Humanized TMPRSS Rodent Model for Human-Specific Antiviral Testing

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Solution Overview

Problem

There is a need for an in vivo system to identify and test compounds targeting human type II transmembrane serine proteases for the treatment and prevention of viral infections, as existing models are inadequate.

Innovation Solution

Genetically modify rodents to include humanized Tmprss genes, specifically encoding human TMPRSS proteins with high sequence identity to their rodent counterparts, to create an in vivo model for testing therapeutic compounds.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If rodent models with endogenous Tmprss genes are used, then the model is simple and easy to maintain, but it cannot effectively test therapeutics targeting human TMPRSS proteins due to species differences

Engineering Contradiction:
Improveapplicability for testing human-specific therapeuticsVSAvoidgenetic modification complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The invention applies local quality by replacing only the ectodomain region of the rodent Tmprss gene with the corresponding human TMPRSS sequence, while retaining the rodent's native promoter, transmembrane domain, and cytoplasmic tail. This targeted regional substitution allows the protein to have human-specific functional properties in the ectodomain (enabling therapeutic testing) while maintaining rodent cellular context and simplifying model maintenance.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The Tmprss gene is segmented into functional domains: the ectodomain (replaced with human sequence for therapeutic relevance) and the transmembrane/cytoplasmic portions (retained as rodent sequence for model simplicity). This segmentation allows selective humanization of only the region necessary for therapeutic interaction while preserving rodent model advantages.

Inventive Principle:
Principle #1Segmentation

2Reliability

If humanized Tmprss gene is introduced into rodent genome, then the model can test human-specific compounds, but the genetic engineering process becomes more complex

Engineering Contradiction:
Improvemodel accuracy for human therapeutic testingVSAvoidease of creating the model
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

Instead of complete humanization which would be extremely complex, the invention humanizes only the ectodomain region that directly interacts with viral substrates and therapeutic compounds. This localized approach achieves the necessary reliability for human therapeutic testing while significantly reducing genetic engineering complexity compared to full gene replacement.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The rodent Tmprss gene structure serves as an intermediary framework that accepts the human ectodomain sequence. This hybrid construction allows the model to bridge human-specific therapeutic interactions with rodent model simplicity, achieving reliable therapeutic testing without requiring complete human genome introduction.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If complete human TMPRSS gene is used, then human protein function is perfectly replicated, but the model loses rodent physiological context

Engineering Contradiction:
Improvehuman protein function replicationVSAvoidrodent model utility
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention applies local quality by selectively replacing only the ectodomain with human sequence while maintaining rodent sequences for transmembrane and cytoplasmic regions. This ensures human-specific functional properties where needed (ectodomain for viral interaction) while preserving rodent physiological context (cellular environment, signaling pathways) for model utility.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The protein is segmented into functional regions with different origins: human ectodomain for specific therapeutic interactions and rodent transmembrane/cytoplasmic portions for physiological context. This segmentation allows the model to maintain both human protein function replication and rodent model versatility simultaneously.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP3895529B1Rodents having a humanized tmprss gene
Publication Date: 2026.04.29 REGENERON PHARMACEUTICALS INC
  • EP3895529B1 patent drawingFigure 1A
  • EP3895529B1 patent drawingFigure 1B
  • EP3895529B1 patent drawingFigure 1C

AI summary

Genetically modified rodents such as mice and rats, and methods and compositions for making and using the same, are provided. The rodents comprise a humanization of at least one endogenous rodent Tmprss gene, such as an endogenous rodent Tmprss2, Tmprss4, or Tmprss11d gene.