Aggrelyte Lens Protein Solubilization for Presbyopia Treatment

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Solution Overview

Problem

Presbyopia, a vision-impeding condition affecting millions, is caused by the age-related hardening and stiffening of the lens due to protein crosslinking and aggregation, necessitating compositions and methods to treat, prevent, or reverse this condition.

Innovation Solution

Administration of aggrelytes, such as N,S-diacetyl-L-cysteine methyl ester, S-acetyl-N-(3,3-dimethylbutanoyl)-L-cysteinate, and N-acetyl cysteine methyl ester, to solubilize aggregated lens proteins and reduce lens stiffness through acetylation and disulfide bond reduction.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If lens proteins undergo posttranslational modifications and crosslinking over time, then the lens becomes more stable structurally, but the lens stiffness increases and accommodation ability is lost

Engineering Contradiction:
Improvelens structural stabilityVSAvoidlens stiffness
Core Design Contradiction:
Stability of the object's compositionVSStrength

Solution Approach 1:

The patent changes the chemical parameters of lens proteins by introducing acetylation modifications through aggrelyte treatment. This chemical modification alters the physical properties of the proteins, specifically reducing crosslinking and aggregation while maintaining structural stability, thereby decreasing lens stiffness without compromising integrity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses aggrelyte as an intermediary substance that mediates the interaction between lens proteins and acetyl groups. This intermediary facilitates the acetylation process, which in turn modifies protein-protein interactions and reduces harmful crosslinking and aggregation, resolving the contradiction between stability and stiffness

Inventive Principle:
Principle #24Intermediary (Mediator)

2Quantity of substance

If lens proteins accumulate and aggregate with age, then the lens maintains its mass, but the lens becomes insoluble and stiffens

Engineering Contradiction:
Improvelens protein massVSAvoidlens hardness
Core Design Contradiction:
Quantity of substanceVSStrength

Solution Approach 1:

The patent converts the harmful effect of protein aggregation into a beneficial outcome by using aggrelyte-induced acetylation. The aggregation process is reversed or prevented through chemical modification, transforming the accumulated proteins from a harmful stiffening factor into a beneficial soluble component that maintains lens flexibility and function

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

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

Aggrelytes effectively solubilize aggregated lens proteins, decrease lens stiffness, and acetylate lysine residues, thereby reducing lens hardness and improving accommodation ability, with potential applications in treating or preventing presbyopia.

Implementation Method 1

acetylation of lens proteins and reduction of disulfide bonds in lens proteins

Methodology Applied
Scientific EffectAcetylation: Chemical Bonding

Implementation Method 2

acetylation of lens proteins and reduction of disulfide bonds in lens proteins

Methodology Applied
Scientific EffectDisulfide bond reduction: Reduction

Data Source

PatentUS12350250B2Aggrelytes for treating ocular conditions
Publication Date: 2025.07.08 THE REGENTS OF THE UNIVERSITY OF COLORADO
  • US12350250B2 patent drawing
  • US12350250B2 patent drawing
  • US12350250B2 patent drawing

AI summary

Methods of treating, preventing, delaying, or reversing presbyopia in a subject involve administering a pharmaceutically effective amount of an aggrelyte to the subject. The aggrelyte may be one or more of N,S-diacetyl-L-cysteine methyl ester, S-acetyl-N-(3,3,-dimethylbutanoyl)-L-cysteinate, or N-acetyl cysteine methyl ester. The aggrelyte may be administered topically.