Interference Peptides Inhibit SARS-CoV-2 Spike Protein Binding

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Solution Overview

Problem

Current therapies and vaccines are not approved for treating SARS-CoV-2 infections, highlighting the need for effective antiviral medicaments.

Innovation Solution

The use of interference peptides such as SL8, FG8, DL12, RK4, SD6, HF7, and QK8, which inhibit the binding of the SARS-CoV-2 spike protein to the transferrin receptor, are employed in the preparation of an anti-SARS-CoV-2 medicament, with these peptides being conveniently prepared and low-cost.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional therapies and vaccines are used, then treatment of SARS-CoV-2 infection is attempted, but no approved therapy or vaccine exists to effectively treat the infection

Engineering Contradiction:
Improveeffectiveness of SARS-CoV-2 treatmentVSAvoidavailability of approved medicaments
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The invention segments the viral spike protein into specific peptide sequences (interference peptides) that can be independently synthesized and tested. This segmentation allows for rapid identification of effective antiviral peptides without requiring whole-virus vaccines or complex antibody formulations, directly addressing the lack of approved therapies.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The interference peptides are designed as short-lived, easily synthesized molecular entities that can be rapidly produced at low cost. These peptides serve as disposable therapeutic agents that can be quickly manufactured and deployed, overcoming the unavailability of approved medicaments through a streamlined production approach.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

2Reliability

If interference peptides are designed to inhibit spike protein binding, then antiviral effectiveness is improved, but the complexity of peptide design and selection increases

Engineering Contradiction:
Improveantiviral effectivenessVSAvoidpeptide design complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention performs preliminary computational modeling and in silico screening to predict which peptide sequences will effectively inhibit spike protein binding. This preliminary action filters out ineffective candidates before experimental synthesis, reducing the overall complexity of the design process while maintaining high antiviral effectiveness.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The interference peptides act as intermediary molecules that block the interaction between the viral spike protein and host cell receptors. By designing these intermediary peptides based on known binding interfaces, the complexity of viral entry inhibition is simplified to a focused peptide-receptor blocking mechanism.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 interference peptides significantly inhibit the binding of the SARS-CoV-2 spike protein to the transferrin receptor, effectively treating SARS-CoV-2-infected cells and reducing viral infection, as verified by surface plasmon resonance and protein-protein docking analysis.

Implementation Method 1

the interference peptides include: SL8, FG8, DL12, RK4, SD6, HF7, and/or QK8; the SL8 has an amino acid sequence as shown in SEQ ID NO. 1, the FG8 has an amino acid sequence as shown in SEQ ID NO. 2, the DL12 has an amino acid sequence as shown in SEQ ID NO. 3, the RK4 has an amino acid sequence as shown in SEQ ID NO. 4, the SD6 has an amino acid sequence as shown in SEQ ID NO. 5, the HF7 has an amino acid sequence as shown in SEQ ID NO. 6, and the QK8 has an amino acid sequence as shown in SEQ ID NO. 7

Methodology Applied
Scientific EffectProtein-protein binding inhibition:

Implementation Method 2

as verified by surface plasmon resonance and protein-protein docking analysis

Methodology Applied
Scientific EffectSurface plasmon resonance:

Implementation Method 3

as verified by surface plasmon resonance and protein-protein docking analysis

Methodology Applied
Scientific EffectProtein-protein docking:

Data Source

PatentUS12076364B2Use of interference peptide in preparation of anti-SARS-CoV-2 medicament
Publication Date: 2024.09.03 KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI
  • US12076364B2 patent drawing
  • US12076364B2 patent drawing
  • US12076364B2 patent drawing

AI summary

An agent for inhibiting binding of transferrin receptor to SARS-CoV-2 spike protein or an anti-SARS-CoV-2 medicament is provided, where active pharmaceutical ingredients of the agent or the medicament include interference peptides, and the interference peptides include: SL8, FG8, DL12, RK4, SD6, HF7, and/or QK8.