AptuBody DNA Oligonucleotide Aptamer MUC1 Targeting

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Solution Overview

Problem

Current treatments for cancer, autoimmune diseases, and infectious diseases often face challenges in effectively targeting and eliminating pathogenic cells due to limitations in activating the immune system, particularly the complement system, without causing harm to normal tissues.

Innovation Solution

Development of artificial chemical entities, known as AptuBodies, which consist of a biomarker-bonding portion that selectively binds to specific biomarkers and an immune-response trigger, positioning the antibody Fc region in proximity to activate the complement system, thereby triggering targeted immune responses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments are used to eliminate pathogenic cells, then immune system activation is attempted, but normal tissues are harmed due to lack of selectivity

Engineering Contradiction:

Improveselectivity of immune activationVSAvoidharm to normal tissues

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The treatment approach is segmented into two distinct functional components: a targeting module (aptamer) that selectively binds to pathogenic cell markers, and an immune activation module (antibody Fc region) that triggers complement system activation. This segmentation allows selective immune activation only at sites where the biomarker is present, avoiding harm to normal tissues.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The aptamer-antibody conjugate serves as an intermediary molecule that bridges the gap between selective target recognition and immune system activation. The aptamer portion provides selective binding to pathogenic cells, while the antibody Fc region mediates complement system activation, thereby enabling selective immune response without directly exposing the immune system to normal tissues.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Productivity

If the complement system is activated without targeted delivery, then immune response is triggered, but specificity is lost and normal cells are affected

Engineering Contradiction:

Improveimmune response activationVSAvoidtargeting accuracy

Core Design Contradiction:

ProductivityVSMeasurement precision

Solution Approach 1:

The immune activation capability is localized to specific regions where pathogenic cells express the target biomarker. The aptamer portion ensures that the conjugate accumulates selectively at these locations, and the antibody Fc region then activates the complement system only in these localized areas, maintaining both high immune response productivity and precise targeting accuracy.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The aptamer portion performs preliminary selective binding to the biomarker on pathogenic cells before the immune activation function is executed. This preliminary targeting action ensures that subsequent complement system activation occurs only at the correct location, maintaining both immune response effectiveness and targeting precision.

Inventive Principle:

Principle #10Preliminary action

3Reliability

If traditional antibody therapies are used, then immune response is triggered, but the complexity of production and purification increases

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidproduction complexity

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The therapeutic agent is constructed as a composite molecule combining an aptamer (synthetic oligonucleotide) with an antibody Fc region. This composite structure integrates the targeting capability of aptamers with the immune activation capability of antibodies, achieving high therapeutic effectiveness while simplifying production compared to traditional whole-antibody therapies, as the Fc region can be produced recombinantly with consistent quality.

Inventive Principle:

Principle #40Composite materials

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

AptuBodies induce targeted cell death in pathogenic cells by activating the complement system, reducing the risk of harming normal cells and offering a novel therapeutic approach for cancer, autoimmune diseases, and infectious diseases.

Implementation Method 1

an oligonucleotide aptamer strand configured to selectively bind to a MUC1 antigen

Methodology Applied

Scientific EffectMolecular recognition and binding:

Implementation Method 2

an immune-response trigger that under in vivo conditions leads to positioning of an antibody Fc region in proximity of the biomarker to which the biomarker-bonding portion is bound

Methodology Applied

Scientific EffectComplement system activation:

Data Source

PatentUS11299740B2Artificial chemical entity comprising a DNA oligonucleotide aptamer that selectively binds MUC1 antigen

Publication Date: 2022.04.12 NUSUM OFER

AI summary

Disclosed are artificial chemical entities, pharmaceutical compositions comprising such chemical entities and methods using the chemical entities. In some embodiments, the artificial chemical entity comprises a biomarker-bonding portion that selectively binds to a specified biomarker and an immune-response trigger that under in vivo conditions leads to positioning of an antibody Fc region in proximity of the biomarker to which the biomarker-bonding portion is bound.