研究目的
Investigating the therapeutic effects of multifunctional fluorescent inhibitors targeting PSMA and hypoxia for prostate cancer.
研究成果
The study concludes that multifunctional inhibitors combining PSMA and hypoxia targeting moieties show higher tumor uptake than inhibitors targeting PSMA alone, suggesting a promising approach for improving prostate cancer diagnosis and therapy.
研究不足
The study is limited by the technical constraints of the experimental methods used, such as the potential influence of the bulky structure of the hypoxia-sensitive group on the inhibitory activity of the multifunctional inhibitors. Additionally, the application of these inhibitors in clinical settings requires further optimization and validation.
1：Experimental Design and Method Selection:
Novel PSMA inhibitors were prepared using lysine as the backbone to connect three different functional groups: the glutamate-urea-lysine (GUL) structure for inhibiting PSMA, 2-nitroimidazole for the hypoxia-sensitive moiety, and a near-infrared fluorophore (sulfo-Cyanine
2：5). Sample Selection and Data Sources:
LNCaP cell lysates were obtained using lysis buffer for in vitro PSMA inhibition assay.
3：List of Experimental Equipment and Materials:
Chemicals and solvents were purchased from Sigma-Aldrich, 2-Nitroimidazole from Futurechem, and the NHS ester of Sulfo-Cyanine
4：5 from Lumiprobe. Experimental Procedures and Operational Workflow:
Synthesis of inhibitors, in vitro PSMA inhibition assay, in vivo and ex vivo imaging and biodistribution assay.
5：Data Analysis Methods:
Enzyme inhibitory constants (Ki values) were derived from the IC50 values using GraphPad Prism version 7.00.
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