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Monovalent and Divalent Designs of Copper Radiotheranostics Targeting Fibroblast Activation Protein in Cancer.
Cancers (Basel)
December 2024
Department of Radiology, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
: Fibroblast activation protein (FAP)-targeted theranostic radiopharmaceuticals have shown desired tumor-to-background organ selectivity due to the ubiquitous presence of FAP within the tumor microenvironment. However, suboptimal tumor retention and fast clearance have hindered their use to deliver effective cancer therapies. With well-documented FAP-targeting moieties and linkers appending them to optimal chelators, the development of copper radiopharmaceuticals has attracted considerable interest, given the fact that an ideal theranostic pair of copper radionuclides (Cu: t = 12.
View Article and Find Full Text PDFRadiopharmaceuticals and their applications in medicine.
Signal Transduct Target Ther
January 2025
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 100050, Beijing, China.
Article Synopsis
- Radiopharmaceuticals deliver radionuclides to specific lesions, providing targeted diagnosis and treatment for diseases, particularly those resistant to standard therapies.
- The FDA's approval of agents like [Lu]Lu-DOTA-TATE and [Ga]Ga-PSMA-11 marks significant progress in clinical oncology, enhancing the use of radiotheranostics in personalized medicine.
- Advancements in radiopharmaceutical development focus on targeting a wider array of diseases, improving therapeutic efficacy, and expanding applications to neurodegenerative and cardiovascular conditions.
Novel Radiotheranostic Ligands Targeting Prostate-Specific Membrane Antigen Based on Dual Linker Approach.
Mol Pharm
January 2025
Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
Radiotheranostics using prostate-specific membrane antigen (PSMA)-targeting radioligands offers precision medicine by performing radionuclide therapy based on results of diagnosis. Albumin binder (ALB) binds to albumin reversibly and contributes to effective radiotheranostics by enhancing tumor accumulation of PSMA-targeting radioligands. We newly developed two ALB-containing PSMA-targeting radioligands including dual functional linkers, a hydrophilic linker, d-glutamic acid, and a hydrophobic linker, 4-(aminomethyl)benzoic acid, with the opposite arrangement (PNT-DA6 and PNT-DA7).
View Article and Find Full Text PDFA cascade X-ray energy converting approach toward radio-afterglow cancer theranostics.
Nat Nanotechnol
November 2024
School of Chemistry, Chemical Engineering and Biotechnology, Nanyang Technological University, Singapore, Singapore.
Leveraging X-rays to initiate prolonged luminescence (radio-afterglow) and stimulate radiodynamic O production from optical agents provides opportunities for diagnosis and therapy at tissue depths inaccessible to light. However, X-ray-responsive organic luminescent materials are rare due to their intrinsic low X-ray conversion efficiency. Here we report a cascade X-ray energy converting approach to develop organic radio-afterglow nanoprobes (RANPs) for cancer theranostics.
View Article and Find Full Text PDFAssembling a new generation of radiopharmaceuticals with supramolecular theranostics.
Nat Rev Chem
December 2024
Department of Chemistry, School of Natural Sciences, Technical University of Munich, Garching bei München, Germany.
Supramolecular chemistry has been used to tackle some of the major challenges in modern science, including cancer therapy and diagnosis. Supramolecular platforms provide synthetic flexibility, rapid generation through self-assembly, facile labelling, unique topologies, tunable reversibility of the enabling noncovalent interactions, and opportunities for host-guest chemistry and mechanical bonding. In this Review, we summarize recent advances in the design and radiopharmaceutical application of discrete self-assembled coordination complexes and mechanically interlocked molecules - namely, metallacages and rotaxanes, respectively - as well as in situ-forming supramolecular aggregates, specifically pinpointing their potential as next-generation radiotheranostic agents.
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