Linker Peptides Reducing Xylose Addition for Homogeneity

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Solution Overview

Problem

Existing protein engineering techniques face challenges in producing homogeneous polypeptide preparations due to post-translational modifications, particularly the addition of xylose residues, which affect the homogeneity, stability, and aggregation of proteins.

Innovation Solution

Incorporating linker peptides with specific amino acid sequences such as (GGGGA)n GGGGS, (GGGGQ)2 GGGGS, (GGGPS)2 GGGGS, and GGGGS(PGGGS)2 that lack the GSG sequence, reducing the ability of enzymes like xylosyltransferase to add xylose, thereby enhancing protein homogeneity and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If standard linker peptides containing GSG sequence are used, then flexibility and unstructured conformation are achieved, but post-translational modifications (xylose addition) occur reducing homogeneity

Engineering Contradiction:
Improvehomogeneity of polypeptide preparationVSAvoidpost-translational modifications
Core Design Contradiction:
Stability of the object's compositionVSObject-generated harmful factors

Solution Approach 1:

The invention extracts and removes the problematic GSG sequence from the linker peptide design. By deliberately excluding this tripeptide motif, the patent eliminates the substrate recognition site for xylosyltransferase while preserving the linker's essential flexible and unstructured conformational properties through alternative glycine and serine arrangements

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention applies local quality modification by specifically altering the amino acid sequence at the linker region where post-translational modifications occur. The linker maintains its overall flexible nature through glycine and serine residues but introduces local sequence variations that prevent enzyme recognition and xylose addition, thereby achieving site-specific modification prevention without compromising global linker function

Inventive Principle:
Principle #3Local quality

2Reliability

If traditional Gly-Ser linkers are used, then domain connection and flexibility are achieved, but aggregation increases and pH stability decreases

Engineering Contradiction:
ImprovepH stability and aggregation resistanceVSAvoidlinker peptide sequence design
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention changes the primary sequence parameters of the linker peptide by modifying the specific arrangement and composition of glycine and serine residues. These parameter changes in the amino acid sequence lead to improved physical-chemical properties including reduced aggregation倾向 and enhanced pH stability, while maintaining the linker's flexible conformational characteristics

Inventive Principle:
Principle #35Parameter changes

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 use of these linker peptides results in polypeptides with reduced aggregation, increased pH stability, and improved homogeneity by minimizing post-translational modifications, leading to more consistent protein products.

Implementation Method 1

the novel linker peptides disclosed herein reduce the ability of enzymes to link carbohydrate adducts to polypeptides comprising these linker peptides, e.g., reduce the ability of xylosyltransferase to link xylose to polypeptides

Methodology Applied
Scientific EffectEnzyme-substrate interaction: Enzyme

Data Source

PatentEP2655624B1Linker peptides and polypeptides comprising same
Publication Date: 2017.11.29 BIOGEN MA INC
  • EP2655624B1 patent drawingFigure 1
  • EP2655624B1 patent drawingFigure 2
  • EP2655624B1 patent drawingFigure 3A~3B

AI summary

The invention is based, at least in part, on the finding that linker peptides which lack the amino acid sequence GSG reduce or eliminate the addition of posttranslational modifications to the polypeptides which comprise them. More specifically, the novel linker peptides disclosed herein reduce the ability of enzymes to link carbohydrate adducts to polypeptides comprising these linker peptides, e.g., reduce the ability of xylosyltransferase to link xylose to polypeptides. These novel linker peptides, molecules comprising same, and methods of their use are described.