Nucleoside Derivative with Purine-Pyrimidine Rings for Aptamer Binding

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Solution Overview

Problem

Existing natural nucleosides and their derivatives often fail to produce binding nucleic acid molecules with sufficient binding ability for certain targets, necessitating the development of modified nucleoside derivatives for applications like aptamer production.

Innovation Solution

A nucleoside derivative or its salt, represented by a specific chemical formula, is used as a building block for polynucleotide synthesis, enhancing binding ability by incorporating a purine and pyrimidine ring structure, which allows for improved interaction with targets.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If natural nucleosides and their derivatives are used for polynucleotide synthesis, then the synthesis process is simple and well-established, but the binding ability to certain targets is insufficient

Engineering Contradiction:
Improvebinding abilityVSAvoidnucleoside structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies composite materials by combining purine and pyrimidine ring structures within a single nucleoside derivative (Formula 1). This composite structural approach creates a nucleoside with enhanced binding capability that integrates multiple functional moieties, allowing the molecule to achieve superior target binding while maintaining a defined chemical structure suitable for synthesis.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent employs parameter changes by modifying the chemical structure of natural nucleosides through systematic variation of substituents (L1, L2, X1, R1 groups) at specific positions of the purine and pyrimidine rings. These structural parameter modifications enable optimization of binding affinity and specificity for target molecules, transforming ordinary nucleosides into high-performance binding agents.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If modified nucleoside derivatives are developed to enhance binding ability, then binding capability improves, but the complexity of synthesis and characterization increases

Engineering Contradiction:
Improvebinding capabilityVSAvoidsynthesis ease
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies segmentation by dividing the complex nucleoside derivative synthesis into modular components: a core nucleoside structure with systematically defined substituent positions (L1, L2, X1, R1 groups). This segmented approach allows independent optimization of each substituent while maintaining overall molecular integrity, facilitating both synthesis and characterization through modular assembly of known chemical building blocks.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS11643660B2Nucleoside derivative or salt thereof, polynucleotide synthesis reagent, method for producing polynucleotide, polynucleotide, and method for producing binding nucleic acid molecule
Publication Date: 2023.05.09 NEC SOLUTION INNOVATORS LTD
  • US11643660B2 patent drawing
  • US11643660B2 patent drawing
  • US11643660B2 patent drawing

AI summary

The present invention provides a novel nucleoside derivative or a salt thereof, a polynucleotide synthesis reagent, a method for producing a polynucleotide, a polynucleotide, and a method for producing a binding nucleic acid molecule. The nucleoside derivative or a salt thereof of the present invention is represented by the following chemical formula (1).In the chemical formula (1), Su is an atomic group having a sugar skeleton at a nucleoside residue or an atomic group having a sugar phosphate skeleton at a nucleotide residue, and may or may not have a protecting group, L1 and L2 are each independently a straight-chain or branched, saturated or unsaturated hydrocarbon group having 2 to 10 carbon atoms, X1 is an imino group (—NR1—), an ether group (—O—), or a thioether group (—S—), and R1 is a hydrogen atom or a straight-chain or branched, saturated or unsaturated hydrocarbon group having 2 to 10 carbon atoms.