ArticleBioconjugate chemistry2014
In vivo imaging of GLP-1R with a targeted bimodal PET/fluorescence imaging agent.
Article in Bioconjugate chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 55 citations in OpenAlex.
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- A New Dual-peak Fluorescent Probe for Water Content Detection Made From Taxus.Journal of fluorescence · 2022Article
- Dual-Labelling Strategies for Nuclear and Fluorescence Molecular Imaging: Current Status and Future Perspectives.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Optoacoustic Imaging of Glucagon-like Peptide-1 Receptor with a Near-Infrared Exendin-4 Analog.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2021Article
- Role of PET/CT and Therapy Management of Pancreatic Neuroendocrine Tumors.Diagnostics (Basel, Switzerland) · 2020Review
- Targeted Optical Imaging of the Glucagonlike Peptide 1 Receptor Using Exendin-4-IRDye 800CW.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2020Article
- Synthesis and in vivo behaviour of an exendin-4-based MRI probe capable of β-cell-dependent contrast enhancement in the pancreas.Dalton transactions (Cambridge, England : 2003) · 2020Article
- Innovative imaging of insulinoma: the end of sampling? A review.Endocrine-related cancer · 2020Review
- Advances in GLP-1 receptor targeting radiolabeled agent development and prospective of theranostics.Theranostics · 2020Review
- Exendin-4 analogs in insulinoma theranostics.Journal of labelled compounds & radiopharmaceuticals · 2019Review
- Molecular imaging of β-cells: diabetes and beyond.Advanced drug delivery reviews · 2019Review
- Targets and probes for non-invasive imaging of β-cells.European journal of nuclear medicine and molecular imaging · 2017Review
- Imaging in pancreatic disease.Nature reviews. Gastroenterology & hepatology · 2017Review
- Hybrid intraoperative imaging techniques in radioguided surgery: present clinical applications and future outlook.Clinical and translational imaging · 2017Review
- A Helix-Stabilizing Linker Improves Subcutaneous Bioavailability of a Helical Peptide Independent of Linker Lipophilicity.Bioconjugate chemistry · 2016Article
- Quantitative Impact of Plasma Clearance and Down-regulation on GLP-1 Receptor Molecular Imaging.Molecular imaging and biology · 2016Article
- The bone-preserving effects of exendin-4 in ovariectomized rats.Endocrine · 2016Article
- Bioorthogonal Fluorophore Linked DFO-Technology Enabling Facile Chelator Quantification and Multimodal Imaging of Antibodies.Bioconjugate chemistry · 2016Article
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
Abstract
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 (<2 mm) with PET and pancreatic β-cell mass by phosphor autoradiography. Using the fluorescent properties of the probe, we were able to detect individual pancreatic islets, confirming specific binding to GLP-1R and surpassing the sensitivity of the radioactive label. The use of bimodal PET/fluorescent imaging probes is promising for preoperative imaging and fluorescence-assisted analysis of patient tissues. We believe that our procedure could become relevant as a protocol for the development of bimodal imaging agents.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.