Y-Shaped DNA Aptamer Complex for VEGF Binding

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Solution Overview

Problem

Conventional aptamers for cancer treatment face limitations due to non-specific accumulation in the body, leading to toxicity and reduced efficacy in targeting cancer cells, with existing anti-VEGF drugs having uncertain efficiency, toxicity, and stability.

Innovation Solution

A highly efficient aptamer complex comprising a branched DNA, specifically a Y-shaped DNA, and an aptamer that targets vascular endothelial growth factor (VEGF), providing enhanced stability and binding efficiency, and a pharmaceutical composition for cancer treatment with improved therapeutic effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional aptamers are injected along a blood vessel for cancer treatment, then they can reach target cells, but they accumulate non-specifically in the body leading to toxicity and reduced efficacy

Engineering Contradiction:
Improvespecificity of target bindingVSAvoidtoxicity from non-specific accumulation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The aptamer is divided into multiple binding units attached to a branched DNA core structure. This segmentation allows the aptamer to present multiple binding sites simultaneously, increasing specificity for target cells while reducing non-specific accumulation through enhanced target affinity and prolonged circulation time

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention creates a composite structure combining branched DNA with multiple aptamer units. This composite design integrates the structural stability of branched DNA with the target-specific binding capability of aptamers, achieving both high specificity and reduced toxicity

Inventive Principle:
Principle #40Composite materials

2Reliability

If conventional aptamers are used for cancer treatment, then they can bind to target cells, but the effect of suppressing cancer cell growth is less than expected

Engineering Contradiction:
Improvebinding efficiency to target moleculeVSAvoidtherapeutic effect on cancer cell growth
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

Multiple aptamer units are merged into a single functional complex on the branched DNA structure. This merging creates a multi-valent binding system that significantly enhances binding efficiency to target molecules, thereby improving the therapeutic effect on cancer cell growth suppression

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The invention changes the valency parameter of the aptamer system by attaching multiple aptamer units to the branched DNA core. This parameter change from monovalent to multivalent binding increases binding strength and efficiency, leading to improved therapeutic outcomes

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 aptamer complex demonstrates improved stability and specificity in capturing VEGF, reducing tumor growth and toxicity, with enhanced therapeutic effects and prolonged in vivo stability, making it suitable for clinical applications.

Implementation Method 1

a highly efficient aptamer complex comprising a branched DNA and an aptamer

Methodology Applied
Scientific EffectDNA hybridization: Chemical Bonding

Data Source

PatentUS11414667B2High efficiency aptamer complex comprising branched DNA and aptamer, and use thereof
Publication Date: 2022.08.16 POSTECH ACADEMY INDUSTRY FOUNDATION
  • US11414667B2 patent drawing
  • US11414667B2 patent drawing
  • US11414667B2 patent drawing

AI summary

The present invention relates to a highly efficient aptamer complex comprising a branched DNA and an aptamer, and a pharmaceutical use thereof. More specifically, the aptamer complex of the present invention relates to a highly efficient aptamer complex including a Y-shaped DNA as the branched DNA and using vascular endothelial growth factor (VEGF) as a target molecule. The aptamer complex of the present invention and a pharmaceutical composition comprising the same as an active ingredient are expected to be widely used in the medical field since the binding efficiency with the target molecule is more remarkable than that of the conventional aptamer.