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Development of a Novel Prosthetic Click-Linker for Radioiodination of Antibody-Based Radiopharmaceuticals with High Stability and Specificity.
Mol Pharm
January 2025
Division of Applied RI, Korea Institute of Radiological & Medical Sciences, Seoul 01812, Korea.
Article Synopsis
- Radioiodine is used in nuclear medicine for diagnosing and treating diseases, primarily through two methods of radioiodination: direct and indirect.
- The newly developed compound 3-[I]IBTTT offers a high radiochemical yield and purity while simplifying purification processes, overcoming issues present in traditional methods.
- This compound demonstrated effective HER2-specific binding in tumor imaging with minimal thyroid uptake, making it a promising option for targeting HER2-positive cancers.
Radioiodinated Nanobody immunoPET probe for in vivo detection of CD147 in pan-cancer.
Eur J Nucl Med Mol Imaging
November 2024
State Key Laboratory of Holistic Integrative Management of Gastrointestinal Cancers, Beijing Key Laboratory of Carcinogenesis and Translational Research, Department of Nuclear Medicine, NMPA Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), Peking University Cancer Hospital & Institute, Beijing, 100142, China.
Background: To develop the extracellular matrix metalloproteinase inducer (CD147)-targeting therapeutic strategies, accurate detection of CD147 expression in tumors is crucial. Owing to their relatively low molecular weights and high affinities, nanobodies (Nbs) may be powerful candidates for cancer diagnosis and therapy. In this study, we developed a novel CD147-targeted nanobody radiotracer, [I]I-NB147, which provides guidance for the noninvasive detection of CD147-overexpressing cancers.
View Article and Find Full Text PDFInvestigation of a Radio-Iodinated Alpha-Mangostin for Targeting Estrogen Receptor Alpha (ERα) in Breast Cancer: In Silico Design, Synthesis, and Biological Evaluation.
Drug Des Devel Ther
October 2024
Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, 260-8675, Japan.
Article Synopsis
- Alpha-mangostin (AM), derived from the Purple Mangosteen, shows potential in breast cancer treatment and is believed to interact with the estrogen receptor alpha (ERα), but no direct binding studies had been conducted until this research.* -
- This study used iodine-125 labeled AM to explore its binding to ERα in lab-grown breast cancer cells (MCF-7) and demonstrated that AM and tamoxifen can inhibit its uptake, indicating that AM's uptake involves ERα.* -
- The injected labeled AM was found to accumulate in tumors in mice, but some of the iodine-125 was lost during the process, highlighting the need for further research to improve retention and effectiveness as a breast cancer treatment
Evaluation of a Radioiodinated G-Quadruplex Binder in Cervical Cancer Models.
ChemMedChem
December 2024
C2TN-Centro de Ciências e Tecnologias Nucleares Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, 2695-066, Bobadela LRS, Portugal.
Article Synopsis
- The study details the creation of an iodine-labeled acridine orange compound ([I]-C) designed to bind G-quadruplexes, with a focus on its potential use in Auger Electron Radiopharmaceutical Therapy (AE-RPT) for treating cervical cancer.
- [I]-C showed significant cellular uptake in HeLa cervical cancer cells, leading to reduced cell viability and severe DNA damage likely caused by the emitted Auger Electrons from iodine.
- Although [I]-C exhibited fast clearance from the bloodstream and good stability, it had poor tumor uptake; combining it with the AS1411 aptamer improved blood retention but did not enhance tumor targeting, suggesting that new delivery methods need to
Preliminary Research of Radiolabeled Atezolizumab for the Noninvasive Evaluation of TNBC PD-L1 Expression In Vivo.
J Labelled Comp Radiopharm
September 2024
Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai, China.
Article Synopsis
- PD-L1 expression is linked to how well triple-negative breast cancer treatments work and patient outcomes.
- The study synthesized a new imaging agent, [I]PI-Atezolizumab, which showed stability in lab settings and maintained effective binding to PD-L1 without losing its affinity.
- Animal studies demonstrated that [I]PI-Atezolizumab has better stability and targeted imaging capabilities for PD-L1, proving useful for monitoring in triple-negative breast cancer models.
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