Nucleic Acid Assembly pH Sensing via i-Motif Conformational Switching

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Solution Overview

Problem

Current methods for obtaining high-resolution spatiotemporal chemical maps of second messengers within cells, particularly pH, are limited by imaging artifacts and temporal resolution, and DNA-based sensors face challenges in delivering precise intracellular targeting and response times.

Innovation Solution

A nucleic acid assembly (NAA) comprising a sensor domain and handle domain, conjugated with an assembly interfaceable motif (AIM) through an artificial receptor, enables precise intracellular targeting and rapid pH sensing by forming an i-motif at acidic pH, with a recombinant antibody binding to the handle domain for trafficking and localization.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If conventional pH sensing methods (fluorescent probes, CARS, SIMS, MALDI) are used to obtain chemical maps of second messengers, then spatial resolution can be achieved, but temporal resolution deteriorates and imaging artifacts increase

Engineering Contradiction:
Improvespatial resolutionVSAvoidtemporal resolution
Core Design Contradiction:
Measurement precisionVSLoss of time

Solution Approach 1:

The patent replaces conventional imaging-based pH sensing methods (fluorescence microscopy, CARS, SIMS, MALDI) with a DNA-based nanosensor system. The DNA sensor utilizes conformational changes (i-motif formation) in response to pH changes, which are then detected through fluorescence resonance energy transfer (FRET) between donor and acceptor fluorophores attached to the DNA structure. This substitution enables both high spatial resolution (nanoscale sensing) and improved temporal resolution (real-time monitoring) while avoiding imaging artifacts associated with conventional methods.

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

2Measurement precision

If DNA-based sensors are used for pH sensing in living cells, then spatial resolution is improved, but delivery to precise intracellular locations and response time are limited

Engineering Contradiction:
Improvespatial resolutionVSAvoidresponse time
Core Design Contradiction:
Measurement precisionVSProductivity

Solution Approach 1:

The DNA sensor is divided into distinct functional domains: a pH-sensing domain that forms an i-motif structure in response to acidic pH, a handle domain for conjugation with targeting motifs, and fluorophore attachment sites for FRET-based detection. This segmentation allows each domain to be optimized independently - the sensing domain for rapid conformational response, the handle domain for efficient cellular delivery, and the fluorophores for sensitive detection - thereby improving both response time and spatial resolution simultaneously.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent optimizes the DNA sequence parameters to enhance sensing speed and delivery efficiency. The i-motif forming sequence is designed with specific cytosine repeat patterns that enable rapid conformational switching in response to pH changes. The handle domain sequence is optimized for conjugation with cell-penetrating peptides or organelle-specific targeting motifs, accelerating delivery to intracellular locations. These parameter optimizations resolve the contradiction between spatial resolution and response time.

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If fluorescent pH probes are conjugated to endocytosable ligands for intracellular targeting, then delivery to specific compartments is improved, but ligand structure or trafficking is disrupted

Engineering Contradiction:
Improveintracellular targetingVSAvoidligand trafficking
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent introduces a DNA handle domain as an intermediary between the pH-sensing i-motif structure and the cell-penetrating or targeting ligands. The handle domain serves as a modular connection point that allows ligand attachment without interfering with the pH-sensing function of the i-motif. This intermediary structure enables flexible conjugation of various targeting motifs (e.g., cell-penetrating peptides, organelle-specific sequences) while maintaining the natural trafficking behavior of the ligands and preserving their ability to deliver the sensor to specific intracellular compartments.

Inventive Principle:
Principle #24Intermediary (Mediator)

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

The NAA achieves fast response times and accurate pH mapping across various cellular compartments, overcoming previous limitations in DNA sensor delivery and response times, allowing for detailed spatiotemporal chemical mapping within living cells.

Implementation Method 1

Acidic pH causes the formation of a non-Watson-Crick based DNA motif called the I-tetraplex, or i-motif that is then transduced into a large scale conformational change of the overall DNA assembly

Methodology Applied
Scientific Effecti-motif formation:

Implementation Method 2

a recombinant antibody binding to the handle domain for trafficking and localization

Methodology Applied
Scientific EffectAntigen-antibody binding:

Implementation Method 3

The NAA achieves fast response times and accurate pH mapping across various cellular compartments

Methodology Applied
Scientific EffectpH sensing through conformational change:

Data Source

PatentEP2766485B1A nucleic acid assembly, vector, cell, methods and kit thereof
Publication Date: 2020.07.08 NAT CENT FOR BIOLOGICAL SCI
  • EP2766485B1 patent drawingFigure 1a~1g
  • EP2766485B1 patent drawingFigure 2~3b
  • EP2766485B1 patent drawingFigure 4~5c

AI summary

The present disclosure relates to a nucleic acid assembly (NAA), comprising sensor domain and handle domain; an assembly interfaceable motif (AIM) sequence optionally along with intracellular targeting motif (ITM) sequence; and an AIM- NAA complex. It also relates to a vector comprising assembly interfaceable motif sequence optionally along with intracellular targeting motif sequence and a cell comprising the vector. Further, the instant disclosure also provides a method to obtain the nucleic acid assembly, method of intracellular targeting and kit thereof.