions) rather than throughout the entire protein structure. The modifications are localized to amino acid positions involved in domain ligation, leaving the immunoglobulin-binding domains intact and preserving their binding activity while improving overall stability and elution properties

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent changes specific chemical parameters at ligation sites by substituting lysine residues and removing hydrophobic amino acids from domain connection regions. These parameter changes improve alkali resistance and enable weak acidic pH elution without affecting the immunoglobulin-binding activity of the functional domains

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If lysine and cysteine residues are removed from protein A domains to enable antibody desorption at weak acidic pH, then elution capability is improved, but overall protein structure and binding activity may be affected

Engineering Contradiction:
Improveantibody desorption capabilityVSAvoidprotein structure stability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent segments the protein A structure into distinct functional regions: ligation elements (domain connection regions) and immunoglobulin-binding domains. Modifications are applied only to the ligation elements to enable weak acidic pH desorption, while the binding domains are preserved to maintain structural stability and binding activity. This segmentation allows independent optimization of different functional regions

Inventive Principle:
Principle #1Segmentation

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 modified protein A exhibits improved resistance to proteases, ensuring stable immunoglobulin-binding activity and prolonged durability as an affinity ligand, even under conditions that would typically cause cleavage, such as increased pH or high temperatures.

Implementation Method 1

a protein which has two or more domains derived from any of E, D, and A domains of protein A... having affinity to immunoglobulin

Methodology Applied
Scientific EffectAffinity binding: Adsorption

Data Source

PatentEP3255058B1Protein having affinity to immunoglobulin, and affinity separation medium and column for liquid chromatography using same
Publication Date: 2021.03.24 MITSUBISHI CHEM CORP
  • EP3255058B1 patent drawingFigure 1
  • EP3255058B1 patent drawingFigure 2
  • EP3255058B1 patent drawingFigure 3A~3C

AI summary

An object of the present invention is to provide a protein which has resistance to a serine protease or thermolysin, has an immunoglobulin-binding activity, and can be favorably used as an affinity ligand. One embodiment of the present invention is a protein having affinity for an immunoglobulin, which is a protein having two or more domains derived from any of the amino acid sequences of E, D, and A domains of protein A, and in the amino acid sequence of at least one of the domains, one or more lysines are included, and the C-terminal lysine is deleted or substituted, or a protein having affinity for an immunoglobulin, which is a protein having two or more domains derived from any of B, C, and Z domains of protein A, and in the amino acid sequence of at least one of the domains, one or more lysines are included, and lysine at position 4 and the C-terminal lysine are deleted or substituted.