mRNA Sequences with miRNA Binding Sites for Cell-Type Specific Expression

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current methods for delivering polynucleotide sequences, such as mRNA, to specific organs and tissues face challenges in achieving effective targeting and differential expression in various cell types, leading to limitations in therapeutic efficacy and increased side effects.

Innovation Solution

An isolated mRNA sequence is designed with coding sequences for polypeptides, including untranslated regions (UTRs) and multiple micro-RNA (miRNA) binding sites, allowing for differential expression in different cell types within target organs, combined with targeted delivery particles to enhance specificity and efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If non-viral methods are used to deliver polynucleotides to cells, then safety and reduced toxicity are improved, but transfection rates and targeting efficiency deteriorate

Engineering Contradiction:
ImprovetoxicityVSAvoidtransfection rate
Core Design Contradiction:
Object-affected harmful factorsVSProductivity

Solution Approach 1:

The patent modifies the mRNA structure by incorporating specific UTR sequences and miRNA binding sites, changing the biochemical parameters of the polynucleotide to enhance cell-type specific expression and transfection efficiency while maintaining safety

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses miRNA binding sites as intermediaries that mediate between the delivered mRNA and the target cell's gene regulation machinery, enabling selective expression in desired cell types while avoiding toxicity in others

Inventive Principle:
Principle #24Intermediary (Mediator)

2Productivity

If viral vectors are used to deliver coding polynucleotides, then transfection rates and targeting ability are improved, but risks of toxicity and inflammation worsen

Engineering Contradiction:
Improvetransfection rateVSAvoidtoxicity
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent employs transient mRNA expression instead of persistent viral integration, using short-lived mRNA molecules that provide temporary therapeutic effect without the long-term safety risks of viral vectors

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

Solution Approach 2:

The patent engineers specific mRNA structural parameters including UTR sequences and miRNA binding sites to achieve viral-level transfection efficiency and cell-type specificity without invoking the immune response associated with viral vectors

Inventive Principle:
Principle #35Parameter changes

3Adaptability or versatility

If polynucleotides are delivered to achieve broad expression, then therapeutic coverage is improved, but side effects and off-target effects worsen

Engineering Contradiction:
Improvetherapeutic coverageVSAvoidside effects
Core Design Contradiction:
Adaptability or versatilityVSObject-generated harmful factors

Solution Approach 1:

The patent confers cell-type specific expression by incorporating miRNA binding sites that create local regulatory differences in the mRNA, allowing the same polynucleotide to be expressed in some cell types while silenced in others, thereby achieving targeted therapy with reduced side effects

Inventive Principle:
Principle #3Local quality

4Manufacturing precision

If differential expression in different cell types is achieved through targeted delivery, then therapeutic precision is improved, but delivery system complexity worsens

Engineering Contradiction:
Improvetargeting precisionVSAvoiddelivery system complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent extracts the targeting function from the delivery vehicle and embeds it directly into the mRNA molecule itself through incorporated miRNA binding sites, simplifying the overall delivery system while maintaining high targeting precision

Inventive Principle:
Principle #2Taking out (Extraction)

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 enables precise and controlled expression of therapeutic agents in specific cell types, improving treatment outcomes while minimizing side effects by leveraging miRNA-mediated modulation for tissue-specific translation.

Implementation Method 1

The miRNA binding site sequences allow for differential expression of the coding sequence in at least a first and a second cell type within the target organ or organs

Methodology Applied
Scientific EffectmiRNA binding: Absorption (physical)

Data Source

PatentEP4008333A1Compositions and methods for organ-protective expression and modulation of coding ribonucleic acids
Publication Date: 2022.06.08 COMBINED THERAPEUTICS INC
  • EP4008333A1 patent drawingFigure 1
  • EP4008333A1 patent drawingFigure 2
  • EP4008333A1 patent drawingFigure 3

AI summary

Provided is an isolated mRNA sequence for expression of one or more cytokines within one or more target organs, the sequence comprising at least one coding sequence which codes for one or more cytokines (or their ligands) involved in immune response and inflammation selected from one or more of: TNFα, TNFβ, IFNα, IFNβ, IFNgamma, IL1, IL2, IL3, IL4, IL5, IL6, IL7, IL8, IL9, IL10, IL11, IL12, CCL2, CCL3, CCL4, CCL5, CXCL 9, and CXCL10. The sequence also comprises at least a first untranslated region (UTR) sequence, and at least three different micro-RNA (miRNA) binding site sequences. Each of the miRNA binding site sequences is located within, immediately 5' to or immediately 3' to, the first UTR sequence; and the miRNA binding site sequences allow for differential expression of the coding sequence in at least a first and a second cell type within the target organ or organs. Also provided are pharmaceutical compositions comprising the mRNA sequence, and methods for using the sequence or composition, particularly in treatment of disease, such as cancer of the liver, brain, lung, breast, pancreas, colon and kidney.