Optimization of Artificial Siderophores as Ga-Complexed PET Tracers for In Vivo Imaging of Bacterial Infections.
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Langer, Laura N B
Wegener, Sophie M
Bankstahl, Jens P
Bengel, Frank M
Ross, Tobias L
MetadataShow full item record
AbstractThe diagnosis of bacterial infections at deep body sites benefits from noninvasive imaging of molecular probes that can be traced by positron emission tomography (PET). We specifically labeled bacteria by targeting their iron transport system with artificial siderophores. The cyclen-based probes contain different binding sites for iron and the PET nuclide gallium-68. A panel of 11 siderophores with different iron coordination numbers and geometries was synthesized in up to 8 steps, and candidates with the best siderophore potential were selected by a growth recovery assay. The probes [68Ga]7 and [68Ga]15 were found to be suitable for PET imaging based on their radiochemical yield, radiochemical purity, and complex stability in vitro and in vivo. Both showed significant uptake in mice infected with Escherichia coli and were able to discern infection from lipopolysaccharide-triggered, sterile inflammation. The study qualifies cyclen-based artificial siderophores as readily accessible scaffolds for the in vivo imaging of bacteria.
CitationJ Med Chem. 2021 Aug 26;64(16):12359-12378. doi: 10.1021/acs.jmedchem.1c01054. Epub 2021 Aug 9.
AffiliationHZI,Helmholtz-Zentrum für Infektionsforschung GmbH, Inhoffenstr. 7,38124 Braunschweig, Germany.
PublisherAmerican Chemical Society (ACS)
JournalJournal of medicinal chemistry
The following license files are associated with this item:
- Creative Commons
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