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[F]FBC, a Covalent CLIP-Tag Radiotracer for Detection of Viral Reporter Gene Transfer in the Murine Brain.
Bioconjug Chem
February 2024
Werner Siemens Imaging Center, Department of Preclinical Imaging and Radiopharmacy, Eberhard Karls University, 72076 Tuebingen, Germany.
Preclinical models of neurological diseases and gene therapy are essential for neurobiological research. However, the evaluation of such models lacks reliable reporter systems for use with noninvasive imaging methods. Here, we report the development of a reporter system based on the CLIP-tag enzyme and [F]FBC, an F-labeled covalent CLIP-tag-ligand synthesized via a DoE-optimized and fully automated process.
View Article and Find Full Text PDFPretargeted imaging beyond the blood-brain barrier.
RSC Med Chem
March 2023
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen Universitetsparken 2 2100 Copenhagen Denmark
Pretargeting is a powerful nuclear imaging strategy to achieve enhanced imaging contrast for nanomedicines and reduce the radiation burden to healthy tissue. Pretargeting is based on bioorthogonal chemistry. The most attractive reaction for this purpose is currently the tetrazine ligation, which occurs between -cyclooctene (TCO) tags and tetrazines (Tzs).
View Article and Find Full Text PDFImaging of Gα Proteins in Mouse and Human Organs and Tissues.
Pharmaceutics
December 2022
PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical & Medicinal Chemistry, University of Bonn, D-53121 Bonn, Germany.
G protein-coupled receptors (GPCRs) transfer extracellular signals across cell membranes by activating intracellular heterotrimeric G proteins. Several studies suggested G proteins as novel drug targets for the treatment of complex diseases, e.g.
View Article and Find Full Text PDFPreclinical Identification Of Tumor-Draining Lymph Nodes Using a Multimodal Non-invasive In vivo Imaging Approach.
Mol Imaging Biol
June 2023
Werner Siemens Imaging Center, Department of Preclinical Imaging and Radiopharmacy, Eberhard Karls University, Tübingen, Germany.
Purpose: Resection of the tumor-draining lymph -node (TDLN) represents a standard method to identify metastasis for several malignancies. Interestingly, recent preclinical studies indicate that TDLN resection diminishes the efficacy of immune checkpoint inhibitor-based cancer immunotherapies. Thus, accurate preclinical identification of TDLNs is pivotal to uncovering the underlying immunological mechanisms.
View Article and Find Full Text PDFDiscovery and development of brain-penetrant F-labeled radioligands for neuroimaging of the sigma-2 receptors.
Acta Pharm Sin B
March 2022
Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
We have discovered and synthesized a series of indole-based derivatives as novel sigma-2 ( ) receptor ligands. Two ligands with high receptor affinity and subtype selectivity were then radiolabeled with F-18 in good radiochemical yields and purities, and evaluated in rodents. In biodistribution studies in male ICR mice, radioligand [F], or 1-(4-(5,6-dimethoxyisoindolin-2-yl)butyl)-4-(2-[F]fluoroethoxy)-1-indole, was found to display high brain uptake and high brain-to-blood ratio.
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