Antisense Oligonucleotides Modulate eIF4E-BP2 Expression

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Solution Overview

Problem

Current therapeutic agents do not effectively target eIF4E-BP2, which is involved in regulating protein synthesis and is deregulated in various diseases, including cancer and metabolic disorders.

Innovation Solution

Development of antisense compounds, specifically oligonucleotides that hybridize with nucleic acid molecules encoding eIF4E-BP2, to modulate its expression by inhibiting mRNA translation and protein synthesis.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapeutic agents are used, then treatment of diseases is provided, but eIF4E-BP2 expression cannot be effectively targeted

Engineering Contradiction:

Improveeffectiveness of targeting eIF4E-BP2VSAvoidability to target eIF4E-BP2

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs antisense oligonucleotides as intermediary molecules that specifically bind to eIF4E-BP2 mRNA, preventing its translation into protein. This intermediary approach allows selective targeting of eIF4E-BP2 without affecting other cellular components, resolving the contradiction between treatment effectiveness and target specificity.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention replaces conventional therapeutic mechanisms with a nucleic acid-based mechanism. Instead of using small molecule drugs that rely on chemical binding, the patent uses antisense oligonucleotides that exploit complementary base pairing to specifically recognize and inhibit eIF4E-BP2 expression, achieving both reliability and adaptability in targeting.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Object-affected harmful factors

If eIF4E-BP2 expression is not modulated, then normal protein synthesis regulation is maintained, but diseases associated with excessive protein synthesis cannot be treated

Engineering Contradiction:

Improveexcessive protein synthesis in diseaseVSAvoidprotein synthesis rate

Core Design Contradiction:

Object-affected harmful factorsVSProductivity

Solution Approach 1:

The patent applies partial inhibition of eIF4E-BP2 expression rather than complete suppression. By using antisense oligonucleotides at controlled concentrations, the invention achieves sufficient reduction of eIF4E-BP2 to treat diseases with excessive protein synthesis while maintaining enough expression to preserve essential cellular functions, thus balancing harm reduction with productivity maintenance.

Inventive Principle:

Principle #16Partial or excessive action

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 antisense compounds effectively inhibit eIF4E-BP2 expression, potentially treating conditions associated with excessive protein synthesis, such as cancer and metabolic disorders, by regulating translation rates and improving insulin sensitivity and glucose metabolism.

Implementation Method 1

antisense compounds, particularly oligonucleotide compounds, which, in preferred embodiments, hybridize with nucleic acid molecules encoding eIF4E-BP2

Methodology Applied

Scientific EffectHybridization:

Data Source

PatentUS7807652B2Modulation of eIF4E-BP2 expression

Publication Date: 2010.10.05 IONIS PHARMACEUTICALS INC

AI summary

Compounds, compositions and methods are provided for modulating the expression of eIF4E-BP2. The compositions comprise oligonucleotides, targeted to nucleic acid encoding eIF4E-BP2. Methods of using these compounds for modulation of eIF4E-BP2 expression and for diagnosis and treatment of diseases and conditions associated with expression of eIF4E-BP2 are provided.