Ciliate Expression of Mammalian Voltage-Gated Ion Channels

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Solution Overview

Problem

Current methods for expressing voltage-gated ion channels in mammalian cells result in low levels of correctly folded and surface-localized proteins, limiting the availability of high-density ion channels for drug discovery and therapeutic development, particularly for small molecule screening and monoclonal antibody production.

Innovation Solution

Transgenic ciliates, such as Tetrahymena thermophila, are engineered to express mammalian voltage-gated ion channels with optimized codon usage and regulatory sequences, achieving high levels of correct folding and membrane integration, enabling the production of membrane preparations with high densities of functional ion channels.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If voltage-gated ion channels are expressed in mammalian cells using traditional methods, then the expression system is well-established and easy to operate, but the levels of correctly folded and surface-localized proteins are low

Engineering Contradiction:
Improvecorrect folding and surface localizationVSAvoidexpression level
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent changes the host cell parameter from mammalian cells to ciliate cells (Tetrahymena thermophila), which fundamentally alters the cellular environment and protein processing capabilities. This parameter change enables higher expression levels of correctly folded voltage-gated ion channels at the cell surface, resolving the contradiction between reliability of folding and productivity of expression.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If more voltage-gated ion channels are produced to achieve high density, then the availability for drug discovery improves, but the complexity of achieving correct folding and membrane integration increases

Engineering Contradiction:
Improveion channel densityVSAvoidfolding and membrane integration complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The ciliate expression system possesses endogenous capabilities for correct protein folding and membrane integration that automatically service the production of voltage-gated ion channels. The system self-regulates the complex processes of folding and membrane integration without requiring additional external intervention, enabling high ion channel density while managing complexity through the host's natural machinery.

Inventive Principle:
Principle #25Self-service

3Manufacturing precision

If traditional mammalian expression systems are used, then the process is straightforward, but the purity and density of functional ion channels are insufficient for effective drug screening

Engineering Contradiction:
Improveion channel purity and densityVSAvoidexpression system simplicity
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

By changing the host organism parameter from mammalian to ciliate cells, the patent achieves superior manufacturing precision in terms of ion channel purity and density. Although this introduces some complexity in establishing the expression system, the ciliate system's natural properties facilitate high-level production of correctly folded, functional channels that meet drug screening requirements.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3140415B1Expression of voltage-gated ion channels in ciliates
Publication Date: 2022.09.28 ABCELLERA BOSTON INC
  • EP3140415B1 patent drawingFigure 1
  • EP3140415B1 patent drawingFigure 2
  • EP3140415B1 patent drawingFigure 3

AI summary

Methods are disclosed for the production of mammalian voltage-gated ion channels in ciliates. In other aspects, compositions comprising lipid bilayers containing mammalian voltage-gated ion channels are disclosed. In other aspects, compositions comprising purified and reconstituted mammalian voltage-gated ion channels are disclosed.