Exploring Alternative Radiolabeling Strategies for Sialic Acid-Binding Immunoglobulin-Like Lectin 9 Peptide: [Ga]Ga- and [F]AlF-NOTA-Siglec-9
Overview
Authors
Affiliations
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--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 [Ga]Ga or [F]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.
Imaging Inflammation with Positron Emission Tomography.
Iking J, Staniszewska M, Kessler L, Klose J, Luckerath K, Fendler W Biomedicines. 2021; 9(2).
PMID: 33669804 PMC: 7922638. DOI: 10.3390/biomedicines9020212.
Fersing C, Bouhlel A, Cantelli C, Garrigue P, Lisowski V, Guillet B Molecules. 2019; 24(16).
PMID: 31394799 PMC: 6719958. DOI: 10.3390/molecules24162866.