Radiolabelling using isotopic mixtures of (52g/55)Mn(ii) offers fast and easy access to new small molecule PET/MR tracers, composed of chemically identical reporting units. trans-1,2-Diaminocyclohexane-N,N,N',N'-tetraacetic acid (CDTA) was radiolabelled with carrier-added (52g)Mn(ii) in >99% radiochemical yield, producing the first manganese-based bimodal PET/MR probe. The Mn-CDTA chelate was shown to be very stable to air oxidation and sufficiently inert to decomplexation in blood serum. These data sparked our interest in functionalized CDTA ligands for the design of optimized PET/MR tracers.
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http://dx.doi.org/10.1039/c5dt04270d | DOI Listing |
Mol Pharm
January 2025
Key Laboratory of Radiopharmaceuticals of the Ministry of Education, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), College of Chemistry, Beijing Normal University, Beijing 100875, P. R. China.
As an enzyme that plays an important role in DNA repair, poly(ADP-ribose) polymerase-1 (PARP-1) has become a popular target for cancer therapy. Nuclear medicine molecular imaging technology, supplemented by radiolabeled PARP-1 inhibitors, can accurately determine the expression level of PARP-1 at lesion sites to help patients choose an appropriate treatment plan. In this work, niraparib was modified with a hydrazinonicotinamide (HYNIC) group to generate the ligand NPBHYNIC, which has an affinity (IC) of 450.
View Article and Find Full Text PDFMolecules
December 2024
Department of Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang 45363, Indonesia.
Prostate cancer ranks as the fourth most common cancer among men, with approximately 1.47 million new cases reported annually. The emergence of prostate-specific membrane antigen (PSMA) as a critical biomarker has revolutionized the diagnosis and treatment of prostate cancer.
View Article and Find Full Text PDFA successful positron emission tomography imaging program involving carbon-11 radiotracers demands fast, efficient, and reliable synthesis methods, requiring an on-site cyclotron and radiochemistry group, as well as clinical staff trained to operate under the unique constraints of the carbon-11 radionuclide. This study examines the merits and advantages of a captive solvent 'loop method' of radiolabeling four tracers with the carbon-11 radionuclide, producing the radioligands [C]ER-176, [C]MRB, [C]mHED, and [C]PiB. The 'loop method' is compared against the traditional reactor-based method of carbon-11 methylation in the course of synthesizing the same radiotracers on the identical automated platform.
View Article and Find Full Text PDFCancer
January 2025
Stephenson Cancer Center, University of Oklahoma Health Sciences Center/Sarah Cannon Research Institute, Oklahoma City, Oklahoma, USA.
Background: Yttrium-90 FF-21101 (Y-FF-21101) is a radiopharmaceutical that targets P-cadherin as a therapy against solid tumors. A previously reported, first-in-human study determined that a dose of 25 mCi/m was safe, and a patient with clear cell carcinoma of the ovary achieved a complete response. In this article, the authors report the results of Y-FF-21101 treatment in an ovarian carcinoma expansion cohort and in patients with selected solid tumors who had known high P-cadherin expression.
View Article and Find Full Text PDFJ Med Chem
January 2025
Department of Radiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
Fibroblast activation protein (FAP), which is overexpressed in cancer-associated fibroblasts (CAFs), represents a promising target for cancer diagnosis and therapy. Hypoxia is a common feature of solid tumors. A bivalent agent, DOTA-NI-FAPI-04 (), was developed by incorporating hypoxia-sensitive nitroimidazole (NI) into the FAP-targeting agent FAPI-04.
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