(18)F-Based Pretargeted PET Imaging Based on Bioorthogonal Diels–Alder Click Chemistry

[Image: see text] A first-of-its-kind (18)F pretargeted PET imaging approach based on the bioorthogonal inverse electron demand Diels–Alder (IEDDA) reaction between tetrazine (Tz) and trans-cyclooctene (TCO) is presented. As proof-of-principle, a TCO-bearing immunoconjugate of the anti-CA19.9 antibo...

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Detalles Bibliográficos
Autores principales: Meyer, Jan-Philip, Houghton, Jacob L., Kozlowski, Paul, Abdel-Atti, Dalya, Reiner, Thomas, Pillarsetty, Naga Vara Kishore, Scholz, Wolfgang W., Zeglis, Brian M., Lewis, Jason S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2015
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4759614/
https://www.ncbi.nlm.nih.gov/pubmed/26479967
http://dx.doi.org/10.1021/acs.bioconjchem.5b00504
Descripción
Sumario:[Image: see text] A first-of-its-kind (18)F pretargeted PET imaging approach based on the bioorthogonal inverse electron demand Diels–Alder (IEDDA) reaction between tetrazine (Tz) and trans-cyclooctene (TCO) is presented. As proof-of-principle, a TCO-bearing immunoconjugate of the anti-CA19.9 antibody 5B1 and an Al[(18)F]NOTA-labeled tetrazine radioligand were harnessed for the visualization of CA19.9-expressing BxPC3 pancreatic cancer xenografts. Biodistribution and (18)F-PET imaging data clearly demonstrate that this methodology effectively delineates tumor mass with activity concentrations up to 6.4 %ID/g at 4 h after injection of the radioligand.

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