Labeled Reactants Using Linker Groups to Reduce Enzyme Interference

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Solution Overview

Problem

The presence of labeling groups in biological reactions can interfere sterically or chemically with the reaction components, leading to adverse effects such as reduced enzyme activity due to photo-chemically induced reaction intermediates.

Innovation Solution

The use of linker groups that maintain the labeling moiety at a sufficient distance from the reactive portion of the compound, typically at least 2 nm, to minimize negative impacts on the reaction, employing rigid structures like aromatic linkers or double-stranded nucleic acids to ensure the label is kept away from the active site of enzymes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Difficulty of detecting and measuring

If labeling groups are attached to model reaction constituents, then observation of the model molecules is facilitated, but the labeling groups can adversely impact the reaction being observed through steric interference or photo-chemical effects

Engineering Contradiction:
Improvedetection of model moleculesVSAvoidsteric interference and photo-chemical effects
Core Design Contradiction:
Difficulty of detecting and measuringVSObject-affected harmful factors

Solution Approach 1:

The molecule is divided into distinct functional segments: a reactive portion that participates in the biological reaction and a labeling group that facilitates detection. These segments are separated by a linker, allowing each to perform its function independently without interfering with the other.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

A linker group is introduced as an intermediary element between the reactive portion and the labeling group. This linker acts as a mediator that maintains spatial separation, preventing direct interaction between the label and reaction components while still allowing the label to be detected.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Difficulty of detecting and measuring

If large hydrophobic labeling groups are used, then detection capability is improved, but steric interference with the reaction progress is increased

Engineering Contradiction:
Improvedetection capabilityVSAvoidreaction progress
Core Design Contradiction:
Difficulty of detecting and measuringVSEase of operation

Solution Approach 1:

The labeling group is positioned in a different spatial dimension relative to the reactive portion through the use of extended linkers. This dimensional separation allows the hydrophobic label to exist without occupying the same spatial space as the reaction components, reducing steric interference.

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

3Difficulty of detecting and measuring

If fluorescent molecules are placed in close proximity to enzymatic reaction components, then detection sensitivity is improved, but enzyme activity decays due to photo-chemically induced reaction intermediates

Engineering Contradiction:
Improvedetection sensitivityVSAvoidenzyme activity
Core Design Contradiction:
Difficulty of detecting and measuringVSReliability

Solution Approach 1:

The linker serves as a protective intermediary that prevents direct contact between the fluorescent molecule and enzymatic components. This spatial buffer eliminates photo-chemical interactions while maintaining fluorescence detection capability.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces physical proximity-based detection with fluorescence-based detection. Instead of relying on the fluorescent molecule being in direct contact with the enzyme, the system uses fluorescence emission as a remote indicator of enzymatic activity, eliminating the need for close proximity.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

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 configuration reduces the negative impact of the label on enzyme activity by at least 20%, preventing photo-induced decay and maintaining enzyme functionality during reactions.

Implementation Method 1

linker groups that maintain the labeling moiety at a sufficient distance from the reactive portion of the compound, typically at least 2 nm

Methodology Applied
Scientific EffectSpatial separation through rigid linker structure:

Implementation Method 2

fluorescent labels that emit light in response to excitation by light of a different wavelength

Methodology Applied
Scientific EffectFluorescence: Fluorescence

Implementation Method 3

the presence of fluorescent molecules in close proximity to enzymatic reaction components can lead to decay in the level of enzyme activity through photo-chemically induced reaction intermediates

Methodology Applied
Scientific EffectPhoto-chemical effects: Photo-oxidation

Data Source

PatentEP2263087B1Labeled reactants and their uses
Publication Date: 2017.08.09 PACIFIC BIOSCIENCES OF CALIFORNIA INC
  • EP2263087B1 patent drawingFigure 1
  • EP2263087B1 patent drawingFigure 2
  • EP2263087B1 patent drawingFigure 3

AI summary

Labeled reactant compositions, and particularly labeled nucleic acid reaction compositions, that include structural components that maintain potentially damaging labeling components sufficiently distal from the reactant portion of the molecule such that damaging effects of the label group on other reaction components, such as enzymes, are reduced, minimized and/or eliminated.