Engineered Cas9 Variants for AAV Delivery and High-Fidelity Editing

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Solution Overview

Problem

Existing Cas9 proteins are too large for effective delivery via methods like AAV and have low activity, limiting their suitability for therapeutic genome editing applications.

Innovation Solution

Engineering Cas9 proteins with specific amino acid modifications, such as substitutions at positions 37, 39, 46, 47, 54, 57, 59, 61, 94, 315, 501, 508, 556, 566, 911, 912, 978, 980, 1073, 1091, 1122, 1160, 1161, 1164, 1206, 1226, and 1229, to enhance endonuclease activity and fidelity, and incorporating nuclear localization signals (NLS) for improved delivery and activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If wild type Cas9 proteins are used, then they can perform genome editing functions, but their large size prevents effective delivery via AAV and their activity is insufficient for therapeutic applications

Engineering Contradiction:
Improveendonuclease activityVSAvoidCas9 protein size
Core Design Contradiction:
ReliabilityVSWeight of moving object

Solution Approach 1:

The patent applies parameter changes by systematically modifying amino acid residues at specific positions (37, 39, 46, 47, 54, 57, 59, 61, 94, 315, 501, 508, 556, 566, 911, 912, 978, 980, 1073, 1091, 1122, 1160, 1161, 1164, 1206, 1226, and 1229) to optimize the Cas9 protein's endonuclease activity while maintaining a compact size suitable for AAV delivery

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite structure by combining multiple amino acid modifications with nuclear localization signals (NLS) to generate a hybrid Cas9 variant that integrates enhanced enzymatic activity, proper cellular localization, and reduced size into a single functional protein

Inventive Principle:
Principle #40Composite materials

2Reliability

If Cas9 proteins are engineered with multiple amino acid modifications, then endonuclease activity and fidelity are enhanced, but the complexity of protein engineering increases

Engineering Contradiction:
ImprovefidelityVSAvoidprotein engineering complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent systematically changes specific amino acid parameters at predetermined positions to enhance fidelity while maintaining manageable engineering complexity through focused mutagenesis rather than random screening

Inventive Principle:
Principle #35Parameter changes

3Weight of moving object

If Cas9 proteins are modified to reduce size for AAV delivery, then delivery efficiency improves, but endonuclease activity may be compromised

Engineering Contradiction:
ImproveCas9 protein sizeVSAvoidendonuclease activity
Core Design Contradiction:
Weight of moving objectVSReliability

Solution Approach 1:

The patent optimizes the balance between size and activity by selecting specific amino acid positions for modification that reduce protein mass while preserving or enhancing catalytic function through strategic residue changes

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP4678742A1Improved cas9 proteins
Publication Date: 2026.01.14 ASTRAZENECA AB
  • EP4678742A1 patent drawingFigure 1
  • EP4678742A1 patent drawingFigure 2A~2B
  • EP4678742A1 patent drawingFigure 3A~3B

AI summary

The disclosure relates to a Cas9 protein comprising a polypeptide sequence having at least 95% identity, such as 97%, 98% or 99%, to SEQ ID NO: 1, wherein said polypeptide sequence comprises an amino acid modification at one or more positions relative to SEQ ID NO: 1: 37, 39, 46, 47, 54, 57, 59, 61, 94, 315, 501, 508, 556, 566, 911, 912, 978, 980, 1073, 1091, 1122, 1160, 1161, 1164, 1206, 1226 and/or 1229, CRISPR-Cas systems and methods for providing site-specific modification of a target sequence in a eukaryotic cell.