Affinity Purification for Protein Variant Analysis

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Solution Overview

Problem

Current methods for analyzing protein variants of recombinant proteins, such as monoclonal antibodies and Fc-fusion proteins, in mammalian samples are limited by high sample volume requirements, low sensitivity, and inability to analyze individual variants effectively, particularly in pre-clinical studies where only small sample volumes are available.

Innovation Solution

A method involving affinity purification of recombinant proteins using a specific affinity ligand, followed by analysis with techniques like HPLC, capillary electrophoresis, or mass spectrometry, utilizing an internal standard to distinguish and quantify protein variants due to deamidation, oxidation, N-terminal heterogeneity, C-terminal heterogeneity, isomerization, or disulfide isoforms, allowing for high-throughput analysis in small sample volumes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If conventional analysis methods are used for protein variants in mammalian samples, then analysis can be performed, but large sample volumes are required and sensitivity is low

Engineering Contradiction:
ImprovesensitivityVSAvoidsample volume
Core Design Contradiction:
Measurement precisionVSQuantity of substance

Solution Approach 1:

The patent extracts and isolates the recombinant protein of interest from complex mammalian samples using affinity purification with immobilized affinity ligands. This extraction concentrates the target protein from large sample volumes into small eluate volumes, enabling sensitive analysis of protein variants with minimal sample consumption while maintaining high measurement precision

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the physical and chemical parameters of the sample through affinity purification, concentrating the recombinant protein by factors of 10-1000x. This parameter change from dilute to concentrated state enables detection of protein variants at very low concentrations, achieving high sensitivity with minimal sample volume

Inventive Principle:
Principle #35Parameter changes

2Measurement precision

If affinity purification is performed to isolate recombinant protein, then specificity is improved, but sample preparation complexity increases

Engineering Contradiction:
ImprovespecificityVSAvoidsample preparation
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent introduces affinity ligands as intermediaries that specifically bind to the recombinant protein of interest. These ligands are immobilized on solid supports and act as mediators to selectively capture the target protein from complex samples, achieving high specificity while simplifying the overall purification process through single-step binding

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces complex mechanical purification systems with affinity-based biochemical recognition. Instead of multiple mechanical filtration and centrifugation steps, the system uses specific molecular interactions between affinity ligands and target proteins, reducing mechanical complexity while maintaining high specificity

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

3Productivity

If high throughput analysis is implemented, then productivity is improved, but measurement precision may be compromised

Engineering Contradiction:
ImprovethroughputVSAvoidaccuracy
Core Design Contradiction:
ProductivityVSMeasurement precision

Solution Approach 1:

The patent segments the analysis process into distinct modular steps: affinity purification, sample concentration, and variant analysis. Each module can be independently optimized and performed in parallel for multiple samples, enabling high throughput while maintaining measurement precision through standardized protocols and quality control at each stage

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent develops a universal affinity purification platform that can analyze multiple types of protein variants (glycosylation, deamidation, oxidation, isomerization) using the same core methodology. This multi-functional approach enables high throughput analysis of different variant types without compromising accuracy, as the same validated protocol is applied across all analyses

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

Enables sensitive and specific analysis of protein variants in small sample volumes, facilitating the determination of pharmacokinetic parameters with high accuracy and efficiency, suitable for pre-clinical studies and clinical trials.

Implementation Method 1

immobilizing the recombinant protein of interest on a separate solid support coupled to an affinity ligand specific for the recombinant protein of interest

Methodology Applied
Scientific EffectAffinity binding: Absorption (physical)

Implementation Method 2

analyzing the protein variants using an analytic separating method such as HPLC

Methodology Applied
Scientific EffectChromatography: Chromatography

Implementation Method 3

analyzing the protein variants using an analytic separating method such as capillary electrophoresis

Methodology Applied
Scientific EffectElectrophoresis: Electrophoresis

Implementation Method 4

analyzing the protein variants using an analytic separating method such as MS

Methodology Applied
Scientific EffectMass spectrometry:

Data Source

PatentEP3196646B1Methods of mapping protein variants
Publication Date: 2019.12.18 HEXAL AG
  • EP3196646B1 patent drawingFigure 1
  • EP3196646B1 patent drawingFigure 2
  • EP3196646B1 patent drawingFigure 3

AI summary

The present invention relates to a method for analysing protein variants of a recombinant protein of interest, such as antibodies or Fc-fusion proteins, in a liquid sample of a mammal. Specifically the method comprises a step of affinity purifying the recombinant protein of interest from the sample together with an internal standard, and analyzing the protein variants using an analytic separating method such as HPLC, capillary electrophoresis or MS. This method is particularly suited to measure pharmacokinetic parameters of a recombinant protein of interest, such as a biopharmaceutical, in a mammal in clinical or pre-clinical studies. It allows for the use of a small sample volume and the possibility to operate with high throughput, such as in a 96-well plate sample preparation. It also provides high sensitivity and allows analysis of protein variants individually.