Hepatocellular carcinoma (HCC) represents the predominant form of primary liver cancer, yet early, precise, and noninvasive detection continues to pose a considerable clinical challenge. Glypican-3 (GPC3), a membrane-bound proteoglycan, is markedly overexpressed in most HCC cases, while exhibiting low expression in normal and hepatitis-affected liver tissues. Given its crucial role in malignant transformation and tumor progression, GPC3 emerges as a compelling target for imaging.
View Article and Find Full Text PDFPurpose: Somatostatin receptor (SSTR) antagonists have recently emerged as preferable radiotracers for SSTR-targeted imaging and therapy. This study aimed to design a novel SSTR antagonist, [F]AlF-NOTA-Asp-PEG-JR11, and compare its preclinical performance with the previously reported antagonist, [F]AlF-NOTA-JR11, and the agonist [Ga]Ga-DOTA-TATE.
Methods: [F]AlF-NOTA-Asp-PEG-JR11 was synthesized via a one-step radiolabeling process involving [F]AlF chelation.
Recently, the folate receptor (FR) has become an exciting target for the diagnosis of FR-positive malignancies. Nevertheless, suboptimal in vivo pharmacokinetic properties, particularly high uptake in the renal and hepatobiliary systems, are important limiting factors for the clinical translation of most FR-based radiotracers. In this study, we developed a novel F-labeled FR-targeted positron emission tomography (PET) tracer [F]AlF-NOTA-Asp-PEG-Folate modified with a hydrophilic linker (-Asp-PEG) to optimize its pharmacokinetic properties and conducted a comprehensive preclinical assessment.
View Article and Find Full Text PDFGlypican-3 (GPC3) is markedly overexpressed in hepatocellular carcinoma (HCC) and not expressed in normal liver tissues. In this study, a novel peptide PET imaging agent ([F]AlF-NOTA-IPB-GPC3P) was developed to target GPC3 expressed in tumors. The overall radiochemical yield of [F]AlF-NOTA-IPB-GPC3P was 10-15 %, and its lipophilicity, expressed as the logD value at a pH of 7.
View Article and Find Full Text PDFImmunotherapy has brought great benefits to cancer patients, but only some patients benefit from it. Noninvasive, real-time and dynamic monitoring of the effectiveness of immunotherapy through PET imaging may provide assistance for the treatment plan of immunotherapy. In this study, we designed and synthesized a new targeted PD-L1 peptide NOTA-PEG-Asp-PDL1P, which was labeled with nuclide F to obtain a new imaging agent [F]AlF-NOTA-PEG-Asp-PDL1P.
View Article and Find Full Text PDFBackground: Nasopharyngeal carcinoma (NPC) is a type of head and neck malignant tumor with a high incidence in specific regional distribution, and its traditional therapies face some challenges. It has become an urgent need to seek new therapeutic strategies without or with low toxicity and side effects. At present, more and more researchers has been attracting attention by nanotheranostic platform.
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