Fucosyltransferase Engineered E. coli for HMOS Production

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Solution Overview

Problem

The production of human milk oligosaccharides (HMOS) is hindered by high costs, stereo-specificity issues, and limited availability of precursor molecules, making it challenging to manufacture large quantities inexpensively through chemical synthesis or existing methods.

Innovation Solution

A nucleic acid construct encoding a lactose-utilizing α(1,2)fucosyltransferase enzyme, specifically the FutL enzyme, is used to produce fucosylated oligosaccharides in bacteria like E. coli, enhancing intracellular pools of lactose and GDP-fucose, and reducing β-galactosidase activity to efficiently synthesize HMOS like 2'-fucosyllactose and lactodifucotetraose.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If chemical synthesis is used to produce human milk oligosaccharides, then production capability is achieved, but cost is high and stereo-specificity issues occur

Engineering Contradiction:
Improveproduction capabilityVSAvoidmanufacturing cost and complexity
Core Design Contradiction:
ProductivityVSEase of manufacture

Solution Approach 1:

The patent replaces chemical synthesis methods with a biological system (genetically engineered bacteria) to produce human milk oligosaccharides. The bacteria express fucosyltransferase enzymes that catalyze the formation of fucosylated oligosaccharides through biochemical pathways, substituting chemical reactions with enzymatic processes that naturally occur in living systems.

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

Solution Approach 2:

The genetically engineered bacteria serve themselves by utilizing their own metabolic pathways and intracellular pools of precursors (GDP-fucose and lactose) to synthesize the desired oligosaccharides. The bacteria's natural cellular machinery, including its enzyme systems and metabolic networks, is harnessed to produce the target compounds without requiring external chemical synthesis infrastructure.

Inventive Principle:
Principle #25Self-service

2Productivity

If existing methods are used to produce HMOS, then some production is achieved, but precursor availability is limited and costs remain high

Engineering Contradiction:
Improveproduction outputVSAvoidprecursor availability
Core Design Contradiction:
ProductivityVSQuantity of substance

Solution Approach 1:

The patent enhances the intracellular pools of precursors (GDP-fucose and lactose) within the bacterial cells before the actual oligosaccharide synthesis occurs. By pre-accumulating these essential building blocks through metabolic engineering and optimized culture conditions, the system ensures sufficient substrate availability for high-level product formation.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The bacterial host system performs multiple functions: it serves as a factory for synthesizing GDP-fucose through its metabolic pathways, stores lactose as an intracellular precursor, expresses the fucosyltransferase enzyme, and ultimately produces the fucosylated oligosaccharides. This multi-functional biological system replaces the need for separate precursor synthesis and assembly steps required in chemical methods.

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

3Productivity

If β-galactosidase activity is present in the production system, then lactose metabolism occurs, but oligosaccharide production efficiency decreases

Engineering Contradiction:
Improveoligosaccharide production efficiencyVSAvoidlactose metabolism interference
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent removes or reduces β-galactosidase activity from the bacterial production system. By eliminating this enzyme that would otherwise metabolize lactose, the system prevents the degradation of the lactose precursor and directs metabolic flux toward oligosaccharide synthesis instead, thereby improving production efficiency.

Inventive Principle:
Principle #2Taking out (Extraction)

4Quantity of substance

If recombinant fucosyltransferase is produced in bacteria, then enzyme availability increases, but enzyme stability and toxicity issues arise

Engineering Contradiction:
Improveenzyme availabilityVSAvoidenzyme stability and safety
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent optimizes various parameters including the bacterial host strain selection, cultivation conditions, and enzyme expression levels to enhance the stability and safety of the recombinant fucosyltransferase. By adjusting these parameters, the system achieves high enzyme availability while maintaining cellular viability and product safety.

Inventive Principle:
Principle #35Parameter changes

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 allows for the economical and efficient production of high-purity fucosylated oligosaccharides, such as 2'-fucosyllactose, overcoming previous limitations by using genetically engineered bacteria to achieve commercially viable yields and improved stability of the enzyme, reducing toxicity, and ensuring safety for use in dietary supplements.

Implementation Method 1

a nucleic acid encoding a lactose- utilizing α(1,2)fucosyltransferase enzyme... the amino acid sequence of said enzyme encoded by said nucleic acid comprises the sequence of SEQ ID NO: 8 for producing a fucosylated oligosaccharide

Methodology Applied
Scientific EffectEnzyme catalysis: Enzyme

Data Source

PatentEP2877574B1Alpha (1,2) fucosyltransferases suitable for use in the production of fucosylated oligosaccharides
Publication Date: 2019.05.15 GLYCOSYN LLC
  • EP2877574B1 patent drawingFigure 1~2
  • EP2877574B1 patent drawingFigure 3A~3C
  • EP2877574B1 patent drawingFigure 4

AI summary

The invention provides compositions and methods for engineering E. coli or other host production bacterial strains to produce fucosylated oligosaccharides, and the use thereof in the prevention or treatment of infection.