ArticleEuropean journal of nuclear medicine and molecular imaging2023
Organotrifluoroborate enhances tumor targeting of fibroblast activation protein inhibitors for targeted radionuclide therapy.
Article in European journal of nuclear medicine and molecular imaging, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Bridging the gaps in fibroblast activation protein targeted radionuclide therapy: a translational perspective.European journal of nuclear medicine and molecular imaging · 2026Review
- Head-to-head comparison ofEuropean journal of nuclear medicine and molecular imaging · 2025Article
- Pharmacokinetics study of FT-FAPI, a novel multi-nuclide label-able FAP targeting tracer, in mice and healthy volunteers.European journal of nuclear medicine and molecular imaging · 2025Article
- Chelator Optimization and Therapeutic Potential ofACS medicinal chemistry letters · 2025Article
- The molar dose of FAPI administered impacts on the FAP-targeted PET imaging and therapy in mouse syngeneic tumor models.European journal of nuclear medicine and molecular imaging · 2025Article
- An overview of the role of radionuclides in targeted cancer treatment: application of biomarkers for patient selection and developments to improve treatment efficacy.Frontiers in oncology · 2025Review
- Fluorine-18 incorporation and radiometal coordination in macropa ligands for PET imaging and targeted alpha therapy.Chemical communications (Cambridge, England) · 2024Article
- Article
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Authors and funding
9 authors.
Funding
Abstract
purposeFibroblast activation protein (FAP) is a pan-cancer target and now the state-of-the-art to develop radiopharmaceuticals. FAP inhibitors have been of great success in developing imaging tracers. Yet, the overly rapid clearance cannot match with the long half-lives of regular therapeutic radionuclides. Though strategies that aim to elongate the circulation of FAPIs are being developed, here we describe an innovation that uses α-emitters of short half-lives (e.g.,
methodsAn organotrifluoroborate linker is engineered to FAPIs to give two advantages: (1) selectively increases tumor uptake and retention; (2) facile
resultsThe organotrifluoroborate linker helps to improve the internalization in cancer cells, resulting in notably higher tumor uptake while the background is clean. In FAP-expressed tumor-bearing mice, this FAPI labeled with
conclusionThe organotrifluoroborate linker may be of importance to optimize FAP-targeted radiopharmaceuticals, and the short half-lived α-emitters may be of choice for the rapid-cleared small molecule-based radiopharmaceuticals.
Indexed as
Identifiers
37103565What Socratic holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.