Chemical Reprogramming of Glial Cells into Neurons

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Solution Overview

Problem

Current therapies for brain disorders such as stroke and Alzheimer's disease lack effective methods for reversing progression due to insufficient neuron regeneration, with cell transplantation facing hurdles like immunorejection, tumorigenesis, and differentiation uncertainty, and existing chemical conversions requiring external cells or viral vectors.

Innovation Solution

The use of FDA-approved compounds like Ceritinib, Pirfenidone, Crizotinib, Flurbiprofen, Lithium Chloride, and Vitamin C to chemically reprogram glial cells into functional neurons in situ, avoiding the need for external cell transplantation and viral vectors, and allowing for in vivo conversion within the nervous system.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If cell transplantation therapy is used to regenerate neurons, then neuron replacement is achieved, but immunorejection and tumorigenesis occur

Engineering Contradiction:
Improveneuron regenerationVSAvoidimmunorejection and tumorigenesis
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent enables the body's own glial cells to convert into neurons through chemical reprogramming, eliminating the need for external cell transplantation. This self-service approach avoids immunorejection and tumorigenesis while achieving neuron regeneration in situ within the nervous system

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent uses a small molecule cocktail as an intermediary to mediate the conversion of glial cells into neurons. This chemical mediator triggers endogenous cell fate changes without requiring external cell introduction, thereby avoiding the harmful effects associated with transplantation

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If viral vectors are used to express transcription factors for cell conversion, then in vivo conversion is achieved, but safety risks from exogenous genes increase

Engineering Contradiction:
Improvein vivo conversionVSAvoidsafety risks from exogenous genes
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent replaces the mechanical/biological system of viral vector delivery with a chemical system using small molecules. This substitution eliminates the safety risks associated with exogenous genes and viral integration while maintaining the ability to achieve in vivo cell conversion through pharmacological agents

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

Solution Approach 2:

The patent uses small molecule compounds that can be administered and cleared from the body, replacing persistent viral vectors. These chemical agents provide temporary but sufficient activity to trigger cell conversion without long-term genomic integration risks

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

3Quantity of substance

If stem cells are manipulated in culture to differentiate into neurons, then neuron production is achieved, but complex manipulation and transplantation requirements increase

Engineering Contradiction:
Improveneuron productionVSAvoidcell manipulation and transplantation process
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent enables glial cells to autonomously convert into neurons through chemical reprogramming within their native tissue environment. This eliminates the need for complex ex vivo manipulation, culture, and transplantation procedures, significantly simplifying the overall process while maintaining neuron production

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent breaks down the complex process of neuron generation into a simple chemical treatment step applied directly in vivo. Instead of multi-step procedures involving cell isolation, culture, differentiation, and transplantation, the solution segments the problem into a single pharmacological intervention that achieves the same outcome

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP3795147B1Chemical reprogramming of human glial cells into neurons with small molecule cocktail
Publication Date: 2023.08.30 THE PENN STATE RES FOUND INC
  • EP3795147B1 patent drawingFigure 1A~1I
  • EP3795147B1 patent drawingFigure 2A~2B
  • EP3795147B1 patent drawingFigure 3A~4C

AI summary

Provided are compositions, articles and methods that relate to promoting neurogenesis or neuroregeneration in mammalian nervous system. Embodiments relate to use of groups of compounds that contain Crizotinib (Cri), Flurbiprofen, Lithium Chloride (Li), Vitamin C (VC), Ceritinib (Cer) or Pirfenidone (PFD). In certain implementations glial cells are converted into functional neurons for the treatment of Huntington's disease.