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

A1 Journal article (refereed)

Internal Authors/Editors

Publication Details

List of Authors: Olli Moisio, Riikka Siitonen, Heidi Liljenbäck, Elli Suomela, Sirpa Jalkanen, Xiang-Guo Li, Anne Roivainen
Publication year: 2018
Journal: Molecules
Volume number: 23
Issue number: 305


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.

Keywords: aluminum fluoride, fluorine-18, gallium-68, inflammation, positron emission tomography, Siglec-9, VAP-1

Last updated on 2020-03-07 at 06:01