18F-ApoPep-7 Peptide for Apoptosis PET Imaging
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Solution Overview
Problem
Current imaging agents for apoptosis, such as Annexin V, have limitations due to poor pharmacokinetics and low target signal/noise ratios, making them less effective for diagnosing diseases through positron emission tomography (PET).
Innovation Solution
Development of an 18F-ApoPep-7 compound, a derivative of the peptide ApoPep-1, which specifically binds to histone H1 exposed on apoptotic cells, labeled with the positron emission isotope F-18, allowing for improved PET imaging of apoptosis-related diseases.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If Annexin V is used as an imaging agent for apoptosis, then it can selectively bind to phosphatidylserine on apoptotic cells, but it has poor pharmacokinetics and low target signal/noise ratio due to slow movement and long accumulation time
Solution Approach 1:
The patent changes the molecular size parameter from Annexin V (36 kD macromolecule) to a smaller peptide structure, which improves pharmacokinetic properties and accumulation speed while maintaining selective binding capability through specific amino acid sequence design
Solution Approach 2:
The patent extracts only the essential binding function from Annexin V by designing a minimal peptide sequence that specifically recognizes phosphatidylserine, eliminating the bulky protein structure that causes slow pharmacokinetics
2Measurement precision
If Annexin V is labeled with positron emission radioisotope for PET imaging, then it can image apoptotic cells, but the short half-life of the radioisotope combined with slow accumulation limits human imaging
Solution Approach 1:
The patent performs preliminary action by designing a peptide with inherently fast pharmacokinetic properties that accumulates rapidly at the target, ensuring sufficient signal accumulation before the radioisotope decays, thereby enabling successful PET imaging within the limited half-life window
Solution Approach 2:
The patent changes the molecular weight parameter from high (Annexin V) to low (peptide), which fundamentally improves in vivo distribution speed and target accumulation rate, allowing imaging to be completed within the short radioisotope half-life
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 18F-ApoPep-7 compound achieves high radiochemical yield, purity, and specific radioactivity, enabling effective diagnosis of apoptosis-related diseases, including tumors and neurodegenerative conditions, with enhanced imaging capabilities compared to existing agents.
Implementation Method 1
ApoPep-1 has the characteristic of binding to histone H1, known as a nuclear protein, and binds to histone H1 protein exposed to the cell surface during apoptosis
Implementation Method 2
labeled with a positron emission radioisotope with a relatively short half-life
Implementation Method 3
18F-ApoPep-7 compound... labeled with the positron emission isotope F-18
Data Source
AI summary
The 18F-ApoPep-7 of chemical formula 1 according to the present invention, which is a derivative of 18F-ApoPep-1, has the manufacturing advantage of labeling the radioisotope F-18 with high radiochemical yield, radiochemical purify, and high specific radioactivity. Therefore, when used as an imaging drug for positron emission tomography, the 18F-ApoPep-7 of the present invention can be applied to the diagnosis of various diseases associated with apoptosis.