ArticleEuropean journal of nuclear medicine and molecular imaging2022
Fatty acid-conjugated radiopharmaceuticals for fibroblast activation protein-targeted radiotherapy.
Article in European journal of nuclear medicine and molecular imaging, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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Who cites it
37 citing papers in PubMed, 76 citations in OpenAlex.
- Coumarin Conjugation as an Albumin-Binding Strategy to Modulate the Pharmacokinetics of FAPI Radiotracers.ACS omega · 2026Article
- Unraveling the roles of fibroblast activation protein‑positive cancer‑associated fibroblasts in cancer: From mechanisms to therapy (Review).International journal of oncology · 2026Review
- Bridging the gaps in fibroblast activation protein targeted radionuclide therapy: a translational perspective.European journal of nuclear medicine and molecular imaging · 2026Review
- Design, Synthesis, and Evaluation of OncoFAP Derivatives with the Albumin Binder as Novel Antitumor Radiopharmaceuticals.Chemical & biomedical imaging · 2026Article
- Linker Chemistry in Radiopharmaceutical Design.Bioconjugate chemistry · 2026Review
- Enhanced in-vivo persistence and PET imaging performance of [EJNMMI research · 2026Article
- Article
- Enhanced Radionuclide Therapy via the Conjugation of Pentadecanoic Acids WithCancer science · 2026Article
- The role of the tumor microenvironment in mediating radiopharmaceutical therapy: bridging nuclear medicine and cancer immunotherapy.Military Medical Research · 2026Review
- Fibroblast activation protein inhibitor radiotheranostics for imaging activated tumor stroma and guiding radionuclide therapy.Frontiers in oncology · 2026Review
- Radionuclide-labeled nanomaterials for tumor therapy: Recent progress and perspectives.Materials today. Bio · 2025Review
- 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
- A heterodimeric radioligand labeled with gallium-68 targeting fibroblast activation protein.EJNMMI research · 2025Article
- Radioiodinated Bicyclic RGD Peptide Derivatives for Enhanced Tumor Accumulation.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Radiopharmaceuticals and their applications in medicine.Signal transduction and targeted therapy · 2025Review
- Based on small molecules: development and application of fibroblast activation protein inhibitors radiopharmaceutical in tumor precision therapy.Frontiers in pharmacology · 2025Review
- Development and evaluation of albumin binder-conjugated heterodimeric radiopharmaceuticals targeting integrin αEuropean journal of nuclear medicine and molecular imaging · 2024Article
- [Pharmaceuticals (Basel, Switzerland) · 2024Article
- Article
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
introductionRadiopharmaceuticals that target cancer-associated fibroblasts (CAFs) have become an increasingly attractive strategy for cancer theranostics. Recently, a series of fibroblast activation protein inhibitor (FAPI)-based radiopharmaceuticals have been successfully applied to the diagnosis of a variety of cancers and exhibited excellent tumor selectivity. Nevertheless, CAF-targeted radionuclide therapy encounters difficulties in cancer treatment, as the tumor uptake and retention of FAPIs are insufficient. To meet this challenge, we tried to conjugate albumin-binding moiety to FAPI molecule for prolonged circulation that may increase the accumulation and retention of radiopharmaceuticals in tumor.
methodsTwo fatty acids, lauric acid (C12) and palmitic acid (C16), were conjugated to FAPI-04 to give two albumin-binding FAPI radiopharmaceuticals, denoted as FAPI-C12 and FAPI-C16, respectively. They had been radiolabeled with gallium-68, yttrium-86, and lutecium-177 for stability study, binding affinity assay, PET and SPECT imaging, biodistribution, and radionuclide therapy study to systematically evaluate their potential for CAF-targeted radionuclide therapy.
resultsFAPI-C12 and FAPI-C16 showed high binding affinity to FAP with the IC
conclusionThis proof-of-concept study validates the hypothesis that conjugation of albumin binders may shift the pharmacokinetics and enhance the tumor uptake of FAPI-based radiopharmaceuticals. This could be a general strategy to transform the diagnostic FAP-targeted radiopharmaceuticals into their therapeutic pairs.
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