In Vivo Imaging of GLP-1R with a Targeted Bimodal PET/Fluorescence Imaging Agent
| العنوان: | In Vivo Imaging of GLP-1R with a Targeted Bimodal PET/Fluorescence Imaging Agent |
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| المؤلفون: | Wolfgang Weber, Thomas Reiner, Christian Brand, Yachao Zhang, Susan M. Clardy, Jason S. Lewis, Sean Carlin, Dalya Abdel-Atti, Edmund J. Keliher |
| المصدر: | Bioconjugate Chemistry |
| بيانات النشر: | American Chemical Society, 2014. |
| سنة النشر: | 2014 |
| مصطلحات موضوعية: | Fluorescence-lifetime imaging microscopy, Pharmaceutical Science, Fluorescent Antibody Technique, Multimodal Imaging, 030218 nuclear medicine & medical imaging, Mice, 0302 clinical medicine, Receptors, Glucagon, Cells, Cultured, medicine.diagnostic_test, Chemistry, Optical Imaging, Adenoma, Islet Cell, Fluorescence, Imaging agent, 3. Good health, medicine.anatomical_structure, Positron emission tomography, Cell Tracking, 030220 oncology & carcinogenesis, Female, Pancreas, Preclinical imaging, Biotechnology, Molecular Sequence Data, Biomedical Engineering, Mice, Nude, Bioengineering, Article, Glucagon-Like Peptide-1 Receptor, 03 medical and health sciences, In vivo, medicine, Animals, Humans, Hypoglycemic Agents, Amino Acid Sequence, Pharmacology, business.industry, Venoms, Organic Chemistry, Xenograft Model Antitumor Assays, Copper Radioisotopes, Positron-Emission Tomography, Exenatide, Radiopharmaceuticals, Nuclear medicine, business, Peptides, Ex vivo, Biomedical engineering |
| الوصف: | Accurate visualization and quantification of β-cell mass is critical for the improved understanding, diagnosis, and treatment of both type 1 diabetes (T1D) and insulinoma. Here, we describe the synthesis of a bimodal imaging probe (PET/fluorescence) for imaging GLP-1R expression in the pancreas and in pancreatic islet cell tumors. The conjugation of a bimodal imaging tag containing a near-infrared fluorescent dye, and the copper chelator sarcophagine to the GLP-1R targeting peptide exendin-4 provided the basis for the bimodal imaging probe. Conjugation was performed via a novel sequential one-pot synthetic procedure including (64)Cu radiolabeling and copper-catalyzed click-conjugation. The bimodal imaging agent (64)Cu-E4-Fl was synthesized in good radiochemical yield and specific activity (RCY = 36%, specific activity: 141 μCi/μg, >98% radiochemical purity). The agent showed good performance in vivo and ex vivo, visualizing small xenografts ( |
| اللغة: | English |
| تدمد: | 1520-4812 1043-1802 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6aaeaa66877491bf57083b8e075e26b7 http://europepmc.org/articles/PMC4215873 |
| Rights: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....6aaeaa66877491bf57083b8e075e26b7 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 15204812 10431802 |
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