PSMA Imaging Compound With Low Bladder and Kidney Background
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Solution Overview
Problem
Current PSMA-targeting radionuclide probes for prostate cancer diagnosis and surgery have issues with severe radionuclide retention in the bladder and high kidney background, affecting accuracy and safety, limiting their widespread application.
Innovation Solution
A compound with a specific structural formula, comprising alkali metal cations and C2-C5 alkyl groups, is synthesized through intermediate steps involving CTC resin and near-infrared dye conjugation, providing high specificity and low renal excretion for PSMA molecular imaging.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If glutamate-urea based radionuclide probes are used for PSMA targeting, then good targeting and affinity for PSMA is achieved, but severe radionuclide retention in the bladder and high radionuclide background in the kidneys occurs
Solution Approach 1:
The patent modifies the molecular structure of PSMA-targeting probes by changing chemical parameters - specifically using glutamate-alanine backbone instead of glutamate-urea, and incorporating specific amino acid sequences (Glu-Ala-Glu-Ala-Glu-Ala) to alter metabolic properties and excretion patterns, thereby reducing renal and bladder retention while maintaining PSMA affinity
Solution Approach 2:
The patent creates composite molecular structures combining specific amino acid sequences with radionuclide probes, integrating multiple functional elements (PSMA targeting motif, metabolic stability elements, and excretion control sequences) into a unified probe molecule that achieves both high targeting affinity and reduced harmful retention
2Measurement precision
If existing PSMA probes are used for preoperative diagnosis, then PSMA targeting is achieved, but accuracy is affected by severe radionuclide retention in the bladder
Solution Approach 1:
The patent changes the metabolic parameters of the probe by modifying the peptide backbone from glutamate-urea to glutamate-alanine, which alters the renal excretion kinetics and reduces bladder accumulation, thereby improving the signal-to-background ratio and detection accuracy in preoperative imaging
3Reliability
If existing PSMA probes are used for surgical navigation, then PSMA targeting is achieved, but safety is compromised by high kidney background
Solution Approach 1:
The patent modifies the molecular parameters of the probe by incorporating specific amino acid sequences (Glu-Ala-Glu-Ala-Glu-Ala) that reduce renal uptake and background signal, thereby improving safety for surgical navigation while maintaining PSMA targeting specificity for accurate lesion localization
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 compound exhibits good recognition for PSMA receptors, offering fast signal response, high resolution, and metabolic safety, enhancing PSMA detection technologies in flow cytometry and in vivo imaging with improved tumor-to-background ratios and rapid clearance.
Implementation Method 1
the compound exhibits good recognition for PSMA receptors
Implementation Method 2
Near-infrared fluorescence surgical navigation technology targeting PSMA mainly utilizes the advantages of near-infrared dyes
Data Source
AI summary
Provided in the present invention are a compound, a preparation method therefor, a composition, a kit, and the use thereof. The compound has a condensed structural formula as follows: wherein the cation M is selected from alkali metal cations, R is a C2-C5 alkyl, and n is an integer in the range of 2-5. The compound and an application product thereof have a good recognition ability and a good targeting performance for a PSMA receptor, can be widely applied to a plurality of scenarios such as flow cytometric analysis and in-vivo imaging in practical applications, and has the advantages of fast signal response speed, high resolution, good safety, excellent metabolic ability, etc.