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Preclinical and First-in-Human Study of a Compact Radionuclide Labeled Self-Assembly Nanomedicine for Chemo-Radio-Theranostics of Cancer.
ACS Nano
January 2025
Department of Diagnostic Radiology, Yong Loo Lin School of Medicine, National University of Singapore, 119074, Singapore.
The emerging combination of chemotherapy and radionuclide therapy has been actively investigated to overcome the limitations of monotherapy and augment therapeutic efficacy. However, it remains a challenge to design a single delivery vehicle that can incorporate chemotherapeutics and radionuclides into a compact structure. Here, a chelator DOTA- or NOTA-modified Evans blue conjugated camptothecin molecule (EB-CPT) nanoprodrug was synthesized, which could self-assemble into nanoparticles due to its inherent amphiphilicity.
View Article and Find Full Text PDFSynthesis and characterisation of DOTA-kisspeptin-10 as a potential gallium-68/lutetium-177 pan-tumour radiopharmaceutical.
J Neuroendocrinol
January 2025
Centre for Neuroendocrinology, University of Pretoria, Pretoria, South Africa.
Kisspeptin (KISS1) and its cognate receptor (KISS1R) are implicated in the progression of various cancers. A gallium-68 labelled kisspeptin-10 (KP10), the minimal biologically active structure, has potential as a pan-tumour radiopharmaceutical for the detection of cancers. Furthermore, a lutetium-177 labelled KP10 could find therapeutic application in treating oncological diseases.
View Article and Find Full Text PDFMathematic Modeling of Tumor Growth During [Lu]Lu-PSMA Therapy: Insights into Treatment Optimization.
J Nucl Med
January 2025
Department of Radiology and Radiological Science, Johns Hopkins University School of Medicine, Baltimore, Maryland; and.
The treatment regimen for [Lu]Lu-prostate-specific membrane antigen (PSMA) 617 therapy follows that of chemotherapy: 6 administrations of a fixed activity, each separated by 6 wk. Mathematic modeling can be used to test the hypothesis that the current treatment regimen for a radiopharmaceutical modality is suboptimal. A mathematic model was developed to describe tumor growth during [Lu]Lu-PSMA therapy.
View Article and Find Full Text PDFComparative Study of Dimeric Fibroblast Activation Protein-Targeting Radioligands Labeled with Fluorine-18, Copper-64, and Gallium-68.
Mol Pharm
December 2024
Department of Nuclear Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul 06351, Republic of Korea.
Fibroblast activation protein inhibitors (FAPIs) labeled with gallium-68 and lutetium-177 show potential for use in the diagnosis and treatment of various cancers expressing FAP. However, Lu-labeled FAPIs often exhibit short tumor retention time, limiting their therapeutic applications. To improve tumor retention, we synthesized three radiolabeled dimeric FAPIs, [F], [Cu], and [Ga].
View Article and Find Full Text PDFRADIOPHARMACEUTICALS BASED ON ANTAGONISTS OF CHEMOCINE RECEPTOR CXCR4 IN DIAGNOSTICS AND TREATMENT OF ONCOLOGICAL DISEASES.
Probl Radiac Med Radiobiol
December 2024
Nonprofit Organization «National Cancer Institute of Ministry of Health of Ukraine», 33/43 Julia Zdanovska Str., Kyiv, 03022, Ukraine.
The review is devoted to the use of a new class of radiopharmaceuticals (RPs) - chemokine receptor ligands - in oncological practice. The chemokine receptor CXCR4 is of particular interest as a molecular target in the diagnosis and treatment of malignant tumors, as it plays an important role in carcinogenesis. By interacting with the chemokine CCXL12, it activates cell signaling pathways that affect tumor cell proliferation, angiogenesis, metastasis growth, and apoptosis inhibition.
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