AGE-SELEX Aptamer Selection Bioactivity Resolution

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Solution Overview

Problem

Current aptamer selection methods, such as SELEX, rely solely on binding affinity and suffer from low resolution, unspecific elution, and limited yield, failing to effectively identify aptamers with specific bioactivity for in vitro or in vivo applications.

Innovation Solution

The AGE-SELEX method enhances aptamer selection by incorporating bioactivity-guided selection rounds, using mutational PCR and target variants to refine affinity and specificity, and includes bioactivity determination steps to characterize aptamers' ability to modulate biochemical or biophysical reactions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If SELEX method is used for aptamer selection, then binding affinity can be obtained, but resolution is low and unspecific elution occurs

Engineering Contradiction:
Improveselection resolutionVSAvoidspecificity of aptamer binding
Core Design Contradiction:
Measurement precisionVSReliability

Solution Approach 1:

The patent segments the selection process into distinct stages: initial SELEX for binding affinity, followed by bioactivity-guided selection rounds. This segmentation allows each stage to optimize for its specific purpose, improving overall resolution and reducing unspecific elution by separating binding selection from functional validation.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent implements feedback mechanisms by using bioactivity determination results to guide subsequent selection rounds. Aptamers showing desired bioactivity are enriched and subjected to further rounds of selection, creating a feedback loop that continuously improves specificity and reduces unspecific binding through iterative optimization.

Inventive Principle:
Principle #23Feedback

2Productivity

If SELEX method is used for aptamer selection, then binding aptamers can be identified, but yield is limited

Engineering Contradiction:
Improveaptamer yieldVSAvoidbioactivity characterization
Core Design Contradiction:
ProductivityVSMeasurement precision

Solution Approach 1:

The patent performs preliminary bioactivity screening on aptamer candidates before final selection. By assessing bioactivity early in the process, the method identifies high-yield aptamers with desired functional properties, avoiding wasted effort on aptamers that bind but lack the required bioactivity.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent changes selection parameters from binding affinity alone to include bioactivity metrics. This parameter change enables identification of aptamers that meet both binding and functional requirements, increasing the yield of truly effective aptamers while maintaining precise bioactivity characterization.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If only binding affinity is used as selection criterion, then selection process is simple, but false positives increase

Engineering Contradiction:
Improveaccuracy of aptamer selectionVSAvoidselection process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges binding affinity selection with bioactivity determination in an integrated selection process. By combining these two criteria, the method eliminates false positives that would pass binding-only selection, improving accuracy while the modular design keeps process complexity manageable.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent replaces simple mechanical binding-based selection with a more sophisticated system that incorporates biochemical activity assessment. This substitution uses enzymatic or cellular readouts to detect true functional aptamers, significantly reducing false positives despite increased process complexity.

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

Data Source

PatentEP4108770A1Age-selex method for aptamer identification and use
Publication Date: 2022.12.28 APTAMIMETICS GMBH
  • EP4108770A1 patent drawingFigure 1
  • EP4108770A1 patent drawingFigure 2
  • EP4108770A1 patent drawingFigure 3

AI summary

The invention relates to a specific SELEX based method named AGE-SELEX which includes various specific steps including at least one bioactivity determination step allowing to obtain aptamers with high bioactivity modulation properties.