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• W4291915059 endingPage "1001" @default.
• W4291915059 startingPage "1001" @default.
• W4291915059 abstract "Prostate-specific membrane antigen (PSMA)-targeting radiopharmaceuticals have become some of the most promising tools for the diagnosis and therapy prostate cancer (PCa). The structure of existing PSMA-targeted PET tracers still needs to be optimized to improve their pharmacokinetic properties and tumor-to-background ratio. In this study, we modified the structure of a well-studied PSMA tracer, and six novel tracers with variable hydrophilicity and pharmacokinetics were developed and evaluated both in vitro and in vivo. All of the novel tracers showed high hydrophilicity (log p = -2.99 ± 0.33 to -3.49 ± 0.01), rapid clearance rates (elimination half-times = 15.55 to 35.97 min), and high affinity for PSMA (Ki = 8.11 ± 0.49 to 42.40 ± 2.11 nM) in vitro. Specific cell binding and micro-PET experiments showed that [68Ga]Ga-PSMA-Q displayed the highest specific PSMA+ cell uptake (3.75 ± 0.35 IA%/106 at 60 min), tumor uptake (SUVmax = 0.97 ± 0.24 at 60 min p.i.), and tumor-to-muscle ratio (59.33 ± 5.72 at 60 min p.i.), while the tumor-to-muscle ratio was much higher than that of [68Ga]Ga-PSMA-617. The results of this study validate the clinical potential of [68Ga]Ga-PSMA-Q for PET imaging and further targeted therapy of prostate cancer." @default.
• W4291915059 created "2022-08-16" @default.
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• W4291915059 date "2022-08-14" @default.
• W4291915059 modified "2023-10-14" @default.
• W4291915059 title "Optimized 68Ga-Labeled Urea-Based PSMA-Targeted PET Tracers for Prostate Cancer" @default.
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• W4291915059 doi "https://doi.org/10.3390/ph15081001" @default.
• W4291915059 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36015149" @default.
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