(18)F-based pretargeted PET imaging based on bioorthogonal Diels-Alder click chemistry Journal Article


Authors: Meyer, J. P.; Houghton, J. L.; Kozlowski, P.; Abdel-Atti, D.; Reiner, T.; Pillarsetty, N. V. K.; Scholz, W. W.; Zeglis, B. M.; Lewis, J. S.
Article Title: (18)F-based pretargeted PET imaging based on bioorthogonal Diels-Alder click chemistry
Abstract: A first-of-its-kind 18F 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[18F]NOTA-labeled tetrazine radioligand were harnessed for the visualization of CA19.9-expressing BxPC3 pancreatic cancer xenografts. Biodistribution and 18F-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. © 2015 American Chemical Society.
Journal Title: Bioconjugate Chemistry
Volume: 27
Issue: 2
ISSN: 1043-1802
Publisher: American Chemical Society  
Date Published: 2016-02-17
Start Page: 298
End Page: 301
Language: English
DOI: 10.1021/acs.bioconjchem.5b00504
PROVIDER: scopus
PMCID: PMC4759614
PUBMED: 26479967
DOI/URL:
Notes: Article -- Export Date: 4 April 2016 -- Source: Scopus
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  1. Jason S Lewis
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  2. Thomas Reiner
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  3. Jan-Philip   Meyer
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