Next generation fibroblast activation protein (FAP) targeting PET tracers : The tetrazine ligation allows an easy and convenient way to 18F-labeled (4-quinolinoyl)glycyl-2-cyanopyrrolidines
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Small-molecular fibroblast activation protein inhibitor (FAPI)-based tracer have been shown to be promising Positron Emission Tomography (PET) 68Ga-labeled radiopharmaceuticals to image a variety of tumors including pancreatic, breast, and colorectal cancers, among others. In this study, we developed a novel 18F-labeled FAPI derivative. [18F]6 was labeled using a synthon approach based on the tetrazine ligation. It showed subnanomolar affinity for the FAP protein and a good selectivity profile against known off-target proteases. Small animal PET studies revealed high tumor uptake and good target-to-background ratios. [18F]6 was excreted via the liver. Overall, [18F]6 showed promising characteristics to be used as a PET tracer and could serve as a lead for further development of halogen-based theranostic FAPI radiopharmaceuticals.
Originalsprog | Engelsk |
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Artikelnummer | 115862 |
Tidsskrift | European Journal of Medicinal Chemistry |
Vol/bind | 262 |
Antal sider | 10 |
ISSN | 0223-5234 |
DOI | |
Status | Udgivet - 2023 |
Bibliografisk note
Funding Information:
The authors thank the Danish Research Council for Independent Research (grant agreement no. 8022-00358B ) for financial support. Yentl Van Rymenant was supported by the FWO-SB fellowship ( 1S64222 N ) and Joni De Loose was supported by FWO-FR fellowship ( 11B3322 N ).
Publisher Copyright:
© 2023 The Authors
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