Fluorescent RGD Peptide Probe for Integrin Alpha v Beta 3 Detection

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Solution Overview

Problem

Current clinical imaging methods for age-related macular degeneration, such as fluorescein angiography and optical coherence tomography, cannot predict the occurrence or recurrence of choroidal neovascularization, a key cause of visual impairment in this disease, due to limited understanding of its mechanisms and lack of molecular information.

Innovation Solution

Development of a fluorescently labeled cyclic RGD peptide probe that targets integrin αvβ3, specifically conjugating NH2-cyclic RGD peptide with materials like FITC, to visualize and diagnose retinochoroidal neovascularization through fluorescence fundus angiography.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Loss of information

If conventional imaging methods (fluorescein angiography and OCT) are used, then structural information on disease status is provided, but molecular information and prediction capability for choroidal neovascularization are lost

Engineering Contradiction:

Improvemolecular informationVSAvoidimaging method complexity

Core Design Contradiction:

Loss of informationVSDevice complexity

Solution Approach 1:

The patent introduces an RGD peptide probe as an intermediary that specifically binds to integrin αvβ3 on angiogenic blood vessels. This probe serves as a mediator between the imaging system and the molecular target, enabling visualization of molecular processes (integrin expression) that conventional imaging methods cannot detect. The probe translates molecular information into detectable optical signals without requiring complex molecular biology techniques.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Measurement precision

If RGD peptide is used as contrast agent, then high affinity for integrin αvβ3 is achieved, but specificity for choroidal neovascularization versus normal tissue is improved

Engineering Contradiction:

Improvediagnostic precisionVSAvoidprobe preparation ease

Core Design Contradiction:

Measurement precisionVSEase of manufacture

Solution Approach 1:

The patent applies local quality by designing the RGD peptide probe with specific structural modifications (cyclic structure, specific amino acid sequences) that enhance its binding affinity and specificity for integrin αvβ3 at the target site (choroidal neovascularization). The probe exhibits different binding characteristics in different tissues: high binding to pathological vessels and low binding to normal vessels, achieving localized diagnostic precision without affecting overall probe simplicity.

Inventive Principle:

Principle #3Local quality

3Reliability

If integrin αvβ3 targeting probe is developed, then prediction of choroidal neovascularization occurrence and recurrence is enabled, but conventional structural imaging capabilities are insufficient

Engineering Contradiction:

Improvedisease progression predictionVSAvoidmolecular target detection

Core Design Contradiction:

ReliabilityVSDifficulty of detecting and measuring

Solution Approach 1:

The patent replaces complex molecular detection methods with an optical imaging approach. Instead of using cumbersome molecular biology techniques to detect integrin expression, the invention uses an optically detectable RGD peptide probe that binds to integrin αvβ3 and can be visualized using standard optical imaging equipment. This substitution enables reliable prediction of disease progression through non-invasive optical detection of molecular targets.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

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 probe effectively visualizes retinochoroidal neovascularization lesions, allowing for the prediction of occurrence and recurrence before structural changes, with intense immunofluorescence staining in affected areas and minimal staining in normal tissues, enhancing diagnostic capabilities.

Implementation Method 1

RGD peptide, which is a peptide in which arginine (R), glycine (G), and aspartic acid (D) are bound, has a high affinity for integrin αvβ3

Methodology Applied

Scientific EffectIntegrin binding:

Implementation Method 2

a fluorescent material-labeled cyclic RGD peptide, which is completed by conjugating an NH2-cyclic RGD peptide precursor to a fluorescent material

Methodology Applied

Scientific EffectFluorescence: Fluorescence

Data Source

PatentUS20220146519A1Integrin alpha v beta 3 targeting probe for diagnosing retinochoroidal neovascular diseases and preparation method therefor

Publication Date: 2022.05.12 SEOUL NAT UNIV HOSPITAL

AI summary

Provided are: an integrin targeting probe, which can be effectively used for the diagnosis or treatment of retinochoroidal neovascularization or age-related macular degeneration by predicting the occurrence and recurrence of retinochoroidal neovascularization before structural changes of retinochoroidal neovascularization occur; and a preparation method therefor. The integrin targeting probe is an integrin αvβ3 targeting probe for diagnosing retinochoroidal neovascular diseases and can comprise a fluorescent material-labeled cyclic RGD peptide, which is completed by conjugating an NH2-cyclic RGD peptide precursor to a fluorescent material.