ArticleProceedings of the National Academy of Sciences of the United States of America2021
An ultra-high-affinity small organic ligand of fibroblast activation protein for tumor-targeting applications.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 71 papers.
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Who cites it
71 citing papers in PubMed, 150 citations in OpenAlex.
- Preclinical evaluation of homodimeric FAPI target modules for UniCAR-mediated targeting of FAP-expressing tumor and stromal cells.Oncoimmunology · 2026Article
- Extracellularly Activatable Conjugates of RGD Peptidomimetics and Cryptophycin for αChemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- The Evolution of FAP-Targeted CAR T-Cell Therapy in Solid Tumors: From Immunotherapy to Immunotheranostic Applications.International journal of molecular sciences · 2026Review
- Unraveling the roles of fibroblast activation protein‑positive cancer‑associated fibroblasts in cancer: From mechanisms to therapy (Review).International journal of oncology · 2026Review
- Nanomedicine targeting ECM stiffness: restoring mechanical homeostasis for cancer immunotherapy.Materials today. Bio · 2026Review
- Article
- From DNA-Encoded Chemistry to Tumor-Targeted Small Molecule Therapeutics.Pharmaceuticals (Basel, Switzerland) · 2026Review
- FAP-targeted [European journal of nuclear medicine and molecular imaging · 2026Article
- A FAP-Targeted SMDC Platform Enables Synergistic Radionuclide-Chemotherapy with PET-Guided Evaluation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Design, Synthesis, and Evaluation of OncoFAP Derivatives with the Albumin Binder as Novel Antitumor Radiopharmaceuticals.Chemical & biomedical imaging · 2026Article
- Fibroblast activation protein inhibitor (FAPI) PET imaging in pulmonary fibrosis: pathophysiology, clinical utility, and emerging theranostic applications.Respiratory research · 2026Review
- FAP-Anchored Retinoic Acid Nanoparticles for Stromal Reprogramming and Enhanced Intratumoral Oxaliplatin Delivery in Fibrotic Colorectal Tumours.Biosensors · 2026Article
- Comparison between [EJNMMI research · 2026Article
- The extracellular matrix in inflammation and cancer.Molecular biomedicine · 2026Review
- A newEJNMMI radiopharmacy and chemistry · 2026Article
- Novel immunotheranostic FAP-inhibitor target modules for imaging and elimination of FAP-positive cells by UniCAR T-cells.Oncoimmunology · 2025Article
- Developing a theranostic nanobody targeting FAP for cancer imaging and therapy.EJNMMI radiopharmacy and chemistry · 2025Article
- Small-molecule control of CAR T cells.Nature reviews. Chemistry · 2025Review
- Generation and characterization of novel high-affinity fully human antibodies targeting prostate-specific membrane antigen and prostatic acid phosphatase.Antibody therapeutics · 2025Article
- Fibroblast activation protein targeting radiopharmaceuticals: From drug design to clinical translation.Acta pharmaceutica Sinica. B · 2025Review
11 more citing papers are in PubMed but not listed here.
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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
We describe the development of OncoFAP, an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential. OncoFAP binds to human FAP with affinity in the subnanomolar concentration range and cross-reacts with the murine isoform of the protein. We generated various fluorescent and radiolabeled derivatives of OncoFAP in order to study biodistribution properties and tumor-targeting performance in preclinical models. Fluorescent derivatives selectively localized in FAP-positive tumors implanted in nude mice with a rapid and homogeneous penetration within the neoplastic tissue. Quantitative in vivo biodistribution studies with a lutetium-177-labeled derivative of OncoFAP revealed a preferential localization in tumors at doses of up to 1,000 nmol/kg. More than 30% of the injected dose had already accumulated in 1 g of tumor 10 min after intravenous injection and persisted for at least 3 h with excellent tumor-to-organ ratios. OncoFAP also served as a modular component for the generation of nonradioactive therapeutic products. A fluorescein conjugate mediated a potent and FAP-dependent tumor cell killing activity in combination with chimeric antigen receptor (CAR) T cells specific to fluorescein. Similarly, a conjugate of OncoFAP with the monomethyl auristatin E-based Vedotin payload was well tolerated and cured tumor-bearing mice in combination with a clinical-stage antibody-interleukin-2 fusion. Collectively, these data support the development of OncoFAP-based products for tumor-targeting applications in patients with cancer.
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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.