Modified Dipeptide Cleavases for Mild, Selective Peptide Sequencing

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Solution Overview

Problem

Existing methods for peptide and protein degradation, such as Edman degradation, are limited by harsh chemical conditions and lack substrate-specific enzymes for efficient amino acid removal, which can be incompatible with sensitive analysis methods like nucleic acid analysis.

Innovation Solution

Development of modified dipeptide cleavases with specific amino acid substitutions in the substrate binding site of dipeptidyl aminopeptidases, allowing for the selective removal of labeled terminal amino acids or dipeptides from polypeptides, while maintaining compatibility with sensitive analysis methods.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If Edman degradation is used for peptide sequencing, then stepwise degradation of N-terminal amino acid can be achieved, but harsh chemical conditions (strong acids, high temperature) are required which are incompatible with sensitive analysis methods

Engineering Contradiction:
Improvepeptide sequencing accuracyVSAvoidharsh chemical conditions
Core Design Contradiction:
Measurement precisionVSObject-affected harmful factors

Solution Approach 1:

The patent replaces the chemical Edman degradation system with an enzymatic system (dipeptide cleavase). The enzyme catalyzes the hydrolysis of peptide bonds to release dipeptides containing N-terminal amino acids, eliminating the need for harsh chemicals like strong acids and anhydrous TFA while maintaining sequencing capability through stepwise amino acid removal.

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

Solution Approach 2:

The invention changes the reaction conditions from extreme chemical parameters (high temperature, strong acid concentration) to mild enzymatic parameters (physiological temperature, neutral pH buffer). This parameter transformation enables peptide sequencing under conditions compatible with sensitive nucleic acid analysis methods.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If natural aminopeptidases are used for amino acid removal, then processive elimination of amino acids can occur, but substrate specificity is limited and cannot selectively remove labeled terminal amino acids

Engineering Contradiction:
Improveamino acid removal efficiencyVSAvoidsubstrate specificity
Core Design Contradiction:
ProductivityVSAdaptability or versatility

Solution Approach 1:

The patent introduces specific amino acid substitutions in the substrate binding site of dipeptidyl aminopeptidase to create localized structural features that recognize and bind labeled amino acids. These local modifications (residues 191, 192, 196, 306, 650) confer specific recognition capability for labeled terminal amino acids while maintaining the enzyme's overall catalytic function for efficient amino acid removal.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The modified dipeptide cleavase automatically recognizes and selectively removes labeled terminal amino acids or dipeptides from polypeptides through its engineered substrate binding site. The enzyme's modified structure enables it to self-distinguish labeled substrates from unlabeled ones, performing selective degradation without requiring additional separation steps.

Inventive Principle:
Principle #25Self-service

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 dipeptide cleavases enable efficient and selective removal of labeled amino acids, facilitating protein sequencing and analysis without the use of harsh chemicals, and can be used in kits for targeted polypeptide treatment.

Implementation Method 1

Enzymes that are involved in degradation of peptides and proteins, e.g., aminopeptidases, dipeptidyl peptidases, carboxypeptidases, endopeptidases, and others, hydrolyze peptide bonds

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentEP4127157B1Modified dipeptide cleavases, uses thereof and related kits
Publication Date: 2026.02.11 ENCODIA INC
  • EP4127157B1 patent drawingFigure 1
  • EP4127157B1 patent drawingFigure 2A~2C
  • EP4127157B1 patent drawingFigure 3

AI summary

Provided herein are modified dipeptide cleavases for removing amino acid(s) from peptides, polypeptides, and proteins. Also provided are methods of using the modified dipeptide cleavases for treating polypeptides, and kits comprising the modified dipeptide cleavase. In some embodiments, the methods and the kits also include other components for macromolecule sequencing and/or analysis.