FAST Tag Reversible Chromophore Binding for Rapid Fluorescent Labeling

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Solution Overview

Problem

Current fluorescent protein-based probes for imaging in living cells face limitations such as slow maturation, oxygen dependency, photobleaching, and size-related functional perturbations, which hinder real-time observation of protein dynamics with high spatial and temporal resolution.

Innovation Solution

A functional derivative of Photoactive Yellow Protein (PYP) that binds reversibly to a fluorogenic chromophore, allowing for rapid fluorescence switching and enhanced photostability, with specific kinetic constants for binding and dissociation, enabling efficient and specific labeling of proteins without interfering with their function.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If GFP-like fluorescent proteins are used for labeling, then the fluorescence can be genetically encoded with absolute specificity, but the maturation process is slow (40 minutes to 2 hours) and requires molecular oxygen

Engineering Contradiction:
Improvespecificity of fluorescent labelingVSAvoidmaturation time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The invention extracts the fluorophore synthesis function from the protein tag itself. Instead of the tag generating its own fluorophore through slow autocatalytic processes, the system uses a separate small-molecule fluorogenic probe that binds to the tag. This separates the genetic encoding function (which provides specificity) from the fluorophore generation function (which now occurs rapidly through probe binding), resolving the contradiction between specificity and maturation speed.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention introduces an intermediary small-molecule fluorogenic probe that acts as a mediator between the genetically encoded tag and the fluorescent signal. The tag serves as an anchor for the probe, while the probe provides the fluorophore function. This intermediary approach allows the system to benefit from both the genetic specificity of the tag and the rapid binding kinetics of the probe, avoiding the slow maturation and oxygen dependency of autocatalytic fluorophore generation.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If GFP-like fluorescent proteins are used, then the fluorophore is covalently formed within the protein, but the photostability is limited with half-times between 5 and 200 seconds

Engineering Contradiction:
ImprovephotostabilityVSAvoidcontinuous observation time
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The invention changes the chemical nature of the fluorophore from a covalently bound protein-based chromophore to a non-covalently bound small-molecule fluorogenic probe. This parameter change in the fluorophore's chemical structure and binding mode fundamentally alters the photostability characteristics. The probe-based system achieves superior photostability because the probe can be replenished from the cellular pool after photobleaching, and the non-covalent binding allows for faster exchange kinetics that prevent permanent damage accumulation.

Inventive Principle:
Principle #35Parameter changes

3Measurement precision

If the fluorescent tag is fused to the protein of interest, then specific labeling is achieved, but the tag may perturb the function, folding, or localization of the native protein

Engineering Contradiction:
Improvespecificity of protein detectionVSAvoidfunctional compatibility with native protein
Core Design Contradiction:
Measurement precisionVSAdaptability or versatility

Solution Approach 1:

The invention extracts the fluorophore-generating capability from a large protein tag and replaces it with a minimal peptide-based binding domain. This dramatically reduces the size of the fusion tag (from 25-30 kDa for GFP to much smaller peptide sequences), minimizing the perturbation to the native protein's function, folding, and localization while retaining the ability to provide specific genetic encoding for targeted labeling.

Inventive Principle:
Principle #2Taking out (Extraction)

4Illumination intensity

If organic fluorophores are used for fluorescence microscopy, then high brightness and specificity are achieved, but photobleaching occurs after a limited number of excitation-emission cycles

Engineering Contradiction:
Improvebrightness of fluorophoreVSAvoidresistance to photobleaching
Core Design Contradiction:
Illumination intensityVSReliability

Solution Approach 1:

The invention implements a discard-and-recover mechanism for the fluorophore. When the fluorogenic probe bound to the tag undergoes photobleaching, it is discarded (loses its fluorescent capability). However, the tag remains intact and can rapidly bind a fresh probe from the cellular pool, effectively recovering the fluorescent signal. This continuous renewal process eliminates the permanent signal loss that occurs with covalently attached fluorophores, enabling long-term observation while maintaining high brightness.

Inventive Principle:
Principle #34Discarding and recovering

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 solution provides a tunable and highly dynamic fluorescent labeling system that overcomes the limitations of existing probes, allowing for real-time imaging with reduced photobleaching and minimal functional disruption, enabling multiplexing and efficient protein tracking in various biological systems.

Implementation Method 1

binds reversibly a fluorogenic chromophore

Methodology Applied
Scientific EffectReversible binding:

Implementation Method 2

fluorescent labeling system that overcomes the limitations of existing probes

Methodology Applied
Scientific EffectFluorescence: Fluorescence

Implementation Method 3

capable of enhancing the brightness of the said fluorogenic chromophore upon complexation

Methodology Applied
Scientific EffectFluorescence enhancement: Fluorescence

Implementation Method 4

inducing the spectral shift of the said fluorogenic chromophore through the ionization of an auxochromic group thereof

Methodology Applied
Scientific EffectSpectral shift:

Implementation Method 5

inducing the spectral shift of the said fluorogenic chromophore through the ionization of an auxochromic group

Methodology Applied
Scientific EffectIonization: Ionisation

Data Source

PatentEP3164411B1Fluorogen activating and shifting tag (FAST)
Publication Date: 2019.08.28 PARIS SCI & LETTRES QUARTIER LATIN
  • EP3164411B1 patent drawingFigure 1~2
  • EP3164411B1 patent drawingFigure 3~4
  • EP3164411B1 patent drawingFigure 5

AI summary

The present invention relates to a functional derivative of a Photoactive Yellow Protein (PYP), or a functional fragment thereof, for fluorescently labelling particles, e.g. proteins, or surfaces, which is capable of binding reversibly a fluorogenic chromophore of formula (I), and which is capable of enhancing the brightness of the said fluorogenic chromophore upon complexation thereto; and of inducing the spectral shift of the said fluorogenic chromophore through the ionization of an auxochromic group thereof.