Cocaine-Binding Ligands Inhibit Beta-Amyloid Aggregation

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Solution Overview

Problem

Current treatments for Alzheimer's Disease are limited in effectively addressing the progression of the disease and reducing beta-amyloid peptide aggregation, with existing therapies mainly targeting neurotransmitter systems and showing only modest effects.

Innovation Solution

The use of cocaine-binding-site ligands and RNA aptamers that bind to beta-amyloid peptides to prevent aggregation, inhibit nicotinic acetylcholine receptor inhibition, and reduce tau phosphorylation, offering a unique trifunctional approach to address the major pathological processes of Alzheimer's Disease.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current Alzheimer's Disease treatments targeting neurotransmitter systems are used, then some symptomatic relief is achieved, but they show only modest effects and do not clearly affect disease progression

Engineering Contradiction:
Improveeffectiveness in modifying clinical symptomsVSAvoideffectiveness in delaying disease progression
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The invention uses ligands that bind to multiple targets simultaneously - cocaine-binding-site ligands that interact with both nicotinic acetylcholine receptors and beta-amyloid peptides. This multi-functionality allows a single compound to address both neurotransmitter deficits and amyloid aggregation, potentially achieving both symptomatic relief and disease modification that current single-target therapies cannot achieve

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Reliability

If new therapeutic agents targeting beta-amyloid aggregation are developed, then disease progression may be delayed, but the complexity of identifying effective compounds increases

Engineering Contradiction:
Improveeffectiveness in preventing beta-amyloid aggregationVSAvoidcomplexity of compound identification and screening
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention uses cocaine and its derivatives as intermediary compounds - substances with known pharmacological properties and binding characteristics that serve as starting points for developing anti-amyloid agents. This intermediary approach provides a familiar molecular framework that facilitates drug development and reduces the complexity of identifying effective compounds from scratch

Inventive Principle:
Principle #24Intermediary (Mediator)

3Ease of operation

If existing Alzheimer's treatments are administered, then some neurotransmitter-related symptoms are addressed, but they fail to prevent beta-amyloid peptide aggregation and tau phosphorylation

Engineering Contradiction:
Improveavailability of approved therapiesVSAvoidability to prevent key pathological processes
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The invention merges two previously separate therapeutic approaches - cholinergic enhancement (via nicotinic acetylcholine receptor ligands) and anti-amyloid therapy (via beta-amyloid binding compounds) - into a single unified treatment strategy. This combination approach addresses multiple pathological processes simultaneously, including neurotransmitter deficits, amyloid aggregation, and potentially tau phosphorylation, thereby preventing key pathological processes that existing single-target therapies cannot prevent

Inventive Principle:
Principle #5Merging (Combining)

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

These compounds demonstrate the potential to prevent beta-amyloid aggregation, nicotinic acetylcholine receptor inhibition, and tau phosphorylation, providing a novel therapeutic strategy for treating and preventing Alzheimer's Disease by effectively targeting key pathological processes.

Implementation Method 1

cocaine-binding-site ligands and cocaine-binding-site RNA aptamers that bind with high affinity to a site (e.g., a cocaine-binding site) on beta-amyloid peptides and prevent their aggregation

Methodology Applied
Scientific EffectMolecular binding: Adsorption

Data Source

PatentUS9233106B2Inhibition of beta-amyloid peptide aggregation
Publication Date: 2016.01.12 CORNELL RES FOUNDATION INC
  • US9233106B2 patent drawing
  • US9233106B2 patent drawing
  • US9233106B2 patent drawing

AI summary

The present invention relates to methods of using cocaine-binding-site ligands and cocaine-binding-site RNA aptamers to treat or prevent Alzheimer's Disease and to reduce or prevent aggregation of beta-amyloid peptides in a subject.