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Title
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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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Author
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Abstract
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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. |
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Language
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English
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Source (journal)
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European journal of medicinal chemistry. - Paris, 1974, currens
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Publication
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Paris
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2023
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ISSN
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0223-5234
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DOI
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10.1016/J.EJMECH.2023.115862
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Volume/pages
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262
(2023)
, p. 1-10
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Article Reference
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115862
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ISI
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001096361200001
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Pubmed ID
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37883899
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Medium
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E-only publicatie
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Full text (Publisher's DOI)
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Full text (open access)
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