Cysteine-Optimized Stradomers for Aggregation Control

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Solution Overview

Problem

Recombinant anti-inflammatory and anti-autoimmune agents face challenges due to cysteine residues not involved in disulfide bond formation, which can lead to unwanted chemical modifications and aggregation, reducing the stability and functionality of stradomers.

Innovation Solution

Development of cysteine-optimized multimerizing stradomer units with point mutations at specific amino acid positions, reducing the number of cysteine residues while maintaining multimerization and function, thereby minimizing unwanted oxidation reactions and aggregation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If cysteine residues are present in stradomers, then multimerization and function are maintained, but unwanted chemical modifications and aggregation occur

Engineering Contradiction:
Improvestradomer functionVSAvoidchemical modifications and aggregation
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent removes problematic cysteine residues from the stradomer sequence while preserving the essential multimerization capability. Specific cysteines at positions 5, 11, 14, 152, 210, 237, 240, and 243 are eliminated through point mutations, extracting the harmful chemical reactivity while maintaining the functional core structure

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the amino acid composition parameters by substituting cysteine residues with alternative amino acids at specific positions. This parameter change reduces the chemical reactivity and aggregation propensity while preserving the multimerization function through careful selection of replacement residues

Inventive Principle:
Principle #35Parameter changes

2Object-generated harmful factors

If cysteine residues are reduced in stradomers, then chemical modifications and aggregation are minimized, but multimerization and function may be reduced

Engineering Contradiction:
Improvechemical modificationsVSAvoidstradomer function
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent applies local quality by making site-specific modifications only at particular cysteine positions (5, 11, 14, 152, 210, 237, 240, 243) while leaving other regions intact. This localized approach eliminates harmful cysteines in aggregation-prone regions while preserving cysteines or structural features necessary for multimerization and biological function

Inventive Principle:
Principle #3Local quality

3Stability of the object's composition

If point mutations are introduced at specific amino acid positions, then cysteine residues are reduced and stability is improved, but sequence complexity increases

Engineering Contradiction:
Improvestradomer stabilityVSAvoidamino acid sequence
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent segments the cysteine elimination strategy into specific, discrete position targets (5, 11, 14, 152, 210, 237, 240, 243). Rather than attempting global cysteine removal, the approach divides the problem into manageable site-specific mutations, making the sequence design systematic and controllable

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP3464347B1Cysteine-optimized stradomers
Publication Date: 2023.05.31 GLIKNIK INC
  • EP3464347B1 patent drawingFigure 1
  • EP3464347B1 patent drawingFigure 2
  • EP3464347B1 patent drawingFigure 3~4

AI summary

The present disclosure involves biologically active proteins termed cysteine-optimized multimerizing stradomers. Thus, the present disclosure provides compositions and methods providing anti-autoimmune and anti-inflammatory activities, useful in the treatment of diseases and conditions including autoimmune diseases, inflammatory diseases, or infectious diseases.