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Molecules 2018, 23(2), 305; doi:10.3390/molecules23020305

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.
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)
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Abstract

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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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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