Adenosine Deaminase Mutations for Precise Adenine Base Editing

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Solution Overview

Problem

Current base editors have varying site-dependent editing efficiencies and a wide editing window, leading to unnecessary editing, thus necessitating improvements for more precise and efficient genome editing.

Innovation Solution

A site-directed mutation is performed on the basic sequence of the adenosine deaminase to create an adenine base editor with improved editing efficiency, and a suitable position for embedding adenosine deaminase in the nuclease domain of the base editor fusion protein is identified to enhance editing efficiency.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If current base editors are used, then genome editing can be achieved, but editing efficiency varies by site and editing window is wide causing unnecessary editing

Engineering Contradiction:
Improveediting efficiencyVSAvoidediting precision
Core Design Contradiction:
ProductivityVSManufacturing precision

Solution Approach 1:

The patent applies local quality by introducing a narrow editing window through specific amino acid mutations in the adenosine deaminase domain (positions 104-107 and 148-155). These localized mutations create a more constrained editing window that maintains high editing efficiency at target sites while preventing off-target editing, thus simultaneously improving productivity and manufacturing precision.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent changes key parameters of the adenosine deaminase enzyme through site-directed mutations at specific positions (104V107 and 148-155). These parameter changes in the enzyme's amino acid sequence result in a narrowed editing window and enhanced site-specific editing efficiency, resolving the contradiction between overall editing productivity and precision.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If adenosine deaminase is embedded in nuclease domain at certain positions, then base editing efficiency is improved, but protein structure stability may be affected

Engineering Contradiction:
Improvebase editing efficiencyVSAvoidprotein structure stability
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent segments the base editor fusion protein into distinct functional domains: the nuclease domain (Cas9) and the adenosine deaminase domain. By maintaining this segmentation and placing the deaminase at specific positions (104V107 and 148-155) rather than disrupting the overall protein architecture, the patent achieves improved base editing efficiency while preserving protein structure stability through modular domain organization.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent uses a linker sequence as an intermediary between the nuclease domain and adenosine deaminase domain. This linker acts as a flexible connector that allows the deaminase to be positioned at optimal locations for enhanced editing efficiency while maintaining proper protein folding and structural stability through the mediating linker region.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 base editor achieves significantly higher editing efficiency, particularly on the PCSK9 target and other sites, with great potential for treating diseases associated with point mutations, such as hypercholesterolemia, transthyretin amyloidosis, and β-hemoglobinopathy.

Implementation Method 1

deaminates, under guidance of sgRNA, a target base adenine A located in a base editing active window to form hypoxanthine I

Methodology Applied
Scientific EffectDeamination: Enzyme

Data Source

PatentEP4506454A1Adenosine deaminase, base editor, and use thereof
Publication Date: 2025.02.12 YOLTECH THERAPEUTICS CO LTD
  • EP4506454A1 patent drawingFigure 1
  • EP4506454A1 patent drawingFigure 2~4
  • EP4506454A1 patent drawingFigure 5~6A

AI summary

The present invention belongs to the field of biotechnology, and provides a deaminase and an adenine base editor, and also provides a mutated deaminase and a corresponding adenine base editor. The mutated deaminase undergoes mutation of a plurality of amino acids compared with a parent deaminase, thereby improving a base editing efficiency and obtaining a good application prospect.