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Preclinical Evaluation of Ga/Lu-Labeled FAP-Targeted Peptide for Tumor Radiopharmaceutical Imaging and Therapy.
J Nucl Med
January 2025
Department of Nuclear Medicine, West China Hospital, Sichuan University, Chengdu, China
Fibroblast activation protein (FAP) has been considered a promising target for tumor imaging and therapy. This study designed a novel peptide, FAP-HXN, specifically targeting FAP and exhibiting significant potential as a radionuclide-labeled theranostic agent. Preclinical studies were conducted to evaluate the potency, selectivity, and efficacy of FAP-HXN.
View Article and Find Full Text PDFLu-Labeled Heterodimeric Agent with High Stability Targeting Neovascularization for Tumor Radioligand Therapy.
J Med Chem
January 2025
Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430022, China.
Radiopharmaceutical theranostics holds significant promise in tumor diagnosis and treatment, but suboptimal tumor uptake and retention remain a persistent limitation. We have conjugated a unique albumin binder to our previously developed heterodimeric precursor HX01 and achieved a novel precursor L6, aiming to prolong circulation time and enhance tumor accumulation and retention. However, we observed that the NGR sequence of L6 was gradually rearranged to iso-DGR under alkaline conditions, resulting in decreased stability.
View Article and Find Full Text PDFFully automated radiosynthesis of [F]FCPPC for imaging microglia with PET.
Am J Nucl Med Mol Imaging
December 2024
Cyclotron and Radiochemistry Core, Karmanos Cancer Institute Detroit, MI, USA.
Colony-stimulating factor 1 receptor (CSF1R) is almost exclusively expressed on microglia in the human brain and thus, has promise as a biomarker for imaging microglia density as a proxy for neuroinflammation. [C]CPPC is a radiotracer with selective affinity to CSF1R, and has been evaluated for in-human microglia PET imaging. The flourine-18 labeled CPPC derivative, 5-cyano-N-(4-(4-(2-[F]fluoroethyl)piperazin-1-yl)-2-(piperidin-1-yl)phenyl)furan-2-carboxamide ([F]FCPPC), was previously synthesized, however, with a low radiochemical yield using manual radiosynthesis.
View Article and Find Full Text PDFStrategies for specific multimodal imaging of cancer-associated fibroblasts and applications in theranostics of cancer.
Mater Today Bio
February 2025
Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing, 100142, China.
Fibroblast activating protein (FAP) is up-regulated in cancer-associated fibroblasts (CAFs) of more than 90 % of tumor microenvironment and also highly expressed on the surface of multiple tumor cells like glioblastoma, which can be used as a specific target for tumor diagnosis and treatment. At present, small-molecule radiotracer targeting FAP with high specificity exhibit limited functionality, which hinders the integration of theranostics as well as multifunctionality. In this work, we have engineered a multifunctional nanoplatform utilizing organic melanin nanoparticles that specifically targets FAP, facilitating both multimodal imaging and synergistic therapeutic applications.
View Article and Find Full Text PDFAutoradiography of Intracerebral Tumours in the Chick Embryo Model: A Feasibility Study Using Different PET Tracers.
Mol Imaging Biol
January 2025
Institute of Neuroscience and Medicine (INM-4; INM-5; INM-11), Forschungszentrum Jülich, 52425, Jülich, Germany.
Purpose: In addition to rodent models, the chick embryo model has gained attention for radiotracer evaluation. Previous studies have investigated tumours on the chorioallantoic membrane (CAM), but its value for radiotracer imaging of intracerebral tumours has yet to be demonstrated.
Procedures: Human U87 glioblastoma cells and U87-IDH1 mutant glioma cells were implanted into the brains of chick embryos at developmental day 5.
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