Radioactive Polypeptide Probe for Pancreatic Islet Imaging

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Solution Overview

Problem

Current methods for noninvasive imaging of pancreatic islets are inadequate for early detection and quantification of type-II diabetes, as they fail to provide clear three-dimensional imaging and specific contrast with surrounding organs, limiting their effectiveness in preventing and diagnosing the disease.

Innovation Solution

A molecular probe consisting of specific polypeptides, such as those represented by formulas (1), (2), and (3), which bind to pancreatic islets and are labeled with radioactive nuclides, enabling noninvasive three-dimensional imaging of pancreatic islets through PET or SPECT, allowing for accurate quantification and early diagnosis of type-II diabetes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If existing molecular probes for imaging pancreatic islets are used, then imaging can be performed, but three-dimensional imaging capability and contrast with surrounding organs are insufficient

Engineering Contradiction:
Improveimaging precisionVSAvoidimaging capability
Core Design Contradiction:
Measurement precisionVSDevice complexity

Solution Approach 1:

The patent modifies the molecular probe by changing chemical parameters - specifically incorporating a radioactive nuclide (such as 18F, 11C, 13N, or 64Cu) into the peptide structure at specific positions (N-terminus, C-terminus, or side chains of lysine residues). This parameter change enables PET or SPECT imaging capabilities, providing three-dimensional imaging and improved contrast with surrounding organs while maintaining the probe's ability to bind to pancreatic islets.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If noninvasive imaging methods are used, then patient safety is improved, but detection accuracy and quantification capability are insufficient

Engineering Contradiction:
Improvepatient safetyVSAvoiddetection accuracy
Core Design Contradiction:
ReliabilityVSMeasurement precision

Solution Approach 1:

The patent uses a radioactive nuclide as an intermediary that emits detectable radiation (positrons for PET or gamma rays for SPECT). This intermediary allows noninvasive detection of pancreatic islets through the patient's body without requiring direct tissue biopsy, while providing sufficient detection accuracy and quantification capability through the radioactive signal's measurable properties.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Measurement precision

If existing imaging probes are used, then pancreatic islet imaging is possible, but specific contrast with surrounding organs is inadequate for early diagnosis

Engineering Contradiction:
Improvecontrast ratioVSAvoiddiagnostic information
Core Design Contradiction:
Measurement precisionVSLoss of information

Solution Approach 1:

The patent enhances local quality by ensuring the molecular probe binds specifically to pancreatic islets (particularly beta cells) through its peptide structure, while the radioactive nuclide provides localized signal emission. This creates high specific contrast in the pancreatic islet region compared to surrounding organs, preserving diagnostic information about islet mass and distribution that is crucial for early diabetes detection.

Inventive Principle:
Principle #3Local quality

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 molecular probe achieves improved uptake in the pancreas, providing a high specificity and contrast with surrounding organs, enabling effective noninvasive three-dimensional imaging and quantification of pancreatic islets, thereby facilitating early diagnosis and prevention of type-II diabetes.

Implementation Method 1

labeled with a radioactive nuclide, enabling noninvasive three-dimensional imaging of pancreatic islets through PET or SPECT

Methodology Applied
Scientific EffectRadioactive decay: Radioactive Decay

Data Source

PatentEP2510951B1Molecular probe for imaging of pancreatic islet, and use thereof
Publication Date: 2016.07.13 ARKRAY INC
  • EP2510951B1 patent drawingFigure 1A~1B
  • EP2510951B1 patent drawingFigure 2A~2C
  • EP2510951B1 patent drawingFigure 3A~3B

AI summary

A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe comprises a polypeptide represented by the following formula (1), (2), or (3), or a polypeptide having homology with the foregoing polypeptide, Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (1) (SEQ ID NO. 1) Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2 (2) (SEQ ID NO. 2) B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (3) (SEQ ID NO. 3) where, in formulae (1) and (2), "X" represents a lysine residue, the amino group of the side chain of the lysine residue being labeled with a radioactive nuclide, and "Z-" indicates that the α-amino group at the N-terminus is not modified, or is modified with a modifying group having no electric charge; in formula (3), "B-" indicates that the α-amino group at the N-terminus is labeled with a radioactive nuclide; and in formulae (1), (2), and (3), "-NH2" indicates that the carboxyl group at the C-terminus is amidated.