ArticleEJNMMI radiopharmacy and chemistry2025
Synthesis and preclinical evaluation of FAP-targeting radiotracers for PET and optical imaging.
Article in EJNMMI radiopharmacy and chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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1 citing paper in PubMed.
- Synthesis, radiolabeling, and evaluation of aFrontiers in bioengineering and biotechnology · 2026Article
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5 authors.
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Abstract
backgroundSuccessful treatment of solid cancers relies on precise diagnosis, e.g. using noninvasive molecular imaging, followed by surgical removal and/or chemo/immunotherapy. Despite advances in pre-operative imaging, real-time intraoperative tools remain limited, which often results in high rates of tumor-positive margins and recurrence after tumor resection. To address this limitation, we aimed to develop multifunctional fibroblast activation protein alpha (FAP) targeting tracers for bimodal medical imaging, enabling both pre-operative noninvasive molecular imaging via positron emission tomography (PET) and optical visualization during intraoperative fluorescence-guided surgery.
resultsNODAGA-FAP647 and NODAGA-FAP800 targeting human FAP (hFAP) were synthesized bearing a (R)-NODAGA chelator and a fluorophore (AlexaFluor647 or IRDye800CW, respectively). Binding affinities and binding kinetics of both unlabeled and
conclusionTwo FAP-targeting bimodal ligands were synthesized and evaluated in vitro and in vivo, showing high specificity and selectivity, along with rapid and selective tumor accumulation. Their long tumor retention and high imaging contrast make them promising candidates for clinical translation.
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