ArticleEJNMMI radiopharmacy and chemistry2020
Targeting fibroblast activation protein (FAP): next generation PET radiotracers using squaramide coupled bifunctional DOTA and DATA
Article in EJNMMI radiopharmacy and chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 65 papers.
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Who cites it
65 citing papers in PubMed, 111 citations in OpenAlex.
- Preclinical evaluation of homodimeric FAPI target modules for UniCAR-mediated targeting of FAP-expressing tumor and stromal cells.Oncoimmunology · 2026Article
- Optimizing FAPI homodimers for theranostic applications: The impact of the linker design in DOTAGA.GluEuropean journal of nuclear medicine and molecular imaging · 2026Article
- [⁶⁸Ga]Ga-CTR-FAPI versus [⁶⁸Ga]Ga-FAPI-04 PET/CT for patient evaluation in radioiodine-refractory differentiated thyroid cancer: A prospective comparative study.European journal of nuclear medicine and molecular imaging · 2026Article
- FAP-Inhibitor Homodimers with Engineered Linker-Spacer Units: Toward Optimized Radiopharmaceuticals.ACS omega · 2026Article
- The Evolution of FAP-Targeted CAR T-Cell Therapy in Solid Tumors: From Immunotherapy to Immunotheranostic Applications.International journal of molecular sciences · 2026Review
- FAPI Dimerization for Theranostic Applications: Molecular Design, Preclinical Validation, and Clinical Translation.Chemical & biomedical imaging · 2026Review
- Head-to-Head Comparison of Monomeric, Homodimeric, and Heterodimeric Fibroblast Activation Protein-Targeting Radioligands Based on Small Molecule Inhibitor and Cyclic Peptide.ACS pharmacology & translational science · 2026Article
- Fibroblast Activation Protein Inhibitor (FAPI) PET: A Scoping Review of Emerging Oncologic and Fibroinflammatory Applications.Diagnostics (Basel, Switzerland) · 2026Review
- Colorectal Cancer: A Landscape of New Potential Radiopharmaceuticals.Molecular diagnosis & therapy · 2026Review
- Radionuclide-based pharmaceuticals for breast cancer imaging: state of the art.EJNMMI radiopharmacy and chemistry · 2026Review
- Comparison between [EJNMMI research · 2026Article
- Preclinical evaluation of DOTAGA.Glu.(FAPI)European journal of nuclear medicine and molecular imaging · 2026Article
- Novel immunotheranostic FAP-inhibitor target modules for imaging and elimination of FAP-positive cells by UniCAR T-cells.Oncoimmunology · 2025Article
- FAPI TracerPharmaceuticals (Basel, Switzerland) · 2025Article
- Fibroblast Activation Protein-Targeted Theranostics: Current Status in Clinical Development.Nuclear medicine and molecular imaging · 2025Review
- Fibroblast activation protein targeting radiopharmaceuticals: From drug design to clinical translation.Acta pharmaceutica Sinica. B · 2025Review
- Preclinical evaluation of [EJNMMI radiopharmacy and chemistry · 2025Article
- Improved FAPI-radiopharmaceutical pharmacokinetics from the perspectives of a dose escalation study.European journal of nuclear medicine and molecular imaging · 2025Article
- Molecular Imaging of Fibroblast Activation Protein in Response to Cardiac Injury Using [Pharmaceuticals (Basel, Switzerland) · 2025Article
- Review
5 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
15 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundFibroblast activation protein (FAP) is a proline selective serine protease that is overexpressed in tumor stroma and in lesions of many other diseases that are characterized by tissue remodeling. In 2014, a most potent FAP-inhibitor (referred to as UAMC1110) with low nanomolar FAP-affinity and high selectivity toward related enzymes such as prolyl oligopeptidase (PREP) and the dipeptidyl-peptidases (DPPs): DPP4, DPP8/9 and DPP2 were developed. This inhibitor has been adopted recently by other groups to create radiopharmaceuticals by coupling bifunctional chelator-linker systems. Here, we report squaric acid (SA) containing bifunctional DATA
results[
conclusionIn this work, novel PET radiotracers targeting fibroblast activation protein were synthesized and biochemically investigated. Critical substructures of the novel compounds are a squaramide linker unit derived from the basic motif of squaric acid, DOTA and DATA
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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 OpenQuestion graph.