Optimization of Artificial Siderophores as Ga-Complexed PET Tracers for In Vivo Imaging of Bacterial Infections.
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Authors
Peukert, CarstenLanger, Laura N B
Wegener, Sophie M
Tutov, Anna
Bankstahl, Jens P
Karge, Bianka
Bengel, Frank M
Ross, Tobias L
Brönstrup, Mark

Issue Date
2021-08-09
Metadata
Show full item recordAbstract
The 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.Citation
J Med Chem. 2021 Aug 26;64(16):12359-12378. doi: 10.1021/acs.jmedchem.1c01054. Epub 2021 Aug 9.Affiliation
HZI,Helmholtz-Zentrum für Infektionsforschung GmbH, Inhoffenstr. 7,38124 Braunschweig, Germany.Publisher
American Chemical Society (ACS)Journal
Journal of medicinal chemistryPubMed ID
34370949Type
ArticleLanguage
enEISSN
1520-4804ae974a485f413a2113503eed53cd6c53
10.1021/acs.jmedchem.1c01054
Scopus Count
The following license files are associated with this item:
- Creative Commons
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