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Development of a Radiogallium-Labeled Heterodivalent Imaging Probe Targeting Negative Charges and Integrin on the Surface of Cancer Cell Membranes.
Mol Pharm
March 2025
Laboratory of Clinical Analytical Sciences, Graduate School of Medical Sciences, Kanazawa University, Kakuma-machi, Kanazawa, Ishikawa 920-1192, Japan.
Radiopharmaceuticals targeting tumor-specific environments are powerful tools for cancer diagnosis and treatment. We previously demonstrated the considerable high tumor uptake of the cationic amphiphilic peptide, Ga-NOTA-KV6, in vivo. However, because this radioligand shows a relatively rapid clearance from the tumor over time, further structural optimization is necessary.
View Article and Find Full Text PDFFAPI PET in the Management of Lung Tumors.
Semin Nucl Med
March 2025
Department of Nuclear Medicine, University Hospital Essen, University of Duisburg-Essen, Essen, Germany; German Cancer Consortium (DKTK) - University Hospital Essen, Essen, Germany.
Fibroblast activation protein (FAP), selectively expressed on activated fibroblasts in proliferating tissues, is emerging as a promising target in oncology. In lung cancer, the leading cause of cancer-related deaths worldwide, [F]FDG PET/CT has set the bar high and earned widespread recognition in clinical guidelines for its essential role in staging and follow-up. Yet, FAP-targeted imaging agents like FAPI PET/CT have demonstrated significant potential due to their high tumor specificity, rapid tracer uptake, and low background activity.
View Article and Find Full Text PDFEarly-time-point F-FDG-PET/CT and other prognostic biomarkers of survival in metastatic melanoma patients receiving immunotherapy.
Radiol Oncol
March 2025
1Department of Medical Oncology, Institute of Oncology Ljubljana, Ljubljana, Slovenia.
Background: A considerable proportion of metastatic melanoma (mM) patients do not respond to immune checkpoint inhibitors (ICIs). There is a great need to develop noninvasive biomarkers to detect patients, who do not respond to ICIs early during the course of treatment. The aim of this study was to evaluate the role of early [F]2fluoro-2-deoxy-D-glucose PET/CT (F-FDG PET/CT) at week four (W4) and other possible prognostic biomarkers of survival in mM patients receiving ICIs.
View Article and Find Full Text PDFSynthesis and evaluation of a targeted PET radioligand [F]FCOB02 for monoamine oxidase B.
Bioorg Med Chem Lett
February 2025
College of Environmental Science and Engineering, North China Electric Power University, Beijing, China. Electronic address:
Monoamine oxidase B (MAO-B) is a membrane-bound flavinase that plays an important role in the regulation of monoamine neurotransmission. Positron emission tomography (PET) provides a way to study the molecular mechanisms of MAO-B-related diseases and to evaluate the effects of drugs. In this study, we designed and synthesized [F]FCOB02, a 4-methylcoumarin-like targeting probe.
View Article and Find Full Text PDFDesign, Synthesis, and Biological Evaluation of a Novel [F]AlF-HRESCA-FAPI Radiotracer Targeting Fibroblast Activation Protein.
Pharmaceuticals (Basel)
February 2025
Department of Nuclear Medicine, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China.
Cancer-associated fibroblasts (CAFs) are key contributors to the tumorigenic process, with fibroblast activation protein (FAP) overexpressed on CAFs in numerous epithelial carcinomas. FAP represents a promising target for tumor imaging and therapy. We aimed to develop a novel [F]AlF-HRESCA-FAPI radiotracer with a high labeling yield at room temperature for positron emission tomography (PET) imaging of FAP-expressing tumors.
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