NF-κB Inhibitory Peptides for Targeted Gene Modulation

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Solution Overview

Problem

Current clinical practices for treating diseases associated with NF κB dysregulation, such as inflammation and cancer, rely heavily on TNF α antagonists, which are not sufficiently effective in inhibiting NF κB activation.

Innovation Solution

Development of 4-20 residue peptides, peptide-mimetics, or peptoids that specifically inhibit NF κB activation, differentially modulating genes affected by NF κB to treat diseases and disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If TNF α antagonists are used to treat diseases involving NF κB, then treatment is provided, but the inhibition of NF κB activation is not sufficiently effective

Engineering Contradiction:

Improveeffectiveness of NF κB inhibitionVSAvoidtargeting precision

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention segments the approach by using specific peptide sequences (such as those containing the motif A-X-A-E-A-K) that target particular components or pathways within the NF κB signaling cascade, rather than using broad-spectrum TNF α antagonists. This segmentation allows for more precise inhibition of NF κB activation while maintaining therapeutic effectiveness.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The patent applies local quality by designing peptides with specific local sequences (like A-X-A-E-A-K motifs) that are tailored to interact with specific targets in the NF κB pathway. These localized sequence features provide enhanced binding affinity and specificity, improving the reliability of NF κB inhibition compared to general TNF α antagonists.

Inventive Principle:

Principle #3Local quality

2Adaptability or versatility

If broad-spectrum TNF α antagonists are used, then coverage is provided, but the therapeutic effect on NF κB dysregulation is insufficient

Engineering Contradiction:

Improvebroad coverageVSAvoidtherapeutic effectiveness

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The invention achieves universality by designing peptide inhibitors that can address multiple diseases and disorders associated with NF κB dysregulation through a common mechanism. The peptides (containing motifs like A-X-A-E-A-K) are universally applicable across various conditions including cancer, inflammatory diseases, and viral infections, providing both broad coverage and high therapeutic effectiveness.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent employs parameter changes by modifying the peptide sequence parameters (specifically incorporating the A-X-A-E-A-K motif with variable positions) to optimize both the breadth of applicability and the strength of NF κB inhibition. This allows the same peptide framework to effectively treat multiple conditions while maintaining high therapeutic effectiveness.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS20260015386A1Inhibitors of NF kappa-b activity for treatment of diseases and disorders

Publication Date: 2026.01.15 BHATNAGAR RAJENDRA SAHAI

AI summary

Peptides and methods of use thereof, are disclosed for use in treating various disease and disorders, including inflammation, pain, oral mucositis, oral lesions, and cancer. The peptides modulate the activity of the transcription factor NF κB.