Composite Expression Cassette for High-Level Target Gene Expression

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current gene therapy methods face challenges in achieving high titer, efficient expression of target genes in target cells, specific integration into host chromosomes, and reducing immune responses, particularly for conditions like hereditary angioedema, which requires a minimum C1-INH protein concentration of 112 µg/ml for therapeutic effect.

Innovation Solution

An expression cassette with a specific structure (Z1-Z2-Z3-Z4-Z5-Z6-Z7-Z8) is developed, comprising elements like HCR, DSE, TPL, eMlp, intron, and poly(A), optimized for high expression and low side-effects, integrated into an AAV-based gene delivery system for long-term expression.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional gene therapy methods are used, then gene delivery can be achieved, but the expression level of target genes is insufficient to reach therapeutic concentration

Engineering Contradiction:
ImproveC1-INH protein concentrationVSAvoidtherapeutic effectiveness
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent combines multiple enhancer elements (HCR, DSE, TPL, eMlp) and intron elements into a single expression cassette to achieve synergistic enhancement of gene expression. This merging of multiple functional elements allows the system to overcome the limitation of individual elements and achieve the high expression levels needed for therapeutic effectiveness.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The expression cassette is constructed as a composite structure containing multiple different functional elements (enhancers, introns, promoter regions) that work together to maximize gene expression. This composite approach allows each element to contribute its specific function, resulting in cumulative enhancement that achieves therapeutic protein concentrations.

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If high dose gene therapy is administered to achieve therapeutic protein levels, then expression level increases, but immune responses are triggered

Engineering Contradiction:
Improvetarget gene expression levelVSAvoidimmune response
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent optimizes the expression cassette parameters including enhancer combinations, intron sequences, and promoter regions to achieve high expression efficiency at lower dosages. By changing these molecular parameters, the system can reach therapeutic protein levels without requiring high doses that would trigger immune responses.

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If gene therapy is administered to achieve curative effect, then therapeutic benefit is achieved, but long-term stable expression and specific integration are not achieved

Engineering Contradiction:
Improvetherapeutic protein concentrationVSAvoidlong-term expression stability
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The patent uses AAV vectors as intermediaries to deliver the optimized expression cassette to target cells. AAV provides site-specific integration capability and long-term stable expression, acting as a mediator between the therapeutic gene and the host genome, thereby achieving both therapeutic effectiveness and long-term stability.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP4613861A1Expression cassette for target gene and use thereof
Publication Date: 2025.09.10 SUZHOU HEGUANG KEHUI BIOTECHNOLOGY CO LTD
  • EP4613861A1 patent drawingFigure 1A~1B
  • EP4613861A1 patent drawingFigure 2A~2B
  • EP4613861A1 patent drawingFigure 3

AI summary

The present invention provides an expression cassette for a target gene and use thereof. Specifically, the present invention provides an expression cassette having elements such as HCR, DSE, TPL and eMlp, an encoding nucleic acid thereof, an expression vector thereof, a host cell thereof, a pharmaceutical composition thereof, a gene delivery system thereof, and use thereof. The present invention further provides a C1-INH protein-encoding nucleic acid molecule and use thereof.