Monomolecular Fluorescent Sensor for Protein Surface Tracking

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Solution Overview

Problem

Current fluorescent molecular sensors face challenges in tracking changes on specific protein surfaces due to high background signals in complex biochemical mixtures and within cells, and they often require significant conformational changes or labeling at specific positions, limiting their ability to detect protein modifications and binding interactions effectively.

Innovation Solution

Development of a monomolecular compound comprising a His-tag binder, a non-selective binder, and a fluorophore, where the His-tag binder selectively binds to His-tagged proteins, and the non-selective binder interacts with protein surfaces, enabling the detection of changes without requiring significant conformational changes or specific labeling, using a flexible linker and modifiable synthetic receptor to match different protein regions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If fluorescent molecular sensors utilize photo-induced electron transfer (PET), electronic energy transfer (EET), or fluorescence resonance energy transfer (FRET) processes to detect proteins, then detection sensitivity is improved, but background signal increases complicating use in complex biochemical mixtures and within cells

Engineering Contradiction:
Improvedetection sensitivityVSAvoidbackground signal
Core Design Contradiction:
Measurement precisionVSObject-generated harmful factors

Solution Approach 1:

The patent extracts the fluorescent detection function from the protein binding function by using a separate fluorophore that binds to a peptide motif on the protein surface. This allows the sensor to detect protein presence and conformational changes without the harmful background signals associated with PET/EET/FRET processes in complex biochemical mixtures.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent introduces a peptide motif as an intermediary element that mediates between the fluorophore and the protein target. The fluorophore binds to this peptide motif, which is itself bound to the protein, creating a indirect detection mechanism that reduces background signal while maintaining detection sensitivity.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Measurement precision

If genetically encoded fluorescent proteins (FPs) are used to track protein expression and localization, then spatial and temporal resolution is improved, but the large size of FPs interrupts the normal function of labeled proteins

Engineering Contradiction:
Improvespatial and temporal resolutionVSAvoidprotein function interference
Core Design Contradiction:
Measurement precisionVSObject-affected harmful factors

Solution Approach 1:

The patent segments the detection function into two separate components: a small fluorophore that binds to a peptide motif on the protein surface, rather than using a large fluorescent protein fusion. This segmentation allows the protein to maintain its native function while still enabling detection with high spatial and temporal resolution.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent uses a small, simple fluorophore that can be quickly synthesized and applied, replacing the need for complex, large fluorescent protein constructs. This small molecule approach maintains detection capability while minimizing interference with protein function.

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

3Adaptability or versatility

If small molecule-based fluorescent probes bind to short peptide motifs on proteins, then protein labeling in complex biological environments is enabled, but the ability to detect protein modifications and binding interactions is limited without significant conformational changes or specific labeling

Engineering Contradiction:
Improveprotein labeling capabilityVSAvoiddetection of protein modifications
Core Design Contradiction:
Adaptability or versatilityVSMeasurement precision

Solution Approach 1:

The patent makes the sensor system dynamic by allowing the fluorophore-peptide motif complex to respond to protein conformational changes and binding interactions. The sensor can detect these dynamic changes in protein structure and interactions, providing precise measurement of protein modifications without requiring significant conformational changes or specific labeling.

Inventive Principle:
Principle #15Dynamics

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 approach allows for the sensitive detection of protein surface modifications and binding interactions with reduced background noise, enabling the tracking of changes on specific proteins within complex environments without interfering with the protein's normal function.

Implementation Method 1

a fluorophore, which emits fluorescent light when excited

Methodology Applied
Scientific EffectFluorescence: Fluorescence

Implementation Method 2

The His-tag binder is represented by the structure of formula D... M is a metal ion

Methodology Applied
Scientific EffectCoordinate bonding: Chemical Bonding

Data Source

PatentEP3137898B1Fluorescent molecular sensor for targeting changes in protein surfaces, and methods of use thereof
Publication Date: 2023.09.20 YEDA RES & DEV CO LTD
  • EP3137898B1 patent drawingFigure 1~1c
  • EP3137898B1 patent drawingFigure 2~2c
  • EP3137898B1 patent drawingFigure 3

AI summary

This invention is directed to monomolecular sensors, comprising a selective binder, a non-selective binder and a fluorophore, which can track changes that occur on the surface of labeled proteins. This invention is further directed to the use of such sensors for identifying binding partners of specific proteins. This invention is further directed to His-tag binding compounds and uses thereof in the preparation of genetically targeted detectable molecules and sensors which can specifically bind tag-labeled proteins.