Optimization of Artificial Siderophores as Ga-Complexed PET Tracers for In Vivo Imaging of Bacterial Infections.
Cast your vote
You can rate an item by clicking the amount of stars they wish to award to this item.
When enough users have cast their vote on this item, the average rating will also be shown.
Your vote was cast
Thank you for your feedback
Thank you for your feedback
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
- <sup>67</sup>Ga-labeled deferoxamine derivatives for imaging bacterial infection: Preparation and screening of functionalized siderophore complexes.
- Authors: Ioppolo JA, Caldwell D, Beiraghi O, Llano L, Blacker M, Valliant JF, Berti PJ
- Issue date: 2017 Sep
- <sup>68</sup>Ga-labelled desferrioxamine-B for bacterial infection imaging.
- Authors: Petrik M, Umlaufova E, Raclavsky V, Palyzova A, Havlicek V, Pfister J, Mair C, Novy Z, Popper M, Hajduch M, Decristoforo C
- Issue date: 2021 Feb
- Imaging of Pseudomonas aeruginosa infection with Ga-68 labelled pyoverdine for positron emission tomography.
- Authors: Petrik M, Umlaufova E, Raclavsky V, Palyzova A, Havlicek V, Haas H, Novy Z, Dolezal D, Hajduch M, Decristoforo C
- Issue date: 2018 Oct 24
- Modifying the Siderophore Triacetylfusarinine C for Molecular Imaging of Fungal Infection.
- Authors: Kaeopookum P, Summer D, Pfister J, Orasch T, Lechner BE, Petrik M, Novy Z, Matuszczak B, Rangger C, Haas H, Decristoforo C
- Issue date: 2019 Dec
- In vitro and in vivo evaluation of selected 68Ga-siderophores for infection imaging.
- Authors: Petrik M, Haas H, Schrettl M, Helbok A, Blatzer M, Decristoforo C
- Issue date: 2012 Apr