2020
DOI: 10.3390/molecules25092123
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Hybrid Imaging Agents for Pretargeting Applications Based on Fusarinine C—Proof of Concept

Abstract: Hybrid imaging combining the beneficial properties of radioactivity and optical imaging within one imaging probe has gained increasing interest in radiopharmaceutical research. In this study, we modified the macrocyclic gallium-68 chelator fusarinine C (FSC) by conjugating a fluorescent moiety and tetrazine (Tz) moieties. The resulting hybrid imaging agents were used for pretargeting applications utilizing click reactions with a trans-cyclooctene (TCO) tagged targeting vector for a proof of principle both in v… Show more

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Cited by 9 publications
(10 citation statements)
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“…Because TCO exhibits greater in vivo stability than Tz, the overwhelming majority of IEDDA-based pretargeting strategies employ a TCO-modified immunoconjugate alongside a Tz-bearing radioligand (Figure ). Since our last review, a remarkable surge in the field has yielded pretargeting systems featuring radioligands labeled with gamma-emitters (i.e., 99m Tc and 111 In), β + -emitters (i.e., 68 Ga, 18 F, 64 Cu, 44 Sc, and 89 Zr), , β – -emitters (i.e., 177 Lu and 67 Cu), and α-emitters (i.e., 212 Pb, 211 At, and 225 Ac). , …”
Section: The Inverse Electron-demand Diels–alder Reactionmentioning
confidence: 99%
“…Because TCO exhibits greater in vivo stability than Tz, the overwhelming majority of IEDDA-based pretargeting strategies employ a TCO-modified immunoconjugate alongside a Tz-bearing radioligand (Figure ). Since our last review, a remarkable surge in the field has yielded pretargeting systems featuring radioligands labeled with gamma-emitters (i.e., 99m Tc and 111 In), β + -emitters (i.e., 68 Ga, 18 F, 64 Cu, 44 Sc, and 89 Zr), , β – -emitters (i.e., 177 Lu and 67 Cu), and α-emitters (i.e., 212 Pb, 211 At, and 225 Ac). , …”
Section: The Inverse Electron-demand Diels–alder Reactionmentioning
confidence: 99%
“…Introduction of fluorescent dye (185) to produce a hybrid imaging modality resulted in rapid uptake in A. fumigatus in vitro, and in an infected lung model in rats showed high fluorescent signal levels that were comparable to a PET/CT scan. This demonstrates the potential applicability of siderophores for hybrid imaging, with possible applications in surgical procedures and bioluminescence in humans (186). A group of researchers in the UK did some preliminary in vitro uptake of [ 68 Ga]Ga-ferrichrome C (a fungal siderophore) using E. coli in iron-deficient medium, and in vascular stents incubated with E. coli cells (187).…”
Section: Recent Development Of Siderophore Based Metal Chelatorsmentioning
confidence: 99%
“…Table 2) [67]. Despite their similar thermodynamic stability (Alternative macrocyclic chelators [69][70][71][72][73][74] and acyclic chelators [70,[75][76][77][78][79] have been developed for 89 Zr. Pandya et al were one of the first groups to label DOTA with 89 Zr [69], and more recently, they have extended the application to other polyazamacrocycles [74].…”
Section: Novel Chelators For 89 Zrmentioning
confidence: 99%