The macrocyclic bone-seeking agent, DO2A2P, bears a cyclen core and two pairs of peripheral phosphonate and carboxylate groups. The geometric disposition of the peripheral functionalities gives arise to a pair of geometric isomers: cis-DO2A2P and trans-DO2A2P. In order to compare the biological behavior of the isomer pair, cis-DO2A2P was synthesized. Both isomers were successfully radiolabeled with (177)Lu, which might potentiate their applications in both radiotherapy and imaging of bone diseases. Through a set of biological assays including the hydroxyapatite binding, in vitro stability, and in vivo distribution, we demonstrated that the geometric pair of DO2A2P had virtually identical biological properties.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4386885 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2014.12.016 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Pros and Cons of Alpha versus Beta Bone Seeking Agents in the Treatment of Cancer Pain.
World J Nucl Med
December 2023
Department of Nuclear Medicine, Klinikum Frankfurt (Oder), Brandenburg, Germany.
Bone Metastasis in Prostate Cancer: Bone Scan Versus PET Imaging.
Semin Nucl Med
January 2024
Division of Molecular Imaging and Theranostics, Department of Nuclear Medicine, University Hospital, Paracelsus Medical University, Salzburg, Austria. Electronic address:
Prostate cancer is the second most common cause of malignancy among men, with bone metastasis being a significant source of morbidity and mortality in advanced cases. Detecting and treating bone metastasis at an early stage is crucial to improve the quality of life and survival of prostate cancer patients. This objective strongly relies on imaging studies.
View Article and Find Full Text PDFHierarchically Released Liquid Metal Nanoparticles for Mild Photothermal Therapy/Chemotherapy of Breast Cancer Bone Metastases via Remodeling Tumor Stromal Microenvironment.
Adv Healthc Mater
October 2023
State Key Laboratory of New Textile Materials and Advanced Processing Technologies, Wuhan Textile University, No. 1 Sunshine Avenue, Jiangxia District, Wuhan, Hubei Province, 430200, China.
Currently, the treatment strategy for bone metastasis is mainly to inhibit the growth of tumor cells and the activity of osteoclasts, while ignoring the influence of the tumor stromal microenvironment (TSM) on the progression of bone metastasis. Herein, a dual-target liquid metal (LM)-based drug delivery system (DDS) with favorable photothermal performance is designed to spatially program the delivery of multiple therapeutic agents to enhance the treatment of bone metastasis through TSM remodeling. Briefly, mesoporous silicon-coated LM is integrated into zeolitic imidazolate framework-8 (ZIF-8) with both bone-seeking and tumor-targeting capacities.
View Article and Find Full Text PDFPhase I evaluation of CycloSam (Sm-153-DOTMP) bone seeking radiopharmaceutical in dogs with spontaneous appendicular osteosarcoma.
Vet Radiol Ultrasound
September 2023
Department of Veterinary Medicine and Surgery, College of Veterinary Medicine, University of Missouri, Columbia, Missouri, USA.
Sm-DOTMP (CycloSam ) is a newly-patented radiopharmaceutical for bone tumor treatment. DOTMP (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylene-phosphonate) is a macrocyclic chelating agent with superior binding properties to Sm when compared with EDTMP (Quadramet™, used for palliative treatment of bone cancer). CycloSam was administered at 1 mCi/kg (37 MBq/kg) in a prospective pilot study to seven dogs with bone cancer resulting in no myelosuppression.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!