Sialidase Treatment and Charge-to-Mass Separation for Unusual Glycan Analysis

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Solution Overview

Problem

Unusual modifications to glycans such as sulfation, phosphorylation, and multi-acetylated sialylation are often overlooked in glycoprotein analysis due to their complexity and instability, despite being biologically relevant.

Innovation Solution

A method involving the release of glycans and sialic acids from a therapeutic glycoprotein composition using sialidase treatment, followed by chromatographic separation based on charge-to-mass ratio to identify and quantify unusually modified glycans like sulfated, phosphorylated, and multi-acetylated sialylated glycans.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If conventional glycan analysis methods are used, then common glycan modifications (sialylation) can be detected, but unusual modifications (sulfation, phosphorylation, multi-acetylated sialylation) are overlooked due to analysis complexity and modification instability

Engineering Contradiction:
Improvedetection accuracy of unusual glycan modificationsVSAvoidcomplexity of analysis method
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The analysis method is segmented into distinct stages: (1) selective release of sialic acids using sialidase treatment, (2) separation of released sialic acids from remaining glycans, (3) analysis of unusually modified sialic acids. This segmentation allows focused detection of unusual modifications without being overwhelmed by the complexity of analyzing entire glycoprotein structures.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

Sialidase is used as an intermediary enzyme to selectively cleave and release sialic acid residues from glycoproteins. This intermediary step converts complex glycoprotein structures into simpler, separable components, enabling detection of unusual sialic acid modifications that would otherwise be masked within the complex glycan structure.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Loss of information

If conventional analysis methods are used, then analysis process is simpler, but detection of unusual glycan modifications is incomplete due to instability and complexity of these modifications

Engineering Contradiction:
Improveinformation loss of unusual modificationsVSAvoiddifficulty in detecting unusual modifications
Core Design Contradiction:
Loss of informationVSDifficulty of detecting and measuring

Solution Approach 1:

The method performs preliminary sialidase treatment to release sialic acids before analysis. This preliminary action stabilizes the unusual modifications by isolating them as free sialic acid residues, preventing further degradation or modification that would occur in the intact glycoprotein structure, thereby preserving information about unusual modifications.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The method changes the chemical state parameter of sialic acids by converting them from bound residues within glycans to free residues through enzymatic cleavage. This parameter change enables the use of separation techniques like ion exchange chromatography that can resolve and detect unusual modifications based on their altered charge properties.

Inventive Principle:
Principle #35Parameter changes

3Measurement precision

If sialidase treatment and chromatographic separation are used, then unusual modified glycans can be identified and quantified, but the analysis process becomes more complex

Engineering Contradiction:
Improvequantification accuracy of unusually modified glycansVSAvoidcomplexity of separation and quantification process
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The method replaces direct analysis of complex intact glycoproteins with an enzymatic approach using sialidase treatment. This substitution transforms the analytical problem from separating complex glycoprotein species to separating simpler sialic acid residues, which can be resolved using standard chromatographic techniques with better precision.

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

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 method allows for the effective identification and quantification of biologically relevant unusual glycan modifications, enhancing the analysis of therapeutic glycoproteins and improving understanding of their biological functions.

Implementation Method 1

exposing the therapeutic glycoprotein composition to at least one agent that cleaves sialic acid residues

Methodology Applied
Scientific EffectEnzyme catalysis: Enzyme

Implementation Method 2

subjecting the glycan preparation to a chromatographic separation technique that separates glycans based on charge to mass ratio

Methodology Applied
Scientific EffectChromatography: Chromatography

Data Source

PatentEP2358731B1Methods related to modified glycans
Publication Date: 2016.03.09 MOMENTA PHARMACEUTICALS INC
  • EP2358731B1 patent drawingFigure 1
  • EP2358731B1 patent drawingFigure 2
  • EP2358731B1 patent drawingFigure 3

AI summary

Among other things, the present disclosure provides methods for enriching, identifying, and/or quantifying unusually modified glycans (e.g., phosphorylated glycans, sulfated glycans, and/or multi-acetylated glycans). In many embodiments, methods comprise providing a glycan preparation from which sialic acids have been released; subjecting the sialidase-treated glycan preparation to a separation technique that separates glycans based on charge-to-mass ratio; and quantifying the charged products using at least one quantification standard.