Publication
Title
Druglike, ¹⁸F-labeled PET tracers targeting fibroblast activation protein (FAP)
Author
Abstract
Fibroblast activation protein (FAP) is a very reliable biomarker for tissue remodeling. FAP has so far mainly been studied in oncology, but there is growing interest for the enzyme in other diseases like fibrosis. Recently FAP-targeting diagnostics and therapeutics have emerged, of which the so-called FAPIs are among the most promising representatives. FAPIs typically have a relatively high molecular weight and contain very polar, multi-charged chelator moieties. While this is not limiting the application of FAPIs in oncology, more druglike FAPIs could be required to optimally study diseases characterized by denser, less permeable tissue. In response, we designed the first druglike 18F-labeled FAPIs. We report target potencies, biodistribution and pharmacokinetics and demonstrate FAP-dependent uptake in murine tumor xenografts. Finally, this paper puts forward compound 10 as a highly promising, druglike FAPI for 18F-PET imaging. This molecule is fit for additional studies in fibrosis and its preclinical profile warrants clinical investigation.
Language
English
Source (journal)
Journal of medicinal chemistry. - Washington, D.C., 1963, currens
Publication
Washington, D.C. : 2024
ISSN
0022-2623 [print]
1520-4804 [online]
DOI
10.1021/ACS.JMEDCHEM.3C02402
Volume/pages
(2024) , 20 p.
Pubmed ID
38656144
Full text (Publisher's DOI)
Full text (open access)
The author-created version that incorporates referee comments and is the accepted for publication version Available from 24.10.2024
Full text (publisher's version - intranet only)
UAntwerpen
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Affiliation
Publications with a UAntwerp address
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Record
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Creation 24.04.2024
Last edited 30.04.2024
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