Microarray Device for Functional Protein Inhibitor Screening

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Solution Overview

Problem

Current methods for screening protein inhibitors, such as fluorescence polarization and Alphascreen®, are expensive, complex, and unable to perform functional screening, as conventional microarrays only provide structural information and not functional consequences of protein binding.

Innovation Solution

A microarray device with a solid supporting element and immobilized proteins, where known inhibitors are bound with a detectable label, allowing for the screening of protein inhibitors through displacement assays with minimal material consumption and high sensitivity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Loss of information

If conventional microarrays are used for protein screening, then structural information can be obtained, but functional screening capability is lost

Engineering Contradiction:
Improvefunctional informationVSAvoidscreening capability
Core Design Contradiction:
Loss of informationVSAdaptability or versatility

Solution Approach 1:

The patent combines structural information (protein immobilization on microarray) with functional information (detectable label on inhibitor showing binding activity) into a single integrated system. The microarray simultaneously provides spatial positioning of proteins and real-time detection of inhibitor binding through fluorescence signals, resolving the contradiction between obtaining structural data and performing functional screening.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The detectable label (fluorescent marker) serves as an intermediary that bridges the gap between the inhibitor molecule and the detection system. It allows the functional binding interaction between inhibitor and protein to be visually detected and quantified, enabling functional screening capability that was previously absent in conventional microarrays.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Adaptability or versatility

If expensive methods like fluorescence polarization or Alphascreen® are used, then functional screening capability is achieved, but cost and complexity increase

Engineering Contradiction:
Improvefunctional screening capabilityVSAvoidmethod complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent creates a simplified copy of the functional screening capability found in expensive methods like Alphascreen®. By using a microarray format with immobilized proteins and detectably labeled inhibitors, it replicates the essential functional detection capability while using simpler, more cost-effective equipment and procedures that avoid the complexity of specialized instruments required by conventional methods.

Inventive Principle:
Principle #26Copying

Solution Approach 2:

The microarray uses disposable, inexpensive components (glass slides, printed proteins, fluorescent labels) to achieve functional screening, replacing the need for expensive, complex, and often reusable specialized equipment. Each microarray can be used once and then discarded, eliminating the need for costly instrument maintenance and calibration while providing comparable functional screening capability.

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

3Productivity

If high-throughput screening is performed, then productivity increases, but material consumption and cost increase

Engineering Contradiction:
Improvescreening throughputVSAvoidmaterial consumption
Core Design Contradiction:
ProductivityVSQuantity of substance

Solution Approach 1:

The patent segments the screening process into thousands of individual protein spots arranged in a grid pattern on a single microarray slide. Each spot contains a specific protein that can be screened independently, allowing high-throughput analysis of multiple proteins simultaneously while using minimal amounts of each protein and inhibitor, thus increasing productivity without proportionally increasing material consumption.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent transitions from linear or single-point screening to a two-dimensional array format, where proteins are arranged in spatial positions across the slide surface. This dimensional expansion allows parallel screening of hundreds or thousands of protein-inhibitor interactions simultaneously, dramatically increasing throughput while maintaining efficient use of reagents through the concentrated, localized nature of each interaction site.

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

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

Enables simple, cost-effective, and sensitive screening of protein inhibitors applicable to multiple disease-relevant target structures, providing functional information on protein binding interactions.

Implementation Method 1

at least one known inhibitor of the at least one protein, the inhibitor being bound to the at least one protein and comprising a detectable label

Methodology Applied
Scientific EffectMolecular binding:

Implementation Method 2

the inhibitor being bound to the at least one protein and comprising a detectable label

Methodology Applied
Scientific EffectDetectable label signal:

Data Source

PatentUS9891230B2Microarray device for screening or locating HSP90 inhibitors or inhibitors of further disease-relevant target structures
Publication Date: 2018.02.13 SARTORIUS STEDIM BIOTECH GMBH
  • US9891230B2 patent drawing
  • US9891230B2 patent drawing
  • US9891230B2 patent drawing

AI summary

The present invention relates to a microarray device for the screening or the finding of protein inhibitors, to a method for the production thereof, and to a corresponding method for screening or finding protein inhibitors. The microarray device according to the invention comprises a solid supporting element having a support material, at least one protein immobilized thereon for which inhibitors are to be screened or found, and at least one known inhibitor of the at least one protein, the inhibitor being bound to the at least one protein and comprising a detectable label.