Sol-Gel Protein Chip for High-Throughput PPI Screening

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Solution Overview

Problem

Current methods for developing low-molecular-weight inhibitors of protein-protein interactions are costly and time-consuming, making it difficult for small-scale laboratories to construct high-throughput screening systems for new drug development, particularly for screening small libraries of natural substances.

Innovation Solution

A chip-based method using a protein chip with immobilized sol-gel material and protein spots, where candidate substances are tested for their ability to inhibit protein-protein interactions by measuring binding changes with an antibody assay, allowing for efficient screening of inhibitors from natural substances or aptamers.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional high-throughput screening systems are constructed for screening protein-protein interaction inhibitors, then screening capability is improved, but cost and complexity increase significantly making it difficult for small-scale laboratories to implement

Engineering Contradiction:
Improvescreening capabilityVSAvoidsystem complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent introduces a protein chip as an intermediary platform that bridges the gap between conventional high-throughput screening and small-scale laboratory capabilities. The chip integrates multiple screening functions into a single device, allowing complex protein-protein interaction analysis without requiring elaborate screening systems. This intermediary device enables small laboratories to perform sophisticated screenings by providing a pre-integrated platform that combines sample application, interaction detection, and analysis capabilities.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention changes the scale and configuration parameters of the screening system by transitioning from large-scale automated systems to a compact chip-based platform. The protein chip uses miniaturized spots containing immobilized proteins, allowing high-density screening in a small format. This parameter change enables maintaining screening capability while dramatically reducing system complexity and cost, making it accessible to small-scale laboratories.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If conventional high-throughput screening systems are constructed for screening protein-protein interaction inhibitors, then screening capability is improved, but time and cost consumption increase

Engineering Contradiction:
Improvescreening capabilityVSAvoidscreening time
Core Design Contradiction:
ProductivityVSLoss of time

Solution Approach 1:

The protein chip employs preliminary action by pre-immobilizing multiple target proteins onto the chip surface in a structured array before actual screening begins. This pre-preparation allows candidate compounds to be directly applied and tested against multiple targets simultaneously, eliminating the need for time-consuming sequential protein preparation and interaction setup. The pre-configured chip enables rapid screening by having all interaction partners ready for immediate testing.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The invention merges multiple screening operations into a single integrated chip platform. Multiple protein targets, control elements, and detection mechanisms are combined on one chip, allowing simultaneous testing of candidate compounds against various protein-protein interactions. This consolidation eliminates the need for separate experiments for each target, dramatically reducing total screening time while maintaining comprehensive screening capability.

Inventive Principle:
Principle #5Merging (Combining)

3Measurement precision

If conventional screening methods are used for protein-protein interaction inhibitors, then comprehensive analysis is achieved, but cost-effectiveness decreases making it unsuitable for small-scale laboratories

Engineering Contradiction:
Improveanalysis comprehensivenessVSAvoidcost-effectiveness
Core Design Contradiction:
Measurement precisionVSEase of manufacture

Solution Approach 1:

The protein chip uses copying by creating miniaturized replicas of protein interaction systems on a solid support. Instead of requiring large quantities of proteins and reagents for each assay, the chip contains multiple copies of immobilized target proteins in a compact format. This allows comprehensive interaction analysis using minimal amounts of materials, significantly reducing costs while maintaining analytical comprehensiveness. The copied protein spots enable multiple measurements with small sample volumes.

Inventive Principle:
Principle #26Copying

Solution Approach 2:

The invention applies local quality by creating spatially distinct regions on the chip, each containing specific immobilized proteins with optimized local conditions for their respective interactions. Different spots on the chip can have different protein concentrations, orientations, or environmental conditions tailored to specific protein-protein interactions. This localized optimization maintains high measurement precision for each interaction type while using economical amounts of materials overall, making the system cost-effective for small laboratories.

Inventive Principle:
Principle #3Local quality

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

This method enables simple and cost-effective screening of protein-protein interaction inhibitors, suitable for small-scale laboratories, facilitating the discovery of novel natural substances that inhibit protein interactions, thereby enhancing drug development infrastructure.

Implementation Method 1

a protein chip having immobilized thereon spots comprising a mixture of a sol-gel material and a protein

Methodology Applied
Scientific EffectAdsorption: Adsorption

Data Source

PatentUS10132801B2Method for screening new drug candidate inhibiting target protein-protein interaction for development of first-in-class drug
Publication Date: 2018.11.20 DONGGUK UNIVERSITY INDUSTRY ACADEMIC COOPERATION FOUNDATION
  • US10132801B2 patent drawing
  • US10132801B2 patent drawing
  • US10132801B2 patent drawing

AI summary

The present invention relates to a method for screening a substance inhibiting protein-protein interactions, and more particularly to a method for screening a substance inhibiting protein-protein interactions, the method comprising using a protein chip having immobilized thereon spots comprising a mixture of a sol-gel material and a protein. According to the invention, a protein chip can be easily manufactured in a 96-well plate using a sol-gel material, whereby an inhibitor that inhibits protein-protein interactions can be easily screened from a library of natural substances.