Molecular Probe Precursor for Pancreatic Islet Imaging

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Solution Overview

Problem

Current molecular probes, such as 125I-labeled exendin(9-39), are ineffective for noninvasive three-dimensional imaging of pancreatic islets, making it difficult to detect and quantify pancreatic islets noninvasively, which is crucial for early diabetes diagnosis and prevention.

Innovation Solution

A molecular probe is developed by labeling the amino group at the N-terminus of a precursor polypeptide with a positron emission or single photon emission nuclide, specifically designed to bind to pancreatic islets, allowing for noninvasive three-dimensional imaging using positron emission tomography (PET).

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If conventional molecular probes (e.g., 125I-labeled exendin(9-39)) are used for imaging pancreatic islets, then the imaging can be performed, but noninvasive three-dimensional imaging is not achieved and quantification is difficult

Engineering Contradiction:
Improvequantification capabilityVSAvoidnoninvasive imaging
Core Design Contradiction:
Measurement precisionVSEase of operation

Solution Approach 1:

The patent changes the labeling method from conventional 125I labeling to positron emission nuclide labeling (e.g., 11C, 18F, 62Cu, 64Cu, 89Sr, 90Y), which fundamentally alters the imaging modality from planar to three-dimensional PET imaging, enabling both noninvasive imaging and precise quantification

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent replaces the conventional gamma camera imaging system with a PET imaging system that uses positron emission nuclides, substituting the detection mechanism to achieve superior three-dimensional imaging capability and quantification accuracy

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

2Loss of time

If early detection of pancreatic islet decrease is achieved, then diabetes prevention becomes possible, but current techniques cannot detect functional abnormalities at the appropriate early stage

Engineering Contradiction:
Improvedetection timingVSAvoiddetection accuracy
Core Design Contradiction:
Loss of timeVSMeasurement precision

Solution Approach 1:

The patent replaces indirect functional assessment methods with direct structural imaging of pancreatic islets using PET, enabling visualization and quantification of islet mass at the cellular level before functional abnormalities manifest

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

Solution Approach 2:

The patent changes the detection parameter from functional metrics (glucose tolerance) to structural metrics (islet mass and β-cell quantity), allowing detection of pathological changes at an earlier stage when interventions are most effective

Inventive Principle:
Principle #35Parameter changes

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

Enables noninvasive three-dimensional imaging and quantification of pancreatic islets, facilitating early detection and diagnosis of diabetes by determining the amount of pancreatic islets, thereby aiding in prevention and treatment.

Implementation Method 1

labeling the amino group at the N-terminus of a precursor with a positron emission nuclide or a single photon emission nuclide

Methodology Applied
Scientific EffectPositron emission: Radioactive Decay

Implementation Method 2

labeling the amino group at the N-terminus of a precursor with a positron emission nuclide or a single photon emission nuclide

Methodology Applied
Scientific EffectSingle photon emission: Radioactive Decay

Data Source

PatentEP2335739B1Molecular probe precursor for imaging of pancreatic islet, and use thereof
Publication Date: 2020.04.08 ARKRAY INC
  • EP2335739B1 patent drawingFigure 1A~1C
  • EP2335739B1 patent drawingFigure 2A~2B
  • EP2335739B1 patent drawingFigure 3A~3B

AI summary

A precursor of a molecular probe for imaging of pancreatic islets is provided. The precursor includes a polypeptide represented by any one of the following formulae (1) to (12), or a polypeptide having a homology with the foregoing polypeptide: *-DLSKQMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH2 (1) *-LSKQMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH2 (2) *-SKQMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH2 (3) *-KQMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH2 (4) *-DLSK* QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (5) *-LSW QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (6) *-SK* QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (7) *-K* QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (8) DLSK* QMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH2 (9) LSK* QMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH2 (10) SK* QMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH2 (11) K* QMEEEAVRLFIEWLK* NGGPSSGAPPPS-NH2 (12)