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Open AccessFeature PaperArticle

Exploring Alternative Radiolabeling Strategies for Sialic Acid-Binding Immunoglobulin-Like Lectin 9 Peptide: [68Ga]Ga- and [18F]AlF-NOTA-Siglec-9

1
Turku PET Centre, University of Turku, FI-20521 Turku, Finland
2
Turku Center for Disease Modeling, University of Turku, FI-20520 Turku, Finland
3
MediCity Research Laboratory, University of Turku, FI-20520 Turku, Finland
4
Turku PET Centre, Åbo Akademi University, FI-20521 Turku, Finland
5
Turku PET Centre, Turku University Hospital, FI-20521 Turku, Finland
*
Author to whom correspondence should be addressed.
Molecules 2018, 23(2), 305; https://doi.org/10.3390/molecules23020305
Received: 10 January 2018 / Revised: 26 January 2018 / Accepted: 29 January 2018 / Published: 31 January 2018
(This article belongs to the Special Issue Medicinal Chemistry in Europe)
Amino acid residues 283–297 from sialic acid-binding immunoglobulin-like lectin 9 (Siglec-9) form a cyclic peptide ligand targeting vascular adhesion protein-1 (VAP-1). VAP-1 is associated with the transfer of leukocytes from blood to tissues upon inflammation. Therefore, analogs of Siglec-9 peptide are good candidates for visualizing inflammation non-invasively using positron emission tomography (PET). Gallium-68-labeled 1,4,7,10-tetraazacyclododecane-N,N′,N″,N‴-tetraacetic acid (DOTA)-conjugated Siglec-9 has been evaluated extensively for this purpose. Here, we explored two alternative strategies for radiolabeling Siglec-9 peptide using a 1,4,7-triazacyclononane-triacetic acid (NOTA)-chelator to bind [68Ga]Ga or [18F]AlF. The radioligands were evaluated by in vivo PET imaging and ex vivo γ-counting of turpentine-induced sterile skin/muscle inflammation in Sprague-Dawley rats. Both tracers showed clear accumulation in the inflamed tissues. The whole-body biodistribution patterns of the tracers were similar. View Full-Text
Keywords: aluminum fluoride; fluorine-18; gallium-68; inflammation; positron emission tomography; Siglec-9; VAP-1 aluminum fluoride; fluorine-18; gallium-68; inflammation; positron emission tomography; Siglec-9; VAP-1
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Moisio, O.; Siitonen, R.; Liljenbäck, H.; Suomela, E.; Jalkanen, S.; Li, X.-G.; Roivainen, A. Exploring Alternative Radiolabeling Strategies for Sialic Acid-Binding Immunoglobulin-Like Lectin 9 Peptide: [68Ga]Ga- and [18F]AlF-NOTA-Siglec-9. Molecules 2018, 23, 305.

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