C-5 Sterol Desaturase Optimization for 7-DHC Production

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Solution Overview

Problem

Current methods for producing 7-dehydrocholesterol (7-DHC) in yeast cells result in excessive accumulation of side-products like zymosterol and lanosterol, which are toxic and reduce the efficiency of vitamin D3 production, as the sterol desaturase enzymes involved are non-specific, leading to a diverse steryl ester pool.

Innovation Solution

Modification of host cells to express heterologous enzymes with C-5 sterol desaturase activity, specifically increasing the expression of ERG3-homologs to enhance the production of 7-DHC by shifting the ratio of 7-DHC to side-products, such as cholesta-7-enol and lathosterol, through targeted genetic modification and optimization of polynucleotides for improved enzyme activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If sterol acyltransferase enzymes are used to store excess sterols in lipid bodies, then sterol accumulation is reduced, but the steryl ester pool becomes diverse including toxic side-products like zymosterol, lanosterol, and lathosterol

Engineering Contradiction:
Improvesterol accumulationVSAvoidtoxic side-products
Core Design Contradiction:
Quantity of substanceVSObject-generated harmful factors

Solution Approach 1:

The patent changes the specificity parameter of the sterol acyltransferase enzyme by introducing site-directed mutations (e.g., F592L, G595D, F592L/G595D double mutant) to shift substrate preference from diverse sterols to specifically 7-DHC, thereby producing steryl esters enriched in 7-DHC while reducing toxic side-products

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent introduces heterologous sterol acyltransferase genes (ARE1 and ARE2 from Aspergillus oryzae) with modified sequences into yeast cells to replace or supplement the native non-specific enzyme, creating a copy with improved specificity for 7-DHC production

Inventive Principle:
Principle #26Copying

2Productivity

If non-specific sterol desaturase enzymes are used in yeast cells, then 7-DHC production occurs, but side-products like zymosterol and lanosterol accumulate excessively

Engineering Contradiction:
Improve7-DHC productionVSAvoidside-products
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the specificity parameter of sterol desaturase enzymes through heterologous expression of ERG3 homologs from different fungal sources (Yarrowia lipolytica, Pichia pastoris, Penicillium roqueforti, Schizosaccharomyces pombe) with varying sequence identities, thereby changing the product distribution towards higher 7-DHC specificity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite enzymatic system by combining multiple modified enzymes (modified ERG3 desaturase and modified ARE1/ARE2 sterol acyltransferases) working together in the same yeast cell to achieve synergistic improvement in 7-DHC production and reduced side-products

Inventive Principle:
Principle #40Composite materials

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

The modified yeast cells achieve a significant increase in 7-DHC production, reaching up to 84% of the total sterols, with a corresponding reduction in side-products, thereby improving the efficiency and specificity of vitamin D3 biosynthesis.

Implementation Method 1

expression of heterologous enzymes having C-5 sterol desaturase activity, which leads to higher productivity of the host cell towards 7-DHC

Methodology Applied
Scientific EffectEnzyme catalysis: Enzyme

Data Source

PatentUS12018309B2Optimization of C-5 sterol desaturation
Publication Date: 2024.06.25 DSM IP ASSETS BV

AI summary

The present invention is related to an improved method for production of 7-dehydrocholesterol (7-DHC), an important intermediate towards biotechnological production of vitamin D3 or derivatives/metabolites thereof. The invention features modified host strains expressing enzymes having improved C-5 sterol 5 desaturase activity and their use in a process for production of vitamin D3 or derivatives and/or metabolites thereof.