Publication
Title
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
Author
Abstract
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.
Language
English
Source (journal)
European journal of medicinal chemistry. - Paris, 1974, currens
Publication
Paris : 2023
ISSN
0223-5234
DOI
10.1016/J.EJMECH.2023.115862
Volume/pages
262 (2023) , p. 1-10
Article Reference
115862
ISI
001096361200001
Pubmed ID
37883899
Full text (Publisher's DOI)
Full text (open access)
UAntwerpen
Faculty/Department
Research group
Project info
Development of tools and methods for the evaluation of FAP as a predictive/prognostic biomarker in cancer.
Dipeptidyl peptidase 9 (DPP9) characterization in primary human cells.
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identifier
Creation 04.12.2023
Last edited 30.01.2024
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