Mutated Sortase A Enzyme Enhancing Catalytic Activity

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current sortase enzymes, such as Staphylococcus aureus Sortase A, have limitations in enzymatic activity and substrate specificity, which hinder efficient protein conjugation and ligation reactions, particularly at low substrate concentrations and in preventing reverse reactions.

Innovation Solution

Introducing specific mutations, such as D160S and K196S, into the Staphylococcus aureus Sortase A amino acid sequence enhances enzymatic activity by increasing reaction kinetics and altering substrate preferences, resulting in a sortase with improved catalytic properties and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If wild-type Sortase A is used, then the enzyme maintains natural substrate recognition, but enzymatic activity is limited and reaction efficiency is low

Engineering Contradiction:
Improveenzymatic activityVSAvoidsubstrate specificity
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent applies parameter changes by mutating specific amino acid residues (D160S and K196S) in the Sortase A enzyme sequence. These parameter changes at the molecular level alter the enzyme's catalytic properties, increasing enzymatic activity while preserving the ability to recognize LPXTG substrates. The mutation transforms aspartate to serine at position 160 and lysine to serine at position 196, optimizing the enzyme's catalytic efficiency.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If sortase is used at low substrate concentrations, then reaction cost is reduced, but reaction efficiency decreases

Engineering Contradiction:
Improvesubstrate concentrationVSAvoidreaction efficiency
Core Design Contradiction:
Quantity of substanceVSProductivity

Solution Approach 1:

The mutated Sortase A enzyme with D160S and K196S substitutions exhibits enhanced catalytic efficiency that enables effective protein conjugation reactions even at low substrate concentrations. The parameter changes in the enzyme's amino acid sequence translate to improved kinetic parameters, allowing the enzyme to maintain high productivity under conditions of low substrate availability.

Inventive Principle:
Principle #35Parameter changes

3Ease of manufacture

If sortase reaction is performed, then protein conjugation is achieved, but reverse reactions occur reducing stability

Engineering Contradiction:
Improveprotein conjugationVSAvoidreaction stability
Core Design Contradiction:
Ease of manufactureVSStability of the object's composition

Solution Approach 1:

The patent utilizes parameter changes in the enzyme structure (amino acid mutations) to create a sortase variant that promotes irreversible or highly stable conjugation reactions. The D160S and K196S mutations alter the enzyme's catalytic mechanism or product release kinetics, favoring stable amide bond formation between the substrate and target protein, thereby minimizing reverse reactions and enhancing reaction 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 mutated sortase exhibits a five-fold increase in enzymatic activity compared to wild-type Sortase A, with improved reaction efficiency at low substrate concentrations and enhanced stability, facilitating more effective protein conjugation and ligation reactions.

Implementation Method 1

Sortase A (SrtA) is a membrane bound enzyme which attaches proteins covalently to the bacterial cell wall. The reaction proceeds through a thioester acyl-enzyme intermediate, which is resolved by the attack of an amine nucleophile from the oligoglycine, covalently linking peptidoglycan to a protein substrate and regenerating SrtA.

Methodology Applied
Scientific EffectEnzyme catalysis: Enzyme

Implementation Method 2

Herein is reported a sortase that has improved enzymatic activity and methods of using the same in transamidation reactions.

Methodology Applied
Scientific EffectTransamidation: Chemical Bonding

Data Source

PatentUS11572552B2Sortase
Publication Date: 2023.02.07 F HOFFMANN LA ROCHE INC

AI summary

Reported herein is a sortase comprising an amino acid sequence that is at least 90% identical to the amino acid sequence of SEQ ID NO: 11 and that comprises the mutations D101S and K137S.