A1 Refereed original research article in a scientific journal

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




AuthorsMoisio Olli, Siitonen Riikka, Liljenbäck Heidi, Suomela Elli, Jalkanen Sirpa, Li Xiang-Guo, Roivainen Anne

PublisherMDPI AG

Publishing placeBasel, Switzerland

Publication year2018

JournalMolecules

Journal acronymMolecules

Article numberE305

Volume23

Issue2

Number of pages8

ISSN1420-3049

eISSN1420-3049

DOIhttps://doi.org/10.3390/molecules23020305

Web address http://www.mdpi.com/1420-3049/23/2/305

Self-archived copy’s web addresshttps://research.utu.fi/converis/portal/detail/Publication/29414392


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.


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