Recombinant Microbial Cells for Melatonin Production

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Solution Overview

Problem

Current methods for producing melatonin and related compounds in recombinant microorganisms are inefficient, despite advances in biosynthetic pathways, as they require exogenous cofactors and enzymes, limiting their cost-effectiveness and scalability.

Innovation Solution

Development of recombinant microbial cells expressing variants of E. coli GTP cyclohydrolase I (GCH1) and tryptohan hydroxylase (TPH) with specific mutations, which enhance monooxygenase activity, allowing for the production of oxidation products like 5HTP without the need for exogenous nucleic acids encoding dihydropteridine reductase or dihydromonapterin reductase, utilizing native bacterial compounds to support enzyme activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If exogenous cofactors and enzymes are used in recombinant microorganisms for melatonin production, then the biosynthetic pathway can function, but the production efficiency remains low and costs increase

Engineering Contradiction:
Improvemelatonin production efficiencyVSAvoiddependence on exogenous cofactors and enzymes
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent enables the recombinant microorganism to produce its own required cofactors (BH4 and MH4) through endogenous enzymes (GCH1, PTS, SRP, PCD, DHPR) already present in the host cell, eliminating the need for exogenous supplementation and reducing production complexity

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The patent introduces specific mutations in the GCH1 enzyme (e.g., T198I, D97V, M99I) to optimize its catalytic activity and substrate affinity, thereby improving the efficiency of endogenous BH4 production and overall melatonin synthesis pathway

Inventive Principle:
Principle #35Parameter changes

2Reliability

If multiple exogenous enzymes are introduced into recombinant cells, then the complete biosynthetic pathway is established, but the process complexity and cost increase

Engineering Contradiction:
Improvebiosynthetic pathway completenessVSAvoidnumber of exogenous nucleic acids required
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent extracts and utilizes only the essential endogenous enzymes (GCH1, PTS, SRP, PCD, DHPR) required for cofactor synthesis, removing the need for other exogenous enzymes and simplifying the overall system while maintaining pathway completeness

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent demonstrates that the endogenous GCH1 enzyme system can serve multiple functions: producing BH4 for TPH activity, producing MH4 for phenylalanine hydroxylase activity, and supporting overall cell metabolism, thereby reducing the need for specialized exogenous enzymes

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

3Productivity

If native E. coli GCH1 is used, then the cell maintains normal metabolic function, but the hydroxylation activity of TPH is insufficient for efficient melatonin production

Engineering Contradiction:
Improvehydroxylation activityVSAvoidenzyme activity consistency
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent introduces specific amino acid mutations in GCH1 (T198I, D97V, M99I) to change the enzyme's catalytic parameters, including substrate binding affinity and turnover rate, thereby enhancing TPH hydroxylation activity while maintaining enzyme stability

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

The approach results in a significant increase in melatonin and related compound production, achieving a 10-fold increase in 5HTP production and improved hydroxylation activity, reducing the reliance on exogenous cofactors and enzymes, thereby simplifying and cost-reducing the production process.

Implementation Method 1

GTP cyclohydrolase I (GCH1)...can be biosynthesized from endogenous GTP via a pathway comprising a GTP cyclohydrolase I (GCH1)

Methodology Applied
Scientific EffectEnzymatic catalysis: Enzyme

Implementation Method 2

TPH and many other mammalian aromatic amino acid hydroxylases require oxygen and tetrahydropterin (BH4) as cofactors

Methodology Applied
Scientific EffectCofactor-mediated enzymatic reaction: Enzyme

Implementation Method 3

regenerated into BH4 via consecutive reactions by pterin-4a-carbolamine dehydratase (PCD)

Methodology Applied
Scientific EffectEnzymatic dehydration: Enzyme

Implementation Method 4

regenerated into BH4 via consecutive reactions by pterin-4a-carbolamine dehydratase (PCD) and dihydropterin reductase (DHPR)

Methodology Applied
Scientific EffectRedox reaction: Redox Reactions

Implementation Method 5

variants of E. coli GTP cyclohydrolase I (GCH1)...provides for an increased hydroxylation activity

Methodology Applied
Scientific EffectEnzymatic catalysis enhancement: Enzyme

Implementation Method 6

The first step is this pathway, the conversion of L-tryptophan to 5HTP, is catalyzed by L-tryptophan hydroxylase (TPH)

Methodology Applied
Scientific EffectMonooxygenase hydroxylation: Enzyme

Data Source

PatentEP3436595B1Optimized microbial cells for production of melatonin and other compounds
Publication Date: 2024.02.28 DANMARKS TEKNISKE UNIV
  • EP3436595B1 patent drawingFigure 1
  • EP3436595B1 patent drawingFigure 2
  • EP3436595B1 patent drawingFigure 3

AI summary

Described herein are recombinant microbial host cells comprising biosynthetic pathways and their use in producing oxidation products and downstream products, e.g., melatonin and related compounds, as well as enzyme variants, nucleic acids, vectors and methods useful for preparing and using such cells. In specific aspects, the present invention relates to monooxygenases, e.g., amino acid hydroxylases, with a modified cofactor-dependency, and to enzyme variants and microbial cells providing for an improved supply of cofactors.