ArticleMolecular imaging and biology2021
A Trifunctional Theranostic Ligand Targeting Fibroblast Activation Protein-α (FAPα).
Article in Molecular imaging and biology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 32 citations in OpenAlex.
- Fibroblast Activation Protein Inhibitor (FAPI) PET: A Scoping Review of Emerging Oncologic and Fibroinflammatory Applications.Diagnostics (Basel, Switzerland) · 2026Review
- Branching beyond bifunctional linkers: synthesis of macrocyclic and trivalent PROTACs.Nature protocols · 2026Review
- Fibroblast activation protein targeting radiopharmaceuticals: From drug design to clinical translation.Acta pharmaceutica Sinica. B · 2025Review
- Development and Application of Radioactive Ligands Targeting Fibroblasts with Albumin-Binding Sites.Molecular cancer therapeutics · 2025Article
- Improved FAPI-radiopharmaceutical pharmacokinetics from the perspectives of a dose escalation study.European journal of nuclear medicine and molecular imaging · 2025Article
- Based on small molecules: development and application of fibroblast activation protein inhibitors radiopharmaceutical in tumor precision therapy.Frontiers in pharmacology · 2025Review
- [Molecular imaging and biology · 2024Article
- Tailoring Fibroblast-Activation Protein Targeting for Theranostics: A Comparative Preclinical Evaluation of theMolecules (Basel, Switzerland) · 2024Article
- Translational assessment of a DATA-functionalized FAP inhibitor with facileEuropean journal of nuclear medicine and molecular imaging · 2023Article
- FAPI PET/CT Imaging-An Updated Review.Diagnostics (Basel, Switzerland) · 2023Review
- Synthesis and Preclinical Evaluation of NovelPharmaceuticals (Basel, Switzerland) · 2023Article
- Synthesis and Evaluation ofMolecules (Basel, Switzerland) · 2023Article
- Albumin-Mediated Size Exclusion Chromatography: The Apparent Molecular Weight of PSMA Radioligands as Novel Parameter to Estimate Their Blood Clearance Kinetics.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy.European journal of nuclear medicine and molecular imaging · 2022Article
- Albumin Binder-Conjugated Fibroblast Activation Protein Inhibitor Radiopharmaceuticals for Cancer Therapy.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Article
- Review
- New Frontiers in Cancer Imaging and Therapy Based on Radiolabeled Fibroblast Activation Protein Inhibitors: A Rational Review and Current Progress.Pharmaceuticals (Basel, Switzerland) · 2021Review
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeFibroblast activation protein-α (FAPα) is uniquely expressed in activated fibroblasts, including cancer-associated fibroblasts that populate tumor stroma and contribute to proliferation and immunosuppression. Radiolabeled FAPα inhibitors enable imaging of multiple human cancers, but time-dependent clearance from tumors currently limits their utility as FAPα-targeted radiotherapeutics. We sought to increase the area under the curve (AUC) by constructing a trifunctional ligand that binds FAPα with high affinity and also binds albumin and theranostic radiometals. PROCEDURES: RPS-309 comprised a FAPα-targeting moiety, an albumin-binding group, and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA). Inhibition of recombinant human FAPα (rhFAPα) was determined by colorimetric assay. Affinity for human serum albumin (HSA) was determined by high-performance affinity chromatography. The tissue distribution of [
resultsRPS-309 inhibits rhFAPα with IC
conclusionsRPS-309 is a high-affinity FAPα inhibitor with prolonged plasma residence. Introduction of the albumin-binding group did not compromise FAPα binding. Although initial tumor uptake was high and FAPα-specific, RPS-309 also progressively cleared from tumors. Nevertheless, RPS-309 incorporates multiple sites in which structural diversity can be introduced, and therefore serves as a platform for future structure-activity relationship studies.
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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.