Yeast GPCR Evolution Through Cell Wall Permeabilization

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

The challenge of achieving high functional expression levels of transmembrane receptors, particularly GPCRs, in eukaryotic cells is hindered by the cell wall, which restricts access of ligands and requires methods like yeast display that are not suitable for insoluble transmembrane receptors.

Innovation Solution

A method involving permeabilization of yeast cell walls with an alkaline pH buffer containing lithium ions and reducing agents, followed by fluorescent labeling and sorting, allows for the selection and expansion of yeast cells expressing functional GPCRs, enabling multiple rounds of selection and amplification.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If yeast display method is used to present proteins outside the cell wall, then accessibility of ligands to membrane receptors is improved, but this approach is not suitable for insoluble transmembrane receptors that must be located in the plasma membrane

Engineering Contradiction:
Improveaccessibility of ligands to receptorsVSAvoidsuitability for insoluble transmembrane receptors
Core Design Contradiction:
Ease of operationVSAdaptability or versatility

Solution Approach 1:

The invention extracts and removes the cell wall barrier from yeast cells to enable ligand access to membrane receptors while maintaining the cells' eukaryotic expression capabilities. This is achieved through enzymatic digestion of cell wall components, allowing the system to be adapted for selecting insoluble transmembrane receptors that require plasma membrane localization.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

Instead of presenting proteins outside the cell wall as fusion proteins (yeast display approach), the invention inverts the approach by keeping transmembrane receptors in their native plasma membrane location and removing the cell wall barrier to enable ligand access. This inversion makes the system suitable for insoluble receptors that cannot be expressed as soluble fusion proteins.

Inventive Principle:
Principle #13The other way round (Inversion)

2Reliability

If mammalian or insect cells are used as eukaryotic hosts for directed evolution, then functional expression of transmembrane receptors is improved, but these cells are not easily transformed with libraries

Engineering Contradiction:
Improvefunctional expression of transmembrane receptorsVSAvoidtransformation with libraries
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The invention makes yeast cells universal by combining their ease of transformation with the ability to properly fold and functionalize eukaryotic transmembrane receptors. By removing the cell wall barrier, yeast acquire the dual capability of being easily transformable like prokaryotes while maintaining eukaryotic protein processing functions, making them suitable for directed evolution of membrane proteins.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The invention changes the physical-chemical parameters of yeast cells by removing the cell wall structure. This parameter change transforms yeast from having a rigid cell wall barrier to having a permeabilized state that allows ligand access, while maintaining the eukaryotic cellular machinery needed for proper receptor folding and function.

Inventive Principle:
Principle #35Parameter changes

3Strength

If cell wall is present in yeast cells, then yeast cells maintain structural integrity, but this restricts access of administered ligands to expressed receptors in the plasma membrane

Engineering Contradiction:
Improvestructural integrity of yeast cellsVSAvoidaccess of ligands to receptors
Core Design Contradiction:
StrengthVSEase of operation

Solution Approach 1:

The invention extracts specific components of the cell wall (primarily glucans and mannans) while leaving the plasma membrane and cellular machinery intact. This selective removal maintains sufficient structural integrity for cell viability while creating permeability channels that allow ligand access to plasma membrane receptors.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The invention applies local quality change by selectively modifying the cell wall structure rather than completely removing it. The cell wall is partially degraded in specific regions to create access pathways for ligands, while maintaining overall structural integrity and cellular function. This localized modification enables ligand access without compromising cell strength.

Inventive Principle:
Principle #3Local quality

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 method significantly increases functional expression levels of GPCRs in yeast cells, allowing for the selection of high-expression variants and improving their stability and functionality.

Implementation Method 1

permeabilizing the cell wall of said plurality of yeast cells in a permeabilization step, wherein the permeabilization step comprises exposing the plurality of yeast cells to a chemical treatment

Methodology Applied
Scientific EffectPermeabilization:

Implementation Method 2

wherein the chemical treatment is a buffer of alkaline pH comprising lithium ions, a reducing agent and/or a chelating agent

Methodology Applied
Scientific EffectReduction: Reduction

Implementation Method 3

contacting said plurality of viable permeabilized cells in a labelling step with a ligand capable of binding to said GPCR, wherein said ligand comprises a detectable label

Methodology Applied
Scientific EffectFluorescence: Fluorescence

Implementation Method 4

selecting a subset of said plurality of viable labelled cells as a function of detectable label present in said plurality of viable labelled cells in a selection step, yielding a selection of viable cells, wherein said detectable label is a fluorescent dye and said selection step is accomplished by fluorescent cell sorting

Methodology Applied
Scientific EffectFluorescence-activated cell sorting:

Data Source

PatentEP3237908B1Directed evolution of membrane proteins in eukaryotic cells with a cell wall
Publication Date: 2026.04.22 UNIVERSITY OF ZURICH
  • EP3237908B1 patent drawingFigure 1
  • EP3237908B1 patent drawingFigure 2A~2F
  • EP3237908B1 patent drawingFigure 3A~3B

AI summary

The invention relates to a method for selecting an expressed sequence from a library, comprising the following steps: Each of a plurality of eukaryotic cells comprising a cell wall comprises a nucleic acid sequence member of a library, which is expressed as a target membrane protein in said eukaryotic cells. The cell wall of the cells is permeabilized. The permeabilized cells are labeled with a ligand capable of binding to the target membrane protein. The ligand bears a detectable label. A subset of the labelled cells is selected as a function of detectable label present. Finally, an expressed nucleic acid sequence is isolated from said selection of cells in an isolation step.